克他命
- CAS号:104104-50-9
- 英文名:SR-95531
- 中文名:克他命
- CBNumber:CB9356638
- 分子式:C15H18BrN3O3
- 分子量:368.23
- MOL File:104104-50-9.mol
- 熔点 :200 °C(Solv: ethanol (64-17-5))
- 储存条件 :Store at RT
- 溶解度 :DMSO: 30 mg/mL
- 形态 :solid
- 颜色 :white
- WGK Germany :3
克他命性质、用途与生产工艺
- 生物活性 Gabazine是 GABAA 受体 的选择性竞争性拮抗剂,其对 GABA 受体的 IC50 值为 ~0.2 μM。
-
靶点
0.2 μM (GABA receptor).
-
体外研究
Both bicuculline and Gabazine (SR 95531) have been characterized as competitive inhibitors of GABA binding to the GABA A receptor. Gabazine is more potent than bicuculline at blocking currents elicited by GABA, with an IC 50 for currents elicited by 3 μM GABA of ~0.2 μM and a Hill coefficient of 1.0. Gabazine reduces the currents elicited by 10 μM alphaxalone by ~30%, for responses of receptors containing wildtype β2 subunits. The concentration of Gabazine requires producing half the maximal block is ~0.2 μM. Gabazine also could only produce a partial block of currents gated by 300 μM pentobarbital. The maximal reduction, again, is ~30%, and the concentration of Gabazine required to produce half the maximal block is ~0.15 μM.
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