BP-897

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

BP-897 是第一个有效的选择性部分多巴胺 D3 受体激动剂，Ki 为 0.92 nM。

BP-897 is the first, potent, selective partial dopamine D3 receptor agonist with Ki of 0.92 nM; displays 70 times lower affinity for D2 (Ki=61 nM), low affinities for D1 and D4 (Ki= 3 and 0.3 uM) and α1 and α2 adrenergic receptor (Ki=60 and 83 nM), negligible affinities (Ki>1 uM) for muscarinic, histamine and opiate receptors; inhibits cocaine-seeking behaviour that depends upon the presentation of drug-associated cues, without having any intrinsic, primary rewarding effects.Parkinson Disease Phase 2 Discontinued.

——

Animal Model:Male Listar hooded rats Dosage:0.05, 0.5, 1 mg/kg Administration:i.p.; 30 min before the session Result:Reduced cocaine-seeking behaviour before the first infusion of cocaine, in a dose-dependent manner, at doses similar to those at which BP 897 produced its responses on rotations and c-fos expression.

BP897

GPCR/G Protein

Dopamine Receptor

Dopamine Receptor

Neurological Disease

Parkinson Disease

314776-92-6

417.553

C26H31N3O2

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (275.33 mM)

O=C(NCCCCN1CCN(C2=CC=CC=C2OC)CC1)C3=CC=C4C=CC=CC4=C3

N-(4-(4-(2-methoxyphenyl)piperazin-1-yl)butyl)-2-naphthamide

(-20℃)

With Ice Pack

≥ 2 years