Influence of the 5-HT6Receptor on Acetylcholine Release in the Cortex: Pharmacological Characterization of 4-(2-Bromo-6-pyrrolidin-1-ylpyridine-4-sulfonyl)phenylamine, a Potent and Selective 5-HT6Receptor Antagonist
Journal of Medicinal Chemistry2003Vol. 46(7), pp. 1273–1276
Citations Over TimeTop 10% of 2003 papers
Claus Riemer, Edilio Borroni, Bernard Levet‐Trafit, James R. Martin, Sonia Poli, Richard H. Porter, Michael Bös
Abstract
A small series of aryl pyridyl sulfones has been prepared and investigated for its 5-HT(6) receptor binding properties. Thereof, pyrrolidinyl derivative 11 proved to be a very potent (pK(i) 9) and selective 5-HT(6) 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-HT(6) receptors and cholinergic neurotransmission could be shown, supporting the therapeutic potential of 5-HT(6) receptors in the treatment of cognitive deficits.
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