Description: Bicuculline methiodide is the methiodide salt of (+)-Bicuculline which is a natural product isolated from Dicentra cucullaria and is a novel, potent and competitive antagonist of GABAA receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels. (+)-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. It is a GABA-A-receptor antagonist and NMDA receptor potentiator used to study GABA signaling. It induces membrane depolarization and prolongs Ca- dependemtn action potentials in neurons.
References: Pflugers Arch. 1999 Aug;438(3):314-21; Eur J Pharmacol. 2003 Mar 7;464(1):1-8.
Related CAS: 53552-05-9 [(–)-Bicuculline methochloride]; 40709-69-1 (Bicuculline methiodide)