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.
This is a preview of subscription content, log in via an institution to check access.
Similar content being viewed by others
References
G. G. Neznamov, S. A. Syunyakov, D. V. Chumakov, et al., Psikhiatriya Psikhofarmakoter., 4(8), 8–13 (2006).
I. P. Galaeva, T. L. Garibova, T. A.Voronina, et al., Byull. Eksp. Biol. Med., 140(11), 545–548 (2005).
T. A. Antipova, D. S. Sapozhnikova, L. Yu. Bakhtina, et al., Eksp. Klin. Farmakol., 72(1), 12–14 (2009).
J. Cuevas, A. Behensky, W. Deng, et al., J. Pharmacol. Exp. Ther., 339(1), 152–160 (2011).
A. O. Viglinskaya, G. B. Kolyvanov, A. A. Litvin, et al., Byull. Eksp. Biol. Med., 143(5), 528–530 (2007).
B. Wunsch, Curr. Pharm. Des., 18(7), 930–937 (2012).
T. Ya. Mozhaeva, M. A. Yarkova, V. P. Lezina, et al., Khim.-farm. Zh., 45(3), 19–22 (2011).
RF Pat. No. 2,061,686; Byull. Izobret., 16, (1996).
M. E. Ganapathy, P. D. Prasad, W. Huang, et al., J. Pharmacol. Exp. Ther., 289(1), 251–260 (1999).
N. A. Colabufo, F. Berardi, M. Contino, et al., Naunyn-Schmiedeberg’s Arch. Pharmacol., 368(2), 106–112 (2003).
T. Hayashi and T. Su, Curr. Neuropharmacol., 3(4), 267–280 (2005).
S. Y. Tsai, T. Hayashi, T. Mori, et al., Cent. Nerv. Syst. Agents Med. Chem., 9(3), 184–189 (2009).
S. D. Banister and M. Kassiou, Curr. Pharm. Des., 18(7), 884–901 (2012).
Author information
Authors and Affiliations
Additional information
Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 46, No. 6, pp. 12 – 13, June, 2012.
Rights and permissions
About this article
Cite this article
Ryaskina, E.V., Voronin, M.V. & Seredenin, S.B. Interaction of 2-mercaptobenzimidazole derivatives with sigma-1 receptors. Pharm Chem J 46, 334–336 (2012). https://doi.org/10.1007/s11094-012-0793-1
Received:
Published:
Issue Date:
DOI: https://doi.org/10.1007/s11094-012-0793-1