BMY-14802 hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BMY-14802 hydrochloride (BMY-14802-1) 是一种选择性和具有口服活性的 σ 受体 (sigma receptor) 拮抗剂，IC50 为 112 nM。BMY-14802 hydrochloride 也是一种 5-HT1A 和肾上腺素 α1 受体激动剂。BMY-14802 hydrochloride 具有抗精神病作用。

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.

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.

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.

——

GPCR/G Protein

5-HT Receptor

5-HT Receptor | Sigma receptor | Adrenergic Receptor

——

——

105565-55-7

384.85

C18H23ClF2N4O

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 125 mg/mL (324.80 mM; 超声助溶 )

Cl.OC(CCCN1CCN(CC1)c1ncc(F)cn1)c1ccc(F)cc1

——

(-20℃)

With Ice Pack

≥ 2 years