| Literature DB >> 11504649 |
G McCort1, C Hoornaert, M Aletru, C Denys, O Duclos, C Cadilhac, E Guilpain, G Dellac, P Janiak, A M Galzin, M Delahaye, F Guilbert, S O'Connor.
Abstract
Quinolin-2-ones bearing a heteroaryl-piperazine linked by a two carbon chain at the 3- or 4-position were synthesised and evaluated as mixed 5-HT(1B)/5-HT(2A) receptor antagonists. Potent mixed antagonists were obtained with thieno[3,2-c]pyridine derivatives. In this series, compound 2.1 (SL 65.0472) proved to be functional antagonist at both the 5-HT(2A) receptor (rat in vivo 5-HT-induced hypertension model) and the 5-HT(1B) receptor (dog in vitro saphenous vein assay).Entities:
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Year: 2001 PMID： 11504649 DOI： 10.1016/s0968-0896(01)00118-3
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641