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抑制剂描述:

产品名称:(+)-Bicuculline

产品别名:见爱必信官网

英文别名:(+)-Bicuculline

靶点:GABA Receptor

CAS:485-49-4

纯度:≥98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

(+)-Bicuculline is an antagonist of the GABA_A receptor. (+)-Bicuculline is the parent compound of the water soluble N-methyl derivatives (-)-Bicuculline methiodide and (-)-Bicuculline methobromide . Antagonism of the GABA_A receptor by (+)-Bicuculline blocks the neurotransmission inhibition function of the GABA system in vitro.

溶解性:DMSO :21 mg/mL warmed (57.16 mM)

体外研究:

(+)-Bicuculline (1-100μM) dose-dependently inhibits the Cl- conductance generated by 40 μM GABA. (+)-Bicuculline also inhibits the agonist action of GABA at 40 μM at α1β2γ2L receptors. (+)-Bicuculline at 1 and 3 μM increases GABA EC50 values 1.6 times (41.0-67.0 μM) and 3.6 times (36.1-129.0 μM), respectively. Atα1β2γ2L GABAA receptors, (+)-bicuculline displays the general property of the competitive antagonist, producing a parallel shift of GABA concentration-effect curves and having no effect on the maximal response of GABA. In addition to being a potent GABAA receptor antagonist, (+)-bicuculine also blocks Ca2+-activated potassium channels.

体内研究:

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