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BP 897

CAS No. : 314776-92-6

MCE 站：BP 897

产品活性：BP 897 是一种有效的，选择性的多巴胺 D3 受体 (dopamine D3 receptor) 部分激动剂，为较弱的多巴胺 D2 受体 (dopamine D2 receptor) 拮抗剂，K_i 值分别为 0.92 nM 和 61 nM，对 D1 和 D4 受体的亲和性较低，K_i 值分别为 3 和 0.3??M。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Dopamine Receptor

In Vitro: BP 897 is a potent and selective dopamine D3 receptor agonist, and a weak dopamine D2 receptor antagonist, with a K_i of 0.92 nM for D3 receptor, a 70 times lower affinity at the D2 receptor (K_i, 61 nM), and shows low affinities at D1 and D4 receptors (K_i = 3 and 0.3??M, respectively). BP 897 also weakly binds to α1 and α2 adrenergic receptors (K_i = 60 and 83?nM, respectively), 5HT1A and 5HT7 receptors (K_i = 84 and 345?nM, respectively), and has negligible affinities (K_i > 1??M) at muscarinic, histamine and opiate receptors. BP 897 inhibits forskolin-induced cyclic AMP accumulation with an EC₅₀ of 1.0 ± 0.3?nM, and increases mitogenesis, another D3-receptor-mediated response (EC₅₀ = 3 ± 1?nM) in NG 108-15 cells expressing the human D3 receptor. However, BP 897 (1??M) does not inhibit cyclic AMP accumulation or trigger mitogenesis in cells expressing the D2 receptor.

In Vivo: BP 897 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, 0.05, 0.5, 1?mg/kg) inhibits cocaine-seeking behaviour that depends upon the presentation of drug-associated cues, without having any intrinsic, primary rewarding effects.

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