PMID: 22359984Mar 1, 2012Paper

Sensitizing effect of tacrine on M-cholinergic receptors in gastric smooth muscle of rats

Folia medica
Natalia A PrisadovaA Krustev

Abstract

To find if tacrine exerts a sensitizing effect on the cholinergic receptors of gastric smooth muscles, and study some of the mechanisms inducing it and measure the relative intensity of tacrine's effects on contractile activity. Isometric recording of the mechanical activity of gastric smooth muscle preparations; determination of acetyl-cholinesterase activity in smooth-muscle tissue homogenates using Ellman's method. We found that the threshold concentration for tacrine not reducing the acetylcholinesterase activity and not having an effect on the smooth muscle preparations was 1 x 10(-8) mol/l. This concentration, however, significantly increased the acetylcholine-induced contraction compared with the controls, after the smooth-muscle tissue was incubated for 60 or 100 min. Treating smooth-muscle preparations with tacrine in a concentration of 5 x 10(-6) mol/l triggered a contraction induced by the drug's anti-cholinesterase activity. A secondary contraction was induced after 38.6 +/- 5.6 min. There was no secondary contraction after the control acetylcholine-induced effect. Atropine (1 x 10(-6) mol/l) inhibits this effect. Preliminary treatment of smooth muscle preparations with hexamethonium (1 x 10(-6) mol/l) did not chang...Continue Reading

References

May 15, 1999·Dementia and Geriatric Cognitive Disorders·H AllainP Brissot
May 19, 2000·Neuroreport·G JeyarasasingamM Quik
Jul 1, 1961·Biochemical Pharmacology·G L ELLMANR M FEATHER-STONE
May 20, 2006·American Journal of Physiology. Gastrointestinal and Liver Physiology·Enrique Rozengurt
Sep 26, 2006·European Journal of Pharmacology·Yuki Takada-TakatoriAkinori Akaike
Jan 16, 2007·Canadian Journal of Physiology and Pharmacology·Atanas D KrustevNatalia A Prissadova

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