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。
产品描述
BP 897 is a potent and selective agonist of dopamine D3 receptor and it is a weak dopamine D2 receptor antagonist, with Kis of 0.92 nM and 61 nM for D3 and D2 receptors. Which shows low affinities at D1 and D4 receptors (Kis, 3 and 0.3 μM, respectively).
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.
Cas No.
314776-92-6
分子式
C26H32ClN3O2
分子量
454
别名
BP 897 hydrochloride
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years