| Literature DB >> 16219465 |
Andreas Kling1, Udo E W Lange, Helmut Mack, Margot H M Bakker, Karla U Drescher, Wilfried Hornberger, Charles W Hutchins, Achim Möller, Reinhold Müller, Martin Schmidt, Liliane Unger, Karsten Wicke, Kurt Schellhaas, Gerd Steiner.
Abstract
Novel 5-HT(1) autoreceptor ligands based on the N-4-aryl-piperazinyl-N'-ethyl-5,6,7,8-tetrahydropyrido[4', 3':4,5]thieno[2,3-d]pyrimidin-4(3H)-one core are described. Aiming at antidepressants with a novel mode of action our objective was to identify potent antagonists showing balanced affinities and high selectivity for the 5-HT(1A) and 5-HT(1B) receptors. Strategies for the development of dual 5-HT(1A) and 5-HT(1B) antagonists based on 1 and 2 as leads and the corresponding results are discussed. Isoquinoline analogue 33 displayed high affinity and an antagonistic mode of action for the 5-HT(1A) and the 5-HT(1B) receptors and was characterized further with respect to selectivity, electrically stimulated [(3)H]5-HT release and in vivo efficacy.Entities:
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Year: 2005 PMID： 16219465 DOI： 10.1016/j.bmcl.2005.04.077
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823