Target family: Adrenoceptors (type: gpcr)
Target: &alpha;<sub>1B</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: A-119637 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.3 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 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: 4 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:  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: 5.099999904632568 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): 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: (-)-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: AH 11110 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.5 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: alfuzosin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2003)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
Published in: J Med Chem

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: 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: cirazoline (Synthetic organic)
Interaction type: Agonist
Action: Partial 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: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 5.099999904632568 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: 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: compound 12 [PMID: 26238322] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.800000190734863 pKi
Reference (Journal): Indolylpiperidine derivatives as potent and selective &#x3b1;1B adrenoceptor antagonists.
Published in: Bioorg Med Chem Lett

Ligand: (+)-cyclazosin (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
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: Inverse agonist
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: 7.6 pKi
Reference (Journal): Affinity of serotonin receptor antagonists and agonists to recombinant and native alpha1-adrenoceptor subtypes.
Published in: Jpn J Pharmacol

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 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: indoramin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: UK (1993)
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: indoramin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: UK (1993)
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: 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: 6.940000057220459 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: L-765314 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.3 pKi
Reference (Journal): 4-Amino-2-[4-[1-(benzyloxycarbonyl)-2(S)- [[(1,1-dimethylethyl)amino]carbonyl]-piperazinyl]-6, 7-dimethoxyquinazoline (L-765,314): a potent and selective alpha1b adrenergic receptor antagonist.
Published in: J Med Chem

Ligand: L-765314 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.699999809265137 pKi
Reference (Journal): 4-Amino-2-[4-[1-(benzyloxycarbonyl)-2(S)- [[(1,1-dimethylethyl)amino]carbonyl]-piperazinyl]-6, 7-dimethoxyquinazoline (L-765,314): a potent and selective alpha1b adrenergic receptor antagonist.
Published in: J Med Chem

Ligand: lorazepam (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: yes
Approval source: FDA (1977)
Primary target: no
Median affinity: 3.799999952316284 pKi
Reference (Journal): Binding, partial agonism, and potentiation of alpha(1)-adrenergic receptor function by benzodiazepines: A potential site of allosteric modulation.
Published in: J Pharmacol Exp Ther

Ligand: mamba toxin CM-3 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8 pKi
Reference (Journal): New &#x3b1;-adrenergic property for synthetic MT&#x3b2; and CM-3 three-finger fold toxins from black mamba.
Published in: Toxicon

Ligand: methoxamine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
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: methoxamine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
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: methoxamine (Synthetic organic)
Interaction type: Agonist
Action: Partial 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: mianserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
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: midazolam (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: yes
Approval source: FDA (2000), EMA (2011)
Primary target: no
Median affinity: 3.700000047683716 pKi
Reference (Journal): Binding, partial agonism, and potentiation of alpha(1)-adrenergic receptor function by benzodiazepines: A potential site of allosteric modulation.
Published in: J Pharmacol Exp Ther

Ligand: muscarinic toxin β (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8 pKi
Reference (Journal): New &#x3b1;-adrenergic property for synthetic MT&#x3b2; and CM-3 three-finger fold toxins from black mamba.
Published in: Toxicon

Ligand: NAN 190 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.2 pKi
Reference (Journal): Affinity of serotonin receptor antagonists and agonists to recombinant and native alpha1-adrenoceptor subtypes.
Published in: Jpn 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): 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:  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): 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: NS-49 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 5.1 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: no
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: 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: 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: oxymetazoline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1986)
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: 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: 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: phenylephrine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1952)
Primary target: yes
Median affinity:  pEC50
Reference (Journal): Pharmacological pleiotropism of the human recombinant alpha1A-adrenoceptor: implications for alpha1-adrenoceptor classification.
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: phenylephrine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1952)
Primary target: no
Median affinity: 3.9000000953674316 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:  pEC50
Reference (Journal): Selectivity of agonists for cloned alpha 1-adrenergic receptor subtypes.
Published in: Mol 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): 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)
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): In vitro alpha1-adrenoceptor pharmacology of Ro 70-0004 and RS-100329, novel alpha1A-adrenoceptor selective antagonists.
Published in: Br J Pharmacol

Ligand: Rec 15/2615 (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 II.
Published in: J Pharmacol Exp Ther

Ligand: Rec 15/2615 (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: rho-TIA (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pKi
Reference (Journal): Subtype-selective noncompetitive or competitive inhibition of human alpha1-adrenergic receptors by rho-TIA.
Published in: J Biol Chem

Ligand: rho-TIA (Peptide)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 9.100000381469727 pIC50
Reference (Journal): Differential antagonism by conotoxin rho-TIA of contractions mediated by distinct alpha1-adrenoceptor subtypes in rat vas deferens, spleen and aorta.
Published in: Eur 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): 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 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
Median affinity: 7.1 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: silodosin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2008), EMA (2010)
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: silodosin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2008), EMA (2010)
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): Pharmacological pleiotropism of the human recombinant alpha1A-adrenoceptor: implications for alpha1-adrenoceptor classification.
Published in: Br J Pharmacol

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: spiperone (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity: 9.2 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
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: [125I]HEAT (BE2254) (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Alpha 1-adrenergic receptor regulation: basic science and clinical implications.
Published in: Pharmacol Ther

Ligand: [125I]HEAT (BE2254) (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
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: [125I]HEAT (BE2254) (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
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: [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: Inverse agonist
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: Inverse agonist
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: Inverse agonist
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: Inverse agonist
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: 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: 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: upidosin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.8 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): 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