105565-55-7

105565-55-7 structure

Name: BMY 14802 hydrochloride
Chemical Name: BMY 14802 hydrochloride,α-(4-Fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanolhydrochloride
CAS Number: 105565-55-7
Molecular Formula: C₁₈H₂₃ClF₂N₄O
Molecular Weight: 384.85100
Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
Create Date: 2017-02-21 22:32:26
Modify Date: 2024-01-08 12:39:41
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].

Name	BMY 14802 hydrochloride,α-(4-Fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanolhydrochloride

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.

Boiling Point	520.8ºC at 760mmHg
Molecular Formula	C₁₈H₂₃ClF₂N₄O
Molecular Weight	384.85100
Flash Point	268.8ºC
Exact Mass	384.15300
PSA	52.49000
LogP	3.19550
Vapour Pressure	1.13E-11mmHg at 25°C

105565-55-7	105565-56-8
1189644-16-3	36362-09-1
1048649-80-4	160901-63-3
61535-49-7	123334-18-9
121524-09-2	161909-82-6