(+)-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.

A GABA A receptor antagonist

≥98%

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

毕扣扣灵(碱)，荷包牡丹碱；山乌龟碱

淡黄色结晶粉末

DMSO ：21 mg/mL warmed (57.16 mM)

GABAA receptor

(+)-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.

[1] Huang SH, et al. Eur J Pharmacol, 2003, 464(1), 1-8.
[2] Khawaled R, et al. Pflugers Arch, 1999, 438(3), 314-321.