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BP 897 hydrochloride

CAS No. : 314776-92-6

MCE 站：BP 897 hydrochloride

产品活性：BP 897 hydrochloride 是一种有效的部分多巴胺 D3 受体激动剂和弱 D2 受体拮抗剂。BP 897 hydrochloride 在多巴胺 D3 受体 (K_i=0.92 nM) 上显示出高亲和力，而在 D2 受体上显示出 70 倍的低亲和力 (K_i=61 nM)。BP897 hydrochloride 表现出对可卡因寻求行为的选择性抑制。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Dopamine Receptor

In Vitro: BP 897 hydrochloride also displays low affinities at D1 and D4 receptors (K_i=3 and 0.3 μM, respectively), as well as at α1 and α2 adrenergic receptors (K_i=60 and 83 nM, respectively), 5HT1A and 5HT7 receptors (K_i=84 and 345 nM, respectively), and negligible affinities (K_i>1 μM) atmuscarinic, histamine and opiate receptors.
In NG 108-15 cells expressing the human D3 receptor, BP 897 hydrochloride inhibits forskolin-induced cyclic AMP accumulation with an EC₅₀ of 1 nM. BP 897 hydrochloride activates mitogenesis and this response is antagonized by the preferential D3 receptor antagonist Nafadotride (1 μM). BP 897 hydrochloride also partially antagonized the response induced by quinpirole (10 nM).

In Vivo: BP 897 hydrochloride binds to D2-receptor in mouse striatum with an ED₅₀ of 15?mg/kg, and the D3-receptor occupancy is blow 0.5?mg/kg. BP 897 (0.05, 0.5, 1 mg/kg; i.p.; 30 min before the session) hydrochloride reduces cocaine-seeking behaviour before the first infusion of cocaine, in a dose-dependent manner, at doses similar to those at which BP 897 hydrochloride produced its responses on rotations and c-fos expression.

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