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

Ligand: A-1262543 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pEC50
Reference (Journal): A selective &#x3b1;2 B adrenoceptor agonist (A-1262543) and duloxetine modulate nociceptive neurones in the medial prefrontal cortex, but not in the spinal cord of neuropathic rats.
Published in: Eur J Pain

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: 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: (-)-adrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (no history prior to 1951)
Primary target: no
Median affinity: 6.300000190734863 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: (-)-adrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (no history prior to 1951)
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: (-)-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 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:  pKi
Reference (Journal): Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding.
Published in: Biochem Pharmacol

Ligand: apomorphine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2001), FDA (2004)
Median affinity: 7.2 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: ARC-239 (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: 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: 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): Pharmacological characteristics of alpha 2-adrenergic receptors: comparison of pharmacologically defined subtypes with subtypes identified by molecular cloning.
Published in: Mol Pharmacol

Ligand: atipamezole (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.900000095367432 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: brimonidine (UK14304) (Synthetic organic)
Interaction type: Agonist
Action: Partial 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: Partial 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: Agonist
Ligand approved: yes
Approval source: FDA (1996), EMA (2014)
Primary target: no
Median affinity: 7.800000190734863 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: brimonidine (UK14304) (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1996), EMA (2014)
Primary target: no
Median affinity: 7.199999809265137 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: Agonist
Ligand approved: yes
Approval source: FDA (1996), EMA (2014)
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: brimonidine (UK14304) (Synthetic organic)
Interaction type: Agonist
Action: Partial 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: brimonidine (UK14304) (Synthetic organic)
Interaction type: Agonist
Action: Partial 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: 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): 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: 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: cabergoline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1996)
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: 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): 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): 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: Partial 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: Partial 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: 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: clonidine (Synthetic organic)
Interaction type: Agonist
Action: Partial 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: clonidine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1974)
Primary target: no
Median affinity: 8.600000381469727 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: no
Median affinity: 7.400000095367432 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: Partial 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: dexmedetomidine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2011)
Primary target: no
Median affinity: 9.199999809265137 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: Full 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: Full 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: Full agonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2011)
Primary target: no
Median affinity: 10.899999618530273 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: dexmedetomidine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2011)
Primary target: no
Median affinity: 9.899999618530273 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: Full 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: dexmedetomidine (Synthetic organic)
Interaction type: Agonist
Action: Full 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: Full 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: guanabenz (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1982)
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: guanabenz (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1982)
Primary target: no
Median affinity: 7.900000095367432 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: yes
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: guanabenz (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1982)
Primary target: no
Median affinity: 9 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: Full agonist
Ligand approved: yes
Approval source: FDA (1986), EMA (2015)
Primary target: no
Median affinity: 8.699999809265137 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: Full 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: Full agonist
Ligand approved: yes
Approval source: FDA (1986), EMA (2015)
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: guanfacine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1986), EMA (2015)
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: guanfacine (Synthetic organic)
Interaction type: Agonist
Action: Full 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: idazoxan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.400000095367432 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: imiloxan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.3 pKi
Reference (Journal): Assessment of imiloxan as a selective alpha 2B-adrenoceptor antagonist.
Published in: Br J Pharmacol

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

Ligand: lofexidine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: UK (1990), FDA (2018)
Primary target: no
Median affinity: 7.170000076293945 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: 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: mirtazapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1996)
Primary target: yes
Median affinity:  pKi
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: MK-912 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
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;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: 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: moxonidine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Primary target: no
Median affinity: 4.599999904632568 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: 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: moxonidine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
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: (-)-noradrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1950)
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: (-)-noradrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1950)
Primary target: no
Median affinity: 7.800000190734863 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: (-)-noradrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1950)
Primary target: no
Median affinity: 6.900000095367432 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: 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: 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: (-)-noradrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1950)
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: oxymetazoline (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1986)
Primary target: no
Median affinity: 8.800000190734863 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: oxymetazoline (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1986)
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: oxymetazoline (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1986)
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: oxymetazoline (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1986)
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: oxymetazoline (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1986)
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: pergolide (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1988)
Median affinity: 7.5 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: phenoxybenzamine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1953)
Primary target: no
Median affinity: 6.400000095367432 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: phenoxybenzamine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1953)
Primary target: yes
Median affinity: 8.5 pKi
Reference (Journal): Molecular cloning and characterization of a high affinity dopamine receptor (D1 beta) and its pseudogene.
Published in: J Biol Chem

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): 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: 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: (±)-adrenaline (Metabolite)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: 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: prazosin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1976)
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: 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): 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): 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: 8.3 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: roxindole (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.3 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: RS79948 (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;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: 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: 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: 8.100000381469727 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]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): Pharmacological characteristics of alpha 2-adrenergic receptors: comparison of pharmacologically defined subtypes with subtypes identified by molecular cloning.
Published in: Mol Pharmacol

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): 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): 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
Primary target: no
Median affinity: 9.399999618530273 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: 7 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: 6.300000190734863 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: tizanidine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1996)
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: tizanidine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1996)
Primary target: no
Median affinity: 5.800000190734863 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: tolazoline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1948)
Primary target: yes
Median affinity: 5.5 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): 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): 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: 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): 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: 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: xylazine (Synthetic organic)
Interaction type: Agonist
Action: 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:  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: 7.699999809265137 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: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.400000095367432 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: xylometazoline (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Primary target: no
Median affinity: 7.800000190734863 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: xylometazoline (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Primary target: no
Median affinity: 5.400000095367432 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: Agonist
Ligand approved: yes
Primary target: no
Median affinity: 8.800000190734863 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: 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

Ligand: zotepine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: no
Median affinity: 8.199999809265137 pKi
Reference (Journal): Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
Published in: Psychopharmacology (Berl.)