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Ion Channel Topography of the Neuronal Nicotinic Acetylcholine Receptor: Pharmacochemical Approaches |
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| Authors: | V. E. Gmiro N. B. Brovtsyna S. E. Serdyuk N. Ya. Lukomskaya |
| Affiliation: | (1) Russian Academy of Medical Sciences, Institute of Experimental Medicine, Kamennoostrovskii pr. 69/71, St. Petersburg, 197022, Russia;(2) Russian Academy of Sciences, Sechenov Institute of Evolutionary Physiology and Biochemistry, pr. Morisa Toreza 44, St. Petersburg, 194223, Russia;(3) Donetsk Medical University, pr. Il'icha 16, Donetsk, 340003, Ukraine |
| Abstract: | Forty-three bisammonium ganglionic blockers were synthesized to study the structure of the ion channel of nicotinic acetylcholine receptor. The conformational parameters of these blockers were studied, and their effects toward the ganglionic transmission in situ on the sympathetic feline superior cervical ganglia and in vitro on the parasympathetic guinea-pig small intestine ganglia were determined. A model of the binding site for the bisammonium ganglionic blockers in the neuronal ion channel was proposed. |
| Keywords: | conformational analysis ganglionic blockers ion channel neuronal nicotinic acetylcholine receptor parasympathetic ganglion structure– activity relationship sympathetic ganglion |
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