BMY 14802 hydrochloride

Names

[ Name ]:
BMY 14802 hydrochloride

Biological Activity

[Description]:

BMY-14802 hydrochloride (BMY-14802-1) is a selective and orally active sigma receptor antagonist with an IC50 of 112 nM. BMY-14802 hydrochloride is also a 5-HT1A and adrenergic α1 receptors agonist. BMY-14802 hydrochloride has antipsychotic effects[1][2][3].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> Sigma Receptor

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[Target]

5-HT1A Receptor

α1-adrenergic receptor

sigma Receptor:112 nM (IC50)

[In Vitro]

Similar to other 5-HT1A agonists, BMY-14802 hydrochloride affects the firing of 5-HTergic and catecholaminergic neurons and affects behaviors mediated by 5-HT in a 5-HT1A-sensitive manner. BMY-14802 hydrochloride is devoid of significant affinity for the D2 receptor[3].

[In Vivo]

BMY-14802 (5 mg/kg, 10 mg/kg or 20 mg/kg, ip; once) hydrochloride shows anti-dyskinetic efficacy across a 4-fold dose range against L-DOPA-induced dyskinesias (LID) and is also effective in reducing D1 and D2 receptor agonist-induced dyskinesias. Importantly, at anti-LID doses, BMY-14802 hydrochloride does not affect the efficacy of L-DOPA against lesion-induced akinesia[2].

[References]

[1]. J P Yevich, et al. Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents. J Med Chem. 1992 Nov 27;35(24):4516-25.

[2]. Nirmal Bhide, et al. The effects of BMY-14802 against L-DOPA- and dopamine agonist-induced dyskinesia in the hemiparkinsonian rat. Psychopharmacology (Berl). 2013 Jun;227(3):533-44.

[3]. Melanie A Paquette, et al. The sigma-1 antagonist BMY-14802 inhibits L-DOPA-induced abnormal involuntary movements by a WAY-100635-sensitive mechanism. Psychopharmacology (Berl). 2009 Jul;204(4):743-54.