Target family: Adrenoceptors (type: gpcr)
Target: &alpha;<sub>2A</sub>-adrenoceptor

Ligand: 5-(N,N-hexamethylene)-amiloride (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 2.5 pKd
Reference (Journal): Characterization of the allosteric interactions between antagonists and amiloride analogues at the human alpha2A-adrenergic receptor.
Published in: Mol Pharmacol

Ligand: 5-(N,N-hexamethylene)-amiloride (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 2.5 pKd
Reference (Journal): Novel amiloride analog allosterically modulates the alpha 2-adrenergic receptor but does not inhibit Na+/H+ exchange.
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: yes
Median affinity:  pKi
Reference (Journal): Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding.
Published in: Biochem 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: 5.5 pEC50
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-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: 6.5 pIC50
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-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: 8 pEC50
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-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: yes
Median affinity:  pKi
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-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: 6.800000190734863 pEC50
Reference (Journal): Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding.
Published in: Biochem Pharmacol

Ligand: (-)-adrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (no history prior to 1951)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Modulation of agonist binding to recombinant human alpha2-adrenoceptors by sodium ions.
Published in: Biochim Biophys Acta

Ligand: apomorphine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: EMA (2001), FDA (2004)
Median affinity: 6.9 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: apraclonidine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1987)
Primary target: yes
Median affinity: 8.5 pKi
Reference (Journal): Synthesis and evaluation of 2-[(5-methylbenz-1-ox-4-azin-6-yl)imino]imidazoline, a potent, peripherally acting alpha 2 adrenoceptor agonist.
Published in: J Med Chem

Ligand: ARC-239 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological characteristics of alpha 2-adrenergic receptors: comparison of pharmacologically defined subtypes with subtypes identified by molecular cloning.
Published in: Mol Pharmacol

Ligand: ARC-239 (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;2A, &#x3b1;2B, and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: ARC-239 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Further characterization of human alpha 2-adrenoceptor subtypes: [3H]RX821002 binding and definition of additional selective drugs.
Published in: Eur J Pharmacol

Ligand: atipamezole (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.5 pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants and antipsychotics for the human &#x3b1;2A, &#x3b1;2B, and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: atropine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1973)
Primary target: no
Median affinity: 4.849999904632568 pKi
Reference (Journal): Myopia-Inhibiting Concentrations of Muscarinic Receptor Antagonists Block Activation of Alpha2A-Adrenoceptors In Vitro.
Published in: Invest Ophthalmol Vis Sci

Ligand: brimonidine (UK14304) (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1996), EMA (2014)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding.
Published in: Biochem Pharmacol

Ligand: brimonidine (UK14304) (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1996), EMA (2014)
Primary target: yes
Median affinity:  pKi
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: brimonidine (UK14304) (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1996), EMA (2014)
Primary target: no
Median affinity: 8.899999618530273 pIC50
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: brimonidine (UK14304) (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1996), EMA (2014)
Primary target: no
Median affinity: 9.100000381469727 pEC50
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: brimonidine (UK14304) (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1996), EMA (2014)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Gene targeting--homing in on alpha 2-adrenoceptor-subtype function.
Published in: Trends Pharmacol Sci

Ligand: brimonidine (UK14304) (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1996), EMA (2014)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Modulation of agonist binding to recombinant human alpha2-adrenoceptors by sodium ions.
Published in: Biochim Biophys Acta

Ligand: brimonidine (UK14304) (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1996), EMA (2014)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Subtype-specific stimulation of [35S]GTPgammaS binding by recombinant alpha2-adrenoceptors.
Published in: Eur J Pharmacol

Ligand: BRL 44408 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Novel alpha 2-adrenoceptor antagonists show selectivity for alpha 2A- and alpha 2B-adrenoceptor subtypes.
Published in: Eur J Pharmacol

Ligand: BRL 44408 (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;2A, &#x3b1;2B, and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: BRL 44408 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The novel alpha-2 adrenergic radioligand [3H]-MK912 is alpha-2C selective among human alpha-2A, alpha-2B and alpha-2C adrenoceptors.
Published in: J Pharmacol Exp Ther

Ligand: bromocriptine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1978)
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: bromocriptine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1978)
Primary target: no
Median affinity:  pKi
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: C10 (homobivalent 4-aminoquinoline) (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 7.5 pKi
Reference (Journal): Structural Insight into the Mechanism of 4-Aminoquinolines Selectivity for the alpha2A-Adrenoceptor.
Published in: Drug Des Devel Ther

Ligand: cabergoline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1996)
Median affinity: 7.9 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: chlorpromazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1957)
Primary target: no
Median affinity:  pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants and antipsychotics for the human &#x3b1;2A, &#x3b1;2B, and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: chlorpromazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1957)
Primary target: no
Median affinity:  pKi
Reference (Journal): Further characterization of human alpha 2-adrenoceptor subtypes: [3H]RX821002 binding and definition of additional selective drugs.
Published in: Eur J Pharmacol

Ligand: chlorpromazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1957)
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological characteristics of alpha 2-adrenergic receptors: comparison of pharmacologically defined subtypes with subtypes identified by molecular cloning.
Published in: Mol Pharmacol

Ligand: clonidine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1974)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Subtype-specific stimulation of [35S]GTPgammaS binding by recombinant alpha2-adrenoceptors.
Published in: Eur J Pharmacol

Ligand: clonidine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1974)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Modulation of agonist binding to recombinant human alpha2-adrenoceptors by sodium ions.
Published in: Biochim Biophys Acta

Ligand: clonidine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1974)
Primary target: no
Median affinity: 7.599999904632568 pEC50
Reference (Journal): Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding.
Published in: Biochem Pharmacol

Ligand: clonidine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1974)
Primary target: no
Median affinity: 9 pEC50
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: clonidine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1974)
Primary target: no
Median affinity: 8.199999809265137 pIC50
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: clonidine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1974)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding.
Published in: Biochem Pharmacol

Ligand: clonidine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1974)
Primary target: no
Median affinity: 6.400000095367432 pEC50
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: clonidine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1974)
Primary target: yes
Median affinity:  pKi
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: dexmedetomidine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2011)
Primary target: no
Median affinity: 7.599999904632568 pEC50
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: dexmedetomidine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2011)
Primary target: no
Median affinity: 8.5 pEC50
Reference (Journal): Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding.
Published in: Biochem Pharmacol

Ligand: dexmedetomidine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2011)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding.
Published in: Biochem Pharmacol

Ligand: dexmedetomidine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2011)
Primary target: yes
Median affinity:  pKi
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: dexmedetomidine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2011)
Primary target: no
Median affinity: 9.300000190734863 pIC50
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: dexmedetomidine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2011)
Primary target: no
Median affinity: 9.5 pEC50
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: dexmedetomidine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2011)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Gene targeting--homing in on alpha 2-adrenoceptor-subtype function.
Published in: Trends Pharmacol Sci

Ligand: dexmedetomidine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2011)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Subtype-specific stimulation of [35S]GTPgammaS binding by recombinant alpha2-adrenoceptors.
Published in: Eur J Pharmacol

Ligand: dexmedetomidine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2011)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Modulation of agonist binding to recombinant human alpha2-adrenoceptors by sodium ions.
Published in: Biochim Biophys Acta

Ligand: ethylisopropylamiloride (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 1.8 pKd
Reference (Journal): Novel amiloride analog allosterically modulates the alpha 2-adrenergic receptor but does not inhibit Na+/H+ exchange.
Published in: Mol Pharmacol

Ligand: guanabenz (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1982)
Primary target: no
Median affinity: 9.100000381469727 pEC50
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: guanabenz (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1982)
Primary target: no
Median affinity:  pKi
Reference (Journal): Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding.
Published in: Biochem Pharmacol

Ligand: guanabenz (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1982)
Primary target: yes
Median affinity: 7.400000095367432 pIC50
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: guanabenz (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1982)
Primary target: no
Median affinity: 8.300000190734863 pEC50
Reference (Journal): Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding.
Published in: Biochem Pharmacol

Ligand: guanabenz (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1982)
Primary target: no
Median affinity:  pIC50
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: guanabenz (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1982)
Primary target: no
Median affinity:  pIC50
Reference (Webpage): National Toxicology Program: Dept of Health and Human Services.

Ligand: guanabenz (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1982)
Primary target: no
Median affinity:  pKi
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: guanabenz (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1982)
Primary target: yes
Median affinity: 7.400000095367432 pIC50
Reference (Webpage): National Toxicology Program: Dept of Health and Human Services.

Ligand: guanfacine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1986), EMA (2015)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding.
Published in: Biochem Pharmacol

Ligand: guanfacine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1986), EMA (2015)
Primary target: no
Median affinity: 8 pIC50
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: guanfacine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1986), EMA (2015)
Primary target: yes
Median affinity:  pKi
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: guanfacine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1986), EMA (2015)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Characterization of alpha 2-adrenoceptors mediating contraction of dog saphenous vein: identity with the human alpha 2A subtype.
Published in: Br J Pharmacol

Ligand: guanfacine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1986), EMA (2015)
Primary target: no
Median affinity: 6.5 pEC50
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: guanfacine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1986), EMA (2015)
Primary target: no
Median affinity: 9 pEC50
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: guanfacine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1986), EMA (2015)
Primary target: no
Median affinity: 7.300000190734863 pEC50
Reference (Journal): Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding.
Published in: Biochem Pharmacol

Ligand: idazoxan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.199999809265137 pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants and antipsychotics for the human &#x3b1;2A, &#x3b1;2B, and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-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): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants and antipsychotics for the human &#x3b1;2A, &#x3b1;2B, and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-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: lofexidine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: UK (1990), FDA (2018)
Primary target: no
Median affinity: 8.359999656677246 pKi
Reference (Journal): Might the observed α(2A)-adrenoreceptor agonism or antagonism of allyphenyline analogues be ascribed to different molecular conformations?
Published in: Bioorg Med Chem

Ligand: lurasidone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2010), EMA (2014)
Primary target: no
Median affinity:  pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants and antipsychotics for the human &#x3b1;2A, &#x3b1;2B, and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: lurasidone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2010), EMA (2014)
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological profile of lurasidone, a novel antipsychotic agent with potent 5-hydroxytryptamine 7 (5-HT7) and 5-HT1A receptor activity.
Published in: J Pharmacol Exp Ther

Ligand: mirtazapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1996)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.
Published in: J Med Chem

Ligand: mirtazapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1996)
Primary target: yes
Median affinity: 7.099999904632568 pIC50
Reference (Journal): New 2-substituted 1,2,3,4-tetrahydrobenzofuro[3,2-c]pyridine having highly active and potent central alpha 2-antagonistic activity as potential antidepressants.
Published in: Bioorg Med Chem Lett

Ligand: mirtazapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1996)
Primary target: yes
Median affinity:  pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants and antipsychotics for the human &#x3b1;2A, &#x3b1;2B, and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: MK-912 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants and antipsychotics for the human &#x3b1;2A, &#x3b1;2B, and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: moxonidine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Primary target: no
Median affinity: 5.800000190734863 pEC50
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: moxonidine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Primary target: no
Median affinity: 8.5 pEC50
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: moxonidine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Primary target: no
Median affinity: 5 pKi
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: moxonidine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Primary target: no
Median affinity: 7.5 pIC50
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: muscarinic toxin 3 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pKi
Reference (Journal): Myopia-Inhibiting Concentrations of Muscarinic Receptor Antagonists Block Activation of Alpha2A-Adrenoceptors In Vitro.
Published in: Invest Ophthalmol Vis Sci

Ligand: naphazoline (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1971, prior history not available)
Primary target: no
Median affinity: 7 pKi
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: naphazoline (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1971, prior history not available)
Primary target: no
Median affinity: 7.800000190734863 pIC50
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-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: 7.699999809265137 pEC50
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-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 signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-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: 6.599999904632568 pIC50
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-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: 5.300000190734863 pEC50
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-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: 6.699999809265137 pEC50
Reference (Journal): Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding.
Published in: Biochem 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): Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding.
Published in: Biochem 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): Modulation of agonist binding to recombinant human alpha2-adrenoceptors by sodium ions.
Published in: Biochim Biophys Acta

Ligand: oxymetazoline (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1986)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Gene targeting--homing in on alpha 2-adrenoceptor-subtype function.
Published in: Trends Pharmacol Sci

Ligand: oxymetazoline (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1986)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding.
Published in: Biochem Pharmacol

Ligand: oxymetazoline (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1986)
Primary target: yes
Median affinity:  pKi
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: oxymetazoline (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1986)
Primary target: no
Median affinity: 8.399999618530273 pIC50
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: oxymetazoline (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1986)
Primary target: yes
Median affinity:  pKi
Reference (Journal): The novel alpha-2 adrenergic radioligand [3H]-MK912 is alpha-2C selective among human alpha-2A, alpha-2B and alpha-2C adrenoceptors.
Published in: J Pharmacol Exp Ther

Ligand: pergolide (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1988)
Median affinity: 7.3 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: phentolamine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1952)
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological characteristics of alpha 2-adrenergic receptors: comparison of pharmacologically defined subtypes with subtypes identified by molecular cloning.
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:  pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants and antipsychotics for the human &#x3b1;2A, &#x3b1;2B, and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: phentolamine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1952)
Primary target: no
Median affinity:  pKi
Reference (Journal): Further characterization of human alpha 2-adrenoceptor subtypes: [3H]RX821002 binding and definition of additional selective drugs.
Published in: Eur J Pharmacol

Ligand: phentolamine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1952)
Primary target: no
Median affinity: 7.099999904632568 pEC50
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: piribedil (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.1 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: Antagonist
Ligand approved: yes
Approval source: FDA (1976)
Primary target: no
Median affinity:  pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants and antipsychotics for the human &#x3b1;2A, &#x3b1;2B, and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: prazosin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1976)
Primary target: no
Median affinity:  pKi
Reference (Journal): Further characterization of human alpha 2-adrenoceptor subtypes: [3H]RX821002 binding and definition of additional selective drugs.
Published in: Eur J Pharmacol

Ligand: prazosin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1976)
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological characteristics of alpha 2-adrenergic receptors: comparison of pharmacologically defined subtypes with subtypes identified by molecular cloning.
Published in: Mol Pharmacol

Ligand: rauwolscine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.4 pKi
Reference (Journal): The novel alpha-2 adrenergic radioligand [3H]-MK912 is alpha-2C selective among human alpha-2A, alpha-2B and alpha-2C adrenoceptors.
Published in: J Pharmacol Exp Ther

Ligand: risperidone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1993), EMA (2022)
Primary target: no
Median affinity: 7.300000190734863 pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants and antipsychotics for the human &#x3b1;2A, &#x3b1;2B, and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: RS79948 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.899999618530273 pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants and antipsychotics for the human &#x3b1;2A, &#x3b1;2B, and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: RX821002 (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;2A, &#x3b1;2B, and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: RX821002 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The novel alpha-2 adrenergic radioligand [3H]-MK912 is alpha-2C selective among human alpha-2A, alpha-2B and alpha-2C adrenoceptors.
Published in: J Pharmacol Exp Ther

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;2A, &#x3b1;2B, and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: spiroxatrine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The novel alpha-2 adrenergic radioligand [3H]-MK912 is alpha-2C selective among human alpha-2A, alpha-2B and alpha-2C adrenoceptors.
Published in: J Pharmacol Exp Ther

Ligand: [125I]p-iodoclonidine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 8.800000190734863 pKd
Reference (Journal): Comparison of ligand binding affinities at human I1-imidazoline binding sites and the high affinity state of alpha-2 adrenoceptor subtypes.
Published in: J Pharmacol Exp Ther

Ligand: [3H]brimonidine (UK14304) (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.100000381469727 pKd
Reference (Journal): Agonist and antagonist binding to alpha 2-adrenergic receptors in purified membranes from human platelets. Implications of receptor-inhibitory nucleotide-binding protein stoichiometry.
Published in: Mol Pharmacol

Ligand: [3H]clonidine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 8.800000190734863 pKd
Reference (Journal): Displacement of [3H]clonidine binding by clonidine analogues in membranes from rat cerebral cortex.
Published in: Eur J Pharmacol

Ligand: [3H]clonidine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pKd
Reference (Journal): Characterization of alpha-adrenergic receptors in human platelets using [3H]clonidine.
Published in: Mol Pharmacol

Ligand: [3H]MK-912 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.899999618530273 pKd
Reference (Journal): The novel alpha-2 adrenergic radioligand [3H]-MK912 is alpha-2C selective among human alpha-2A, alpha-2B and alpha-2C adrenoceptors.
Published in: J Pharmacol Exp Ther

Ligand: [3H]rauwolscine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Buffers differentially alter the binding of [3H]rauwolscine and [3H]RX821002 to the alpha-2 adrenergic receptor subtypes.
Published in: J Pharmacol Exp Ther

Ligand: [3H]rauwolscine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants and antipsychotics for the human &#x3b1;2A, &#x3b1;2B, and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: [3H]rauwolscine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Pharmacological characteristics of alpha 2-adrenergic receptors: comparison of pharmacologically defined subtypes with subtypes identified by molecular cloning.
Published in: Mol Pharmacol

Ligand: [3H]RX821002 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Buffers differentially alter the binding of [3H]rauwolscine and [3H]RX821002 to the alpha-2 adrenergic receptor subtypes.
Published in: J Pharmacol Exp Ther

Ligand: [3H]RX821002 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants and antipsychotics for the human &#x3b1;2A, &#x3b1;2B, and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: [3H]RX821002 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Further characterization of human alpha 2-adrenoceptor subtypes: [3H]RX821002 binding and definition of additional selective drugs.
Published in: Eur J Pharmacol

Ligand: terguride (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity: 9.5 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: tizanidine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1996)
Primary target: no
Median affinity: 5.800000190734863 pEC50
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: tizanidine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1996)
Primary target: no
Median affinity: 8.399999618530273 pEC50
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: tizanidine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1996)
Primary target: no
Median affinity: 6 pKi
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: tizanidine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1996)
Primary target: no
Median affinity: 7.599999904632568 pIC50
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: tolazoline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1948)
Primary target: yes
Median affinity: 6.699999809265137 pKi
Reference (Journal): Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding.
Published in: Biochem 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;2A, &#x3b1;2B, and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-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): Further characterization of human alpha 2-adrenoceptor subtypes: [3H]RX821002 binding and definition of additional selective drugs.
Published in: Eur J Pharmacol

Ligand: WB 4101 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological characteristics of alpha 2-adrenergic receptors: comparison of pharmacologically defined subtypes with subtypes identified by molecular cloning.
Published in: Mol Pharmacol

Ligand: xylazine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.099999904632568 pEC50
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: xylazine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.5 pIC50
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: xylazine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: xylazine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.5 pEC50
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: xylazine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding.
Published in: Biochem Pharmacol

Ligand: xylazine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.699999809265137 pEC50
Reference (Journal): Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding.
Published in: Biochem Pharmacol

Ligand: xylometazoline (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Primary target: no
Median affinity: 7.599999904632568 pKi
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: xylometazoline (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Primary target: no
Median affinity: 8.100000381469727 pIC50
Reference (Journal): The signaling and selectivity of &#x3b1;-adrenoceptor agonists for the human &#x3b1;2A, &#x3b1;2B and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: yohimbine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (no date available)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Further characterization of human alpha 2-adrenoceptor subtypes: [3H]RX821002 binding and definition of additional selective drugs.
Published in: Eur J Pharmacol

Ligand: yohimbine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (no date available)
Primary target: yes
Median affinity:  pKi
Reference (Journal): The novel alpha-2 adrenergic radioligand [3H]-MK912 is alpha-2C selective among human alpha-2A, alpha-2B and alpha-2C adrenoceptors.
Published in: J Pharmacol Exp Ther

Ligand: yohimbine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (no date available)
Primary target: yes
Median affinity:  pKi
Reference (Journal): The affinity and selectivity of &#x3b1;-adrenoceptor antagonists, antidepressants and antipsychotics for the human &#x3b1;2A, &#x3b1;2B, and &#x3b1;2C-adrenoceptors and comparison with human &#x3b1;1 and &#x3b2;-adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: yohimbine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (no date available)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Pharmacological characteristics of alpha 2-adrenergic receptors: comparison of pharmacologically defined subtypes with subtypes identified by molecular cloning.
Published in: Mol Pharmacol