Williams M, Risley E A
J Neurochem. 1984 Mar;42(3):745-53. doi: 10.1111/j.1471-4159.1984.tb02746.x.
The anthelmintic macrolide, ivermectin, enhances the binding of benzodiazepine agonist ( [3H]-diazepam) and antagonist ( [3H] beta-carboline ethyl ester) ligands to rat cortical and cerebellar membrane preparations. Enhancement of benzodiazepine agonist binding is partially additive with that of gamma-aminobutyric acid (GABA) and is inhibited by etazolate, bicuculline, and the steroid GABA antagonist R5135. Ivermectin-stimulated benzodiazepine antagonist binding is enhanced by bicuculline and inhibited by GABA and etazolate. The modulatory effects of bicuculline are chloride-dependent. The stimulatory effects of ivermectin, while quantitatively different in cortex and cerebellum, are qualitatively similar in both brain regions and are reduced in the presence of chloride. Ivermectin effects on benzodiazepine ligand binding to the benzodiazepine receptor complex and the differences in the effects of GABA, bicuculline, and R5135 on ivermectin-stimulated agonist and antagonist binding may provide evidence for distinct differences in the recognition sites for the two classes of benzodiazepine receptor ligand and their interactions with other components of the receptor complex.
抗蠕虫大环内酯类药物伊维菌素可增强苯二氮䓬激动剂（[³H] - 地西泮）和拮抗剂（[³H]β - 咔啉乙酯）配体与大鼠皮质和小脑膜制剂的结合。苯二氮䓬激动剂结合的增强与γ - 氨基丁酸（GABA）的增强部分相加，并受到乙氯唑胺、荷包牡丹碱和类固醇GABA拮抗剂R5135的抑制。伊维菌素刺激的苯二氮䓬拮抗剂结合可被荷包牡丹碱增强，并受到GABA和乙氯唑胺的抑制。荷包牡丹碱的调节作用依赖于氯离子。伊维菌素的刺激作用虽然在皮质和小脑中在数量上有所不同，但在两个脑区在质量上相似，并且在有氯离子存在时会减弱。伊维菌素对苯二氮䓬配体与苯二氮䓬受体复合物结合的影响，以及GABA、荷包牡丹碱和R5135对伊维菌素刺激的激动剂和拮抗剂结合的影响差异，可能为两类苯二氮䓬受体配体的识别位点及其与受体复合物其他成分的相互作用存在明显差异提供证据。
