Influence of the 5-HT6 receptor on acetylcholine release in the cortex: pharmacological characterization of 4-(2-bromo-6-pyrrolidin-1-ylpyridine-4-sulfonyl) …

…, E Borroni, B Levet-Trafit, JR Martin, S Poli…

Index: Riemer, Claus; Borroni, Edilio; Levet-Trafit, Bernard; Martin, James R.; Poli, Sonia; Porter, Richard H. P.; Boes, Michael Journal of Medicinal Chemistry, 2003 , vol. 46, # 7 p. 1273 - 1276

Full Text: HTML

Citation Number: 176

Abstract

A small series of aryl pyridyl sulfones has been prepared and investigated for its 5-HT6 receptor binding properties. Thereof, pyrrolidinyl derivative 11 proved to be a very potent (p K i 9) and selective 5-HT6 receptor antagonist. By means of in vivo microdialysis in the frontal cortex and a passive avoidance paradigm, where 11 reversed a scopolamine induced retention deficit, a functional correlation between 5-HT6 receptors and cholinergic ...