| 产品描述: | BP 897 is a potent and partial dopamine D3 receptor agonist and a weak D2 receptor antagonist. BP 897 displays a high affinity at the dopamine D3 receptor (Ki=0.92 nM) and a 70 times lower affinity at the D2 receptor (Ki=61 nM) |
| 靶点: |
D2 Receptor; D3 Receptor |
| 体外研究: |
BP 897 对 D1 和 D4 受体 (Ki=3 μM 和 0.3 μM)、α1 和 α2 肾上腺素能受体 (Ki=60 nM 和 83 nM) 和 5HT1A 和 5HT7 受体 (Ki=84 nM 和 345 nM) 具有亲和力;对毒蕈碱型受体、组胺受体和阿片受体的亲和力则忽略不计 (Ki>1 μM)。 在表达人 D3 受体的 NG 108-15 细胞中,BP 897 抑制毛喉素诱导的环 AMP 积累,EC50=1 nM。BP 897 激活有丝分裂发生,这种反应优先被 D3 受体拮抗剂 Nafadotride (1 μM) 拮抗。BP 897 也部分拮抗 quinpirole (10 nM) 诱导的反应 |
| 体内研究: |
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. |
| 参考文献: |
1. Pilla M, et al. Selective inhibition of cocaine-seeking behaviour by a partial dopamine D3 receptor agonist [published correction appears in Nature 1999 Sep 23;401(6751):403]. Nature. 1999;400(6742):371-375. |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
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| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |