化合物BP 897 hydrochloride T14767

Product Introduction
Bioactivity


英文名: BP 897 hydrochloride

描述: BP 897 hydrochloride 是有效的部分多巴胺 D3受体激动剂和弱 D2受体拮抗剂，在多巴胺 D3 受体 (Ki=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 (Ki=61 nM)。它表现出对可卡因寻求行为的选择性抑制。

体外活性: 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?μM) does not inhibit cyclic AMP accumulation or trigger mitogenesis in cells expressing the D2 receptor[1]. With a 70 times lower affinity at the D2 receptor (Ki, 61 nM). BP 897 also weakly binds to α1 and α2 adrenergic receptors (Ki = 60 and 83?nM, respectively), 5HT1A and 5HT7 receptors (Ki = 84 and 345?nM, respectively), and has negligible affinities (Ki > 1?μM) at muscarinic, histamine and opiate receptors.

体内活性: 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[1]. 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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 9 mg/mL (19.82 mM)


关键字: Inhibitor | inhibit | stimuli | BP-897 | behaviour | Dopamine Receptor | BP 897 hydrochloride | BP897 Hydrochloride | addiction | rewarding | BP 897 | BP-897 Hydrochloride | BP 897 Hydrochloride | cocaine drug-seeking | motivational | BP897

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