| Title : Influence of the 5-HT6 receptor on acetylcholine release in the cortex: pharmacological characterization of 4-(2-bromo-6-pyrrolidin-1-ylpyridine-4-sulfonyl)phenylamine, a potent and selective 5-HT6 receptor antagonist - Riemer_2003_J.Med.Chem_46_1273 |
| Author(s) : Riemer C , Borroni E , Levet-Trafit B , Martin JR , Poli S , Porter RH , Bos M |
| Ref : Journal of Medicinal Chemistry , 46 :1273 , 2003 |
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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. |
| PubMedSearch : Riemer_2003_J.Med.Chem_46_1273 |
| PubMedID: 12646038 |
Riemer C, Borroni E, Levet-Trafit B, Martin JR, Poli S, Porter RH, Bos M (2003)
Influence of the 5-HT6 receptor on acetylcholine release in the cortex: pharmacological characterization of 4-(2-bromo-6-pyrrolidin-1-ylpyridine-4-sulfonyl)phenylamine, a potent and selective 5-HT6 receptor antagonist
Journal of Medicinal Chemistry
46 :1273
Riemer C, Borroni E, Levet-Trafit B, Martin JR, Poli S, Porter RH, Bos M (2003)
Journal of Medicinal Chemistry
46 :1273