Interaction of 2-mercaptobenzimidazole derivatives with sigma-1 receptors

Research paper by E. V. Ryaskina, M. V. Voronin, S. B. Seredenin

Indexed on: 10 Oct '12Published on: 10 Oct '12Published in: Pharmaceutical Chemistry Journal


The interaction of afobazole and its main metabolite M-11 {2-[2-(3-oxomorpholin-4-yl)ethylthio]-5-ethoxybenzimidazole hydrochloride} with sigma-1 (σ1) receptors was studied in vitro in radioligand binding experiments on human T-cell lymphoblast-like cell line. Afobazole exhibited ligand properties towards σ1 receptors with IC50 = 7.1 × 10–6 M. For M-11, the corresponding value was IC50 = 9.6×10–4 M. Experiments in vitro on CD-1 mouse brain homogenate established that afobazole interacted with σ1 receptors (IC50 = 1.37×10–5 M) whereas M-11 did not show affinity towards σ1 receptors (IC50 > 5×10–4 M). Radioligand analysis results on mongrel CD-1 mice confirmed the results obtained on human T-cell lymphoblast-like cell line and led to the conclusion that σ1 receptors did not contribute to the pharmacological effects of M-11.