Target family: Adrenoceptors (type: gpcr)
Target: &alpha;<sub>1A</sub>-adrenoceptor

Ligand: 5-methylurapidil (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological pleiotropism of the human recombinant alpha1A-adrenoceptor: implications for alpha1-adrenoceptor classification.
Published in: Br J Pharmacol

Ligand: 5-methylurapidil (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Affinity of serotonin receptor antagonists and agonists to recombinant and native alpha1-adrenoceptor subtypes.
Published in: Jpn J Pharmacol

Ligand: 5-methylurapidil (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): KMD-3213, a novel, potent, alpha 1a-adrenoceptor-selective antagonist: characterization using recombinant human alpha 1-adrenoceptors and native tissues.
Published in: Mol Pharmacol

Ligand: 5-methylurapidil (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants, and antipsychotics for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: 5-methylurapidil (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Molecular cloning, genomic characterization and expression of novel human alpha1A-adrenoceptor isoforms.
Published in: FEBS Lett

Ligand: 5-methylurapidil (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Structure activity relationships of a series of buspirone analogs at alpha-1 adrenoceptors: further evidence that rat aorta alpha-1 adrenoceptors are of the alpha-1D-subtype.
Published in: J Pharmacol Exp Ther

Ligand: 5-methylurapidil (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9 pKi
Reference (Journal): Phe-308 and Phe-312 in transmembrane domain 7 are major sites of alpha 1-adrenergic receptor antagonist binding. Imidazoline agonists bind like antagonists.
Published in: J Biol Chem

Ligand: 5-methylurapidil (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of the uroselective alpha-1 antagonist Rec 15/2739 (SB 216469): role of the alpha-1L adrenoceptor in tissue selectivity, part I.
Published in: J Pharmacol Exp Ther

Ligand: A-119637 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.600000381469727 pKi
Reference (Journal): Two novel and potent 3-[(o-methoxyphenyl)piperazinylethyl]-5-phenylthien.
Published in: Bioorg Med Chem Lett

Ligand: A-119637 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.6 pKi
Reference (Journal): Two novel and potent 3-[(o-methoxyphenyl)piperazinylethyl]-5-phenylthien.
Published in: Bioorg Med Chem Lett

Ligand: A-123189 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.5 pKi
Reference (Journal): Two novel and potent 3-[(o-methoxyphenyl)piperazinylethyl]-5-phenylthien.
Published in: Bioorg Med Chem Lett

Ligand: A-123189 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.4 pKi
Reference (Journal): Two novel and potent 3-[(o-methoxyphenyl)piperazinylethyl]-5-phenylthien.
Published in: Bioorg Med Chem Lett

Ligand: A61603 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Quantification of functional selectivity at the human α(1A)-adrenoceptor.
Published in: Mol Pharmacol

Ligand: A61603 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Quantification of functional selectivity at the human α(1A)-adrenoceptor.
Published in: Mol Pharmacol

Ligand: A61603 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): A-61603, a potent alpha 1-adrenergic receptor agonist, selective for the alpha 1A receptor subtype.
Published in: J Pharmacol Exp Ther

Ligand: A61603 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Factors influencing biased agonism in recombinant cells expressing the human α<sub>1A</sub> -adrenoceptor.
Published in: Br J Pharmacol

Ligand: A61603 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: A61603 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): A-61603, a potent alpha 1-adrenergic receptor agonist, selective for the alpha 1A receptor subtype.
Published in: J Pharmacol Exp Ther

Ligand: A61603 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological pleiotropism of the human recombinant alpha1A-adrenoceptor: implications for alpha1-adrenoceptor classification.
Published in: Br J Pharmacol

Ligand: A61603 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Factors influencing biased agonism in recombinant cells expressing the human α<sub>1A</sub> -adrenoceptor.
Published in: Br J Pharmacol

Ligand: A61603 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): The selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: (+)-adrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 5 pKi
Reference (Journal): Cloning and pharmacological characterization of human alpha-1 adrenergic receptors: sequence corrections and direct comparison with other species homologues.
Published in: J Pharmacol Exp Ther

Ligand: (-)-adrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (no history prior to 1951)
Primary target: no
Median affinity:  pKi
Reference (Journal): Cloning and pharmacological characterization of human alpha-1 adrenergic receptors: sequence corrections and direct comparison with other species homologues.
Published in: J Pharmacol Exp Ther

Ligand: (-)-adrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (no history prior to 1951)
Primary target: no
Median affinity:  pKi
Reference (Journal): Selectivity of the imidazoline alpha-adrenoceptor agonists (oxymetazoline and cirazoline) for human cloned alpha 1-adrenoceptor subtypes.
Published in: Br J Pharmacol

Ligand: (-)-adrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (no history prior to 1951)
Primary target: no
Median affinity:  pEC50
Reference (Journal): The selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: (-)-adrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (no history prior to 1951)
Primary target: no
Median affinity:  pKi
Reference (Journal): KMD-3213, a novel, potent, alpha 1a-adrenoceptor-selective antagonist: characterization using recombinant human alpha 1-adrenoceptors and native tissues.
Published in: Mol Pharmacol

Ligand: (-)-adrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (no history prior to 1951)
Primary target: no
Median affinity:  pKi
Reference (Journal): The selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: alfuzosin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2003)
Primary target: yes
Median affinity:  pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants, and antipsychotics for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: alfuzosin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2003)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Adrenoceptor subclassification: an approach to improved cardiovascular therapeutics.
Published in: Pharm Acta Helv

Ligand: alfuzosin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2003)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Revisiting the Pharmacodynamic Uroselectivity of <i>&#x3b1;</i> <sub>1</sub>-Adrenergic Receptor Antagonists.
Published in: J Pharmacol Exp Ther

Ligand: amitriptyline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1961)
Primary target: no
Median affinity: 8.199999809265137 pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants, and antipsychotics for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: BMY-7378 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants, and antipsychotics for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: BMY-7378 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Affinity of serotonin receptor antagonists and agonists to recombinant and native alpha1-adrenoceptor subtypes.
Published in: Jpn J Pharmacol

Ligand: BMY-7378 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Two novel and potent 3-[(o-methoxyphenyl)piperazinylethyl]-5-phenylthien.
Published in: Bioorg Med Chem Lett

Ligand: BMY-7378 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7 pKi
Reference (Journal): Two novel and potent 3-[(o-methoxyphenyl)piperazinylethyl]-5-phenylthien.
Published in: Bioorg Med Chem Lett

Ligand: BODIPY FL-prazosin (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pKi
Reference (Journal): The alpha 1B/D-adrenoceptor knockout mouse permits isolation of the vascular alpha 1A-adrenoceptor and elucidates its relationship to the other subtypes.
Published in: Br J Pharmacol

Ligand: cabergoline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1996)
Median affinity: 6.5 pKi
Reference (Journal): Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
Published in: J Pharmacol Exp Ther

Ligand: carvedilol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1995)
Primary target: no
Median affinity: 8.399999618530273 pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants, and antipsychotics for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: cirazoline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: cirazoline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): The selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: cirazoline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Quantification of functional selectivity at the human α(1A)-adrenoceptor.
Published in: Mol Pharmacol

Ligand: cirazoline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Quantification of functional selectivity at the human α(1A)-adrenoceptor.
Published in: Mol Pharmacol

Ligand: clomipramine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1989)
Primary target: no
Median affinity: 8.100000381469727 pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants, and antipsychotics for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: clozapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1989)
Primary target: no
Median affinity:  pKi
Reference (Journal): Affinity of serotonin receptor antagonists and agonists to recombinant and native alpha1-adrenoceptor subtypes.
Published in: Jpn J Pharmacol

Ligand: clozapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1989)
Primary target: no
Median affinity:  pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants, and antipsychotics for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: (+)-cyclazosin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants, and antipsychotics for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: (+)-cyclazosin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Synthesis and biological profile of the enantiomers of [4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-cis-octahydroquinoxalin- 1-yl]furan-2-ylmethanone (cyclazosin), a potent competitive alpha 1B- adrenoceptor antagonist.
Published in: J Med Chem

Ligand: cyproheptadine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1961)
Median affinity: 7.4 pKi
Reference (Journal): Affinity of serotonin receptor antagonists and agonists to recombinant and native alpha1-adrenoceptor subtypes.
Published in: Jpn J Pharmacol

Ligand: dabuzalgron (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.400000095367432 pKi
Reference (Journal): Pharmacological characteristics of Ro 115-1240, a selective alpha1A/1L-adrenoceptor partial agonist: a potential therapy for stress urinary incontinence.
Published in: BJU Int

Ligand: doxazosin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1990)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Revisiting the Pharmacodynamic Uroselectivity of <i>&#x3b1;</i> <sub>1</sub>-Adrenergic Receptor Antagonists.
Published in: J Pharmacol Exp Ther

Ligand: doxazosin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1990)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of A-131701, a novel R 1 -adrenoceptor antagonist selective for R 1A - and R 1D - compared to R 1B -adrenoceptors.
Published in: Drug Development Research

Ligand: doxazosin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1990)
Primary target: yes
Median affinity:  pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants, and antipsychotics for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: HEAT (BE2254) (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.600000381469727 pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants, and antipsychotics for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: indoramin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: UK (1993)
Primary target: no
Median affinity: 8.399999618530273 pKi
Reference (Journal): Pharmacological pleiotropism of the human recombinant alpha1A-adrenoceptor: implications for alpha1-adrenoceptor classification.
Published in: Br J Pharmacol

Ligand: indoramin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: UK (1993)
Primary target: no
Median affinity: 8.399999618530273 pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants, and antipsychotics for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: indoramin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: UK (1993)
Primary target: no
Median affinity: 8.399999618530273 pKi
Reference (Journal): Human cloned alpha1A-adrenoceptor isoforms display alpha1L-adrenoceptor pharmacology in functional studies.
Published in: Eur J Pharmacol

Ligand: ketanserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity: 8.2 pKi
Reference (Journal): Affinity of serotonin receptor antagonists and agonists to recombinant and native alpha1-adrenoceptor subtypes.
Published in: Jpn J Pharmacol

Ligand: KMUP-1 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.690000057220459 pKi
Reference (Journal): cGMP-enhancing- and alpha1A/alpha1D-adrenoceptor blockade-derived inhibition of Rho-kinase by KMUP-1 provides optimal prostate relaxation and epithelial cell anti-proliferation efficacy.
Published in: Prostate

Ligand: labetalol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1984)
Primary target: no
Median affinity:  pIC50
Reference (Journal): The selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: labetalol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1984)
Primary target: no
Median affinity: 7.300000190734863 pKi
Reference (Journal): The selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: lisuride (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2011)
Primary target: no
Median affinity:  pKi
Reference (Journal): Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
Published in: J Pharmacol Exp Ther

Ligand: lisuride (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2011)
Primary target: no
Median affinity:  pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants, and antipsychotics for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: methoxamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Primary target: yes
Median affinity:  pKi
Reference (Journal): Factors influencing biased agonism in recombinant cells expressing the human α<sub>1A</sub> -adrenoceptor.
Published in: Br J Pharmacol

Ligand: methoxamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Primary target: yes
Median affinity:  pKi
Reference (Journal): The selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: methoxamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Primary target: no
Median affinity:  pEC50
Reference (Journal): Factors influencing biased agonism in recombinant cells expressing the human α<sub>1A</sub> -adrenoceptor.
Published in: Br J Pharmacol

Ligand: methoxamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Primary target: yes
Median affinity:  pKi
Reference (Journal): KMD-3213, a novel, potent, alpha 1a-adrenoceptor-selective antagonist: characterization using recombinant human alpha 1-adrenoceptors and native tissues.
Published in: Mol Pharmacol

Ligand: methoxamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Primary target: no
Median affinity:  pEC50
Reference (Journal): The selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: methoxamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Primary target: yes
Median affinity:  pKi
Reference (Journal): Cloning and pharmacological characterization of human alpha-1 adrenergic receptors: sequence corrections and direct comparison with other species homologues.
Published in: J Pharmacol Exp Ther

Ligand: methoxamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Primary target: yes
Median affinity:  pKi
Reference (Journal): Quantification of functional selectivity at the human α(1A)-adrenoceptor.
Published in: Mol Pharmacol

Ligand: methoxamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Primary target: yes
Median affinity:  pKi
Reference (Journal): Microphysiometric analysis of human alpha1a-adrenoceptor expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: methoxamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Primary target: no
Median affinity:  pEC50
Reference (Journal): Quantification of functional selectivity at the human α(1A)-adrenoceptor.
Published in: Mol Pharmacol

Ligand: mianserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity: 7.6 pKi
Reference (Journal): Affinity of serotonin receptor antagonists and agonists to recombinant and native alpha1-adrenoceptor subtypes.
Published in: Jpn J Pharmacol

Ligand: NAN 190 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 10.100000381469727 pKi
Reference (Journal): Affinity of serotonin receptor antagonists and agonists to recombinant and native alpha1-adrenoceptor subtypes.
Published in: Jpn J Pharmacol

Ligand: naphazoline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1971, prior history not available)
Primary target: no
Median affinity: 6.5 pKi
Reference (Journal): The selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: naphazoline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1971, prior history not available)
Primary target: no
Median affinity:  pEC50
Reference (Journal): The selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: (-)-noradrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1950)
Primary target: no
Median affinity:  pKi
Reference (Journal): Factors influencing biased agonism in recombinant cells expressing the human α<sub>1A</sub> -adrenoceptor.
Published in: Br J Pharmacol

Ligand: (-)-noradrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1950)
Primary target: no
Median affinity:  pEC50
Reference (Journal): The selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: (-)-noradrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1950)
Primary target: no
Median affinity:  pKi
Reference (Journal): The selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: (-)-noradrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1950)
Primary target: no
Median affinity:  pKi
Reference (Journal): KMD-3213, a novel, potent, alpha 1a-adrenoceptor-selective antagonist: characterization using recombinant human alpha 1-adrenoceptors and native tissues.
Published in: Mol Pharmacol

Ligand: (-)-noradrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1950)
Primary target: no
Median affinity:  pEC50
Reference (Journal): Factors influencing biased agonism in recombinant cells expressing the human α<sub>1A</sub> -adrenoceptor.
Published in: Br J Pharmacol

Ligand: (-)-noradrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1950)
Primary target: no
Median affinity:  pKi
Reference (Journal): Microphysiometric analysis of human alpha1a-adrenoceptor expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: (-)-noradrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1950)
Primary target: no
Median affinity:  pKi
Reference (Journal): Quantification of functional selectivity at the human α(1A)-adrenoceptor.
Published in: Mol Pharmacol

Ligand: (-)-noradrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1950)
Primary target: no
Median affinity:  pEC50
Reference (Journal): Quantification of functional selectivity at the human α(1A)-adrenoceptor.
Published in: Mol Pharmacol

Ligand: (-)-noradrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1950)
Primary target: no
Median affinity:  pKi
Reference (Journal): Cloning and pharmacological characterization of human alpha-1 adrenergic receptors: sequence corrections and direct comparison with other species homologues.
Published in: J Pharmacol Exp Ther

Ligand: (-)-noradrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1950)
Primary target: no
Median affinity:  pKi
Reference (Journal): Selectivity of the imidazoline alpha-adrenoceptor agonists (oxymetazoline and cirazoline) for human cloned alpha 1-adrenoceptor subtypes.
Published in: Br J Pharmacol

Ligand: nortriptyline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1964)
Primary target: no
Median affinity: 8.199999809265137 pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants, and antipsychotics for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: NS-49 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 6.199999809265137 pKi
Reference (Journal): NS-49, a novel alpha 1a-adrenoceptor-selective agonist characterization using recombinant human alpha 1-adrenoceptors.
Published in: Eur J Pharmacol

Ligand: olanzapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA & FDA (1996)
Primary target: no
Median affinity: 7.400000095367432 pA2
Reference (Journal): Orthostatic hypotensive effect of antipsychotic drugs in Wistar rats by in vivo and in vitro studies of alpha1-adrenoceptor function.
Published in: Psychopharmacology (Berl.)

Ligand: oxymetazoline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1986)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Selectivity of the imidazoline alpha-adrenoceptor agonists (oxymetazoline and cirazoline) for human cloned alpha 1-adrenoceptor subtypes.
Published in: Br J Pharmacol

Ligand: oxymetazoline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1986)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Cloning and pharmacological characterization of human alpha-1 adrenergic receptors: sequence corrections and direct comparison with other species homologues.
Published in: J Pharmacol Exp Ther

Ligand: oxymetazoline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1986)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Quantification of functional selectivity at the human α(1A)-adrenoceptor.
Published in: Mol Pharmacol

Ligand: oxymetazoline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1986)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Microphysiometric analysis of human alpha1a-adrenoceptor expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: oxymetazoline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1986)
Primary target: no
Median affinity:  pEC50
Reference (Journal): Quantification of functional selectivity at the human α(1A)-adrenoceptor.
Published in: Mol Pharmacol

Ligand: oxymetazoline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1986)
Primary target: yes
Median affinity:  pKi
Reference (Journal): NS-49, a novel alpha 1a-adrenoceptor-selective agonist characterization using recombinant human alpha 1-adrenoceptors.
Published in: Eur J Pharmacol

Ligand: oxymetazoline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1986)
Primary target: yes
Median affinity:  pKi
Reference (Journal): KMD-3213, a novel, potent, alpha 1a-adrenoceptor-selective antagonist: characterization using recombinant human alpha 1-adrenoceptors and native tissues.
Published in: Mol Pharmacol

Ligand: oxymetazoline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1986)
Primary target: no
Median affinity:  pEC50
Reference (Journal): Factors influencing biased agonism in recombinant cells expressing the human α<sub>1A</sub> -adrenoceptor.
Published in: Br J Pharmacol

Ligand: oxymetazoline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1986)
Primary target: no
Median affinity:  pEC50
Reference (Journal): The selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: oxymetazoline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1986)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Factors influencing biased agonism in recombinant cells expressing the human α<sub>1A</sub> -adrenoceptor.
Published in: Br J Pharmacol

Ligand: oxymetazoline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1986)
Primary target: yes
Median affinity:  pKi
Reference (Journal): The selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: phentolamine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1952)
Primary target: yes
Median affinity:  pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants, and antipsychotics for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: phentolamine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1952)
Primary target: yes
Median affinity:  pKi
Reference (Journal): KMD-3213, a novel, potent, alpha 1a-adrenoceptor-selective antagonist: characterization using recombinant human alpha 1-adrenoceptors and native tissues.
Published in: Mol Pharmacol

Ligand: phentolamine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1952)
Primary target: no
Median affinity: 8.100000381469727 pKi
Reference (Journal): Phe-308 and Phe-312 in transmembrane domain 7 are major sites of alpha 1-adrenergic receptor antagonist binding. Imidazoline agonists bind like antagonists.
Published in: J Biol Chem

Ligand: phenylephrine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1952)
Primary target: no
Median affinity:  pEC50
Reference (Journal): Quantification of functional selectivity at the human α(1A)-adrenoceptor.
Published in: Mol Pharmacol

Ligand: phenylephrine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1952)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Microphysiometric analysis of human alpha1a-adrenoceptor expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: phenylephrine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1952)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Quantification of functional selectivity at the human α(1A)-adrenoceptor.
Published in: Mol Pharmacol

Ligand: phenylephrine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1952)
Primary target: yes
Median affinity:  pKi
Reference (Journal): The selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: phenylephrine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1952)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Factors influencing biased agonism in recombinant cells expressing the human α<sub>1A</sub> -adrenoceptor.
Published in: Br J Pharmacol

Ligand: phenylephrine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1952)
Primary target: no
Median affinity:  pEC50
Reference (Journal): Factors influencing biased agonism in recombinant cells expressing the human α<sub>1A</sub> -adrenoceptor.
Published in: Br J Pharmacol

Ligand: phenylephrine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1952)
Primary target: no
Median affinity:  pEC50
Reference (Journal): The selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: piribedil (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.1 pKi
Reference (Journal): Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
Published in: J Pharmacol Exp Ther

Ligand: prazosin (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1976)
Primary target: yes
Median affinity:  pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants, and antipsychotics for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: prazosin (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1976)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Pharmacological pleiotropism of the human recombinant alpha1A-adrenoceptor: implications for alpha1-adrenoceptor classification.
Published in: Br J Pharmacol

Ligand: prazosin (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1976)
Primary target: yes
Median affinity:  pKi
Reference (Journal): KMD-3213, a novel, potent, alpha 1a-adrenoceptor-selective antagonist: characterization using recombinant human alpha 1-adrenoceptors and native tissues.
Published in: Mol Pharmacol

Ligand: prazosin (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1976)
Median affinity: 9.5 pKi
Reference (Journal): Phe-308 and Phe-312 in transmembrane domain 7 are major sites of alpha 1-adrenergic receptor antagonist binding. Imidazoline agonists bind like antagonists.
Published in: J Biol Chem

Ligand: prazosin (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1976)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Molecular cloning, genomic characterization and expression of novel human alpha1A-adrenoceptor isoforms.
Published in: FEBS Lett

Ligand: prazosin (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1976)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Human cloned alpha1A-adrenoceptor isoforms display alpha1L-adrenoceptor pharmacology in functional studies.
Published in: Eur J Pharmacol

Ligand: prazosin (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1976)
Primary target: yes
Median affinity:  pKi
Reference (Journal): In vitro alpha1-adrenoceptor pharmacology of Ro 70-0004 and RS-100329, novel alpha1A-adrenoceptor selective antagonists.
Published in: Br J Pharmacol

Ligand: ρ-Da1a (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Isolation and pharmacological characterization of AdTx1, a natural peptide displaying specific insurmountable antagonism of the alpha1A-adrenoceptor.
Published in: Br J Pharmacol

Ligand: ρ-Da1a (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Orthosteric binding of ρ-Da1a, a natural peptide of snake venom interacting selectively with the α1A-adrenoceptor.
Published in: PLoS ONE

Ligand: rho-TIA (Peptide)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 5 pKi
Reference (Journal): Allosteric alpha 1-adrenoreceptor antagonism by the conopeptide rho-TIA.
Published in: J Biol Chem

Ligand: risperidone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1993), EMA (2022)
Primary target: no
Median affinity:  pKi
Reference (Journal): Affinity of serotonin receptor antagonists and agonists to recombinant and native alpha1-adrenoceptor subtypes.
Published in: Jpn J Pharmacol

Ligand: risperidone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1993), EMA (2022)
Primary target: no
Median affinity:  pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants, and antipsychotics for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: ritanserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.4 pKi
Reference (Journal): Affinity of serotonin receptor antagonists and agonists to recombinant and native alpha1-adrenoceptor subtypes.
Published in: Jpn J Pharmacol

Ligand: Ro-70-0004 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.899999618530273 pKi
Reference (Journal): In vitro alpha1-adrenoceptor pharmacology of Ro 70-0004 and RS-100329, novel alpha1A-adrenoceptor selective antagonists.
Published in: Br J Pharmacol

Ligand: roxindole (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.600000381469727 pKi
Reference (Journal): Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
Published in: J Pharmacol Exp Ther

Ligand: RS-100329 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.600000381469727 pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants, and antipsychotics for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: RS-100329 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.600000381469727 pKi
Reference (Journal): In vitro alpha1-adrenoceptor pharmacology of Ro 70-0004 and RS-100329, novel alpha1A-adrenoceptor selective antagonists.
Published in: Br J Pharmacol

Ligand: RS-17053 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Human cloned alpha1A-adrenoceptor isoforms display alpha1L-adrenoceptor pharmacology in functional studies.
Published in: Eur J Pharmacol

Ligand: RS-17053 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants, and antipsychotics for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: RS-17053 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological pleiotropism of the human recombinant alpha1A-adrenoceptor: implications for alpha1-adrenoceptor classification.
Published in: Br J Pharmacol

Ligand: RS-17053 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Molecular cloning, genomic characterization and expression of novel human alpha1A-adrenoceptor isoforms.
Published in: FEBS Lett

Ligand: RS-17053 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): RS-17053 (N-[2-(2-cyclopropylmethoxyphenoxy)ethyl]-5-chloro-alpha, alpha-dimethyl-1H-indole-3-ethanamine hydrochloride), a selective alpha 1A-adrenoceptor antagonist, displays low affinity for functional alpha 1-adrenoceptors in human prostate: implications for adrenoceptor classification.
Published in: Mol Pharmacol

Ligand: silodosin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2008), EMA (2010)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Revisiting the Pharmacodynamic Uroselectivity of <i>&#x3b1;</i> <sub>1</sub>-Adrenergic Receptor Antagonists.
Published in: J Pharmacol Exp Ther

Ligand: silodosin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2008), EMA (2010)
Primary target: yes
Median affinity:  pKi
Reference (Journal): KMD-3213, a novel, potent, alpha 1a-adrenoceptor-selective antagonist: characterization using recombinant human alpha 1-adrenoceptors and native tissues.
Published in: Mol Pharmacol

Ligand: silodosin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2008), EMA (2010)
Primary target: yes
Median affinity:  pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants, and antipsychotics for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: SNAP5089 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants, and antipsychotics for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: SNAP5089 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Discovery of alpha 1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine.
Published in: J Med Chem

Ligand: SNAP5089 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Adrenoceptor subclassification: an approach to improved cardiovascular therapeutics.
Published in: Pharm Acta Helv

Ligand: SNAP5089 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of the uroselective alpha-1 antagonist Rec 15/2739 (SB 216469): role of the alpha-1L adrenoceptor in tissue selectivity, part I.
Published in: J Pharmacol Exp Ther

Ligand: S(+)-niguldipine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.3 pKi
Reference (Journal): Phe-308 and Phe-312 in transmembrane domain 7 are major sites of alpha 1-adrenergic receptor antagonist binding. Imidazoline agonists bind like antagonists.
Published in: J Biol Chem

Ligand: S(+)-niguldipine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): KMD-3213, a novel, potent, alpha 1a-adrenoceptor-selective antagonist: characterization using recombinant human alpha 1-adrenoceptors and native tissues.
Published in: Mol Pharmacol

Ligand: S(+)-niguldipine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants, and antipsychotics for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: S(+)-niguldipine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological pleiotropism of the human recombinant alpha1A-adrenoceptor: implications for alpha1-adrenoceptor classification.
Published in: Br J Pharmacol

Ligand: spiperone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.3 pKi
Reference (Journal): Affinity of serotonin receptor antagonists and agonists to recombinant and native alpha1-adrenoceptor subtypes.
Published in: Jpn J Pharmacol

Ligand: spiroxatrine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Affinity of serotonin receptor antagonists and agonists to recombinant and native alpha1-adrenoceptor subtypes.
Published in: Jpn J Pharmacol

Ligand: spiroxatrine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants, and antipsychotics for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: [125I]HEAT (BE2254) (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): KMD-3213, a novel, potent, alpha 1a-adrenoceptor-selective antagonist: characterization using recombinant human alpha 1-adrenoceptors and native tissues.
Published in: Mol Pharmacol

Ligand: [125I]HEAT (BE2254) (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Orthosteric binding of ρ-Da1a, a natural peptide of snake venom interacting selectively with the α1A-adrenoceptor.
Published in: PLoS ONE

Ligand: [125I]HEAT (BE2254) (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): NS-49, a novel alpha 1a-adrenoceptor-selective agonist characterization using recombinant human alpha 1-adrenoceptors.
Published in: Eur J Pharmacol

Ligand: [3H]prazosin (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 9.100000381469727 pKd
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants, and antipsychotics for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: tamsulosin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1997)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Pharmacological pleiotropism of the human recombinant alpha1A-adrenoceptor: implications for alpha1-adrenoceptor classification.
Published in: Br J Pharmacol

Ligand: tamsulosin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1997)
Primary target: yes
Median affinity:  pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants, and antipsychotics for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: tamsulosin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1997)
Primary target: yes
Median affinity:  pKi
Reference (Journal): KMD-3213, a novel, potent, alpha 1a-adrenoceptor-selective antagonist: characterization using recombinant human alpha 1-adrenoceptors and native tissues.
Published in: Mol Pharmacol

Ligand: tamsulosin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1997)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Human cloned alpha1A-adrenoceptor isoforms display alpha1L-adrenoceptor pharmacology in functional studies.
Published in: Eur J Pharmacol

Ligand: tamsulosin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1997)
Primary target: yes
Median affinity:  pKi
Reference (Journal): In vitro alpha1-adrenoceptor pharmacology of Ro 70-0004 and RS-100329, novel alpha1A-adrenoceptor selective antagonists.
Published in: Br J Pharmacol

Ligand: tamsulosin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1997)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Cloning and pharmacological characterization of human alpha-1 adrenergic receptors: sequence corrections and direct comparison with other species homologues.
Published in: J Pharmacol Exp Ther

Ligand: tamsulosin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1997)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Revisiting the Pharmacodynamic Uroselectivity of <i>&#x3b1;</i> <sub>1</sub>-Adrenergic Receptor Antagonists.
Published in: J Pharmacol Exp Ther

Ligand: tamsulosin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1997)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Molecular cloning, genomic characterization and expression of novel human alpha1A-adrenoceptor isoforms.
Published in: FEBS Lett

Ligand: terazosin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1987)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Revisiting the Pharmacodynamic Uroselectivity of <i>&#x3b1;</i> <sub>1</sub>-Adrenergic Receptor Antagonists.
Published in: J Pharmacol Exp Ther

Ligand: terazosin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1987)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist for the symptomatic treatment of benign prostatic hyperplasia.
Published in: J Med Chem

Ligand: terazosin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1987)
Primary target: yes
Median affinity:  pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants, and antipsychotics for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: terguride (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity: 8.5 pKi
Reference (Journal): Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
Published in: J Pharmacol Exp Ther

Ligand: upidosin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.600000381469727 pKi
Reference (Journal): Pharmacological pleiotropism of the human recombinant alpha1A-adrenoceptor: implications for alpha1-adrenoceptor classification.
Published in: Br J Pharmacol

Ligand: WB 4101 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants, and antipsychotics for the human &#x3b1;1A, &#x3b1;1B, and &#x3b1;1D-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: WB 4101 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): KMD-3213, a novel, potent, alpha 1a-adrenoceptor-selective antagonist: characterization using recombinant human alpha 1-adrenoceptors and native tissues.
Published in: Mol Pharmacol

Ligand: WB 4101 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological pleiotropism of the human recombinant alpha1A-adrenoceptor: implications for alpha1-adrenoceptor classification.
Published in: Br J Pharmacol

Ligand: WB 4101 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Phe-308 and Phe-312 in transmembrane domain 7 are major sites of alpha 1-adrenergic receptor antagonist binding. Imidazoline agonists bind like antagonists.
Published in: J Biol Chem

Ligand: WB 4101 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Characterization of alpha1-adrenoceptor subtypes mediating contractions to phenylephrine in rat thoracic aorta, mesenteric artery and pulmonary artery.
Published in: Br J Pharmacol

Ligand: WB 4101 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Molecular cloning, genomic characterization and expression of novel human alpha1A-adrenoceptor isoforms.
Published in: FEBS Lett

Ligand: WB 4101 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Human cloned alpha1A-adrenoceptor isoforms display alpha1L-adrenoceptor pharmacology in functional studies.
Published in: Eur J Pharmacol