Theβ-lactam antibiotices, penicillin-G and cefoselis have different mechanisms and sites of action at GABA_A receptors

摘要

The action of theβ-lactam antibiotics, penicillin-G(PCG)and cefoselis(CFSL)on GABA_A receptors(GABA_A-R)was investigated using the two-electrode voltage clamp technique and Xenopus oocyte expressed murine GABA_A-R. Murine GABA_A-Rs were expressed in Xenopus oocytes by injecting cRNA that encoded for each Subunit(α1,β2, andγ2)and the effects of PCG and CFSL on theα1β2γ2s subunit receptors were Examined using two-electrode voltage clamp. Using theα1β2γ2s GABA_A-R, PCG and CFSL Inhibited GABA_A-induced currents in a concentration-dependent manner, with IC_50s of 557.1±125.4 And 185.0±26.6μM, respectively.