产品
编 号:F018022
分子式:C15H18BrN3O3
分子量:368.23
产品类型
结构图
CAS No: 104104-50-9
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生物活性:
Gabazine is a selective and competitive antagonist of GABAA receptor, with an IC50 of ~0.2 μM for GABA receptor.
体外研究:
Both bicuculline and Gabazine (SR 95531) have been characterized as competitive inhibitors of GABA binding to the GABAA receptor. Gabazine is more potent than bicuculline at blocking currents elicited by GABA, with an IC50 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.