Harrison N L, Simmonds M A
Eur J Pharmacol. 1983 Jan 28;87(1):155-8. doi: 10.1016/0014-2999(83)90064-x.
The potency and site of action of Ro5-3663 as a GABA antagonist were investigated in the rat cuneate slice in vitro. A Schild plot for Ro5-3663 was clearly non-linear but enabled a pA2 value of 3.97 to be calculated. Combination studies using the 'classical' GABA antagonists bicuculline and picrotoxin indicated that Ro5-3663 acted at a separate site from bicuculline, but may share a common site with picrotoxin.
在体外大鼠楔状核切片中研究了Ro5-3663作为GABA拮抗剂的效力和作用位点。Ro5-3663的Schild图明显呈非线性,但仍能计算出pA2值为3.97。使用“经典”GABA拮抗剂荷包牡丹碱和印防己毒素的联合研究表明,Ro5-3663的作用位点与荷包牡丹碱不同,但可能与印防己毒素有共同位点。