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ID: ALA1155434

Journal: Bioorg Med Chem Lett

Title: Discovery of a new series of 5-HT1A receptor agonists.

Authors: Franchini S, Prandi A, Sorbi C, Tait A, Baraldi A, Angeli P, Buccioni M, Cilia A, Poggesi E, Fossa P, Brasili L.

Abstract: Starting from compounds previously identified as alpha(1)-adrenoceptor antagonists that were also found to bind to the 5-HT(1A) receptor, in an attempt to separate the two activities, a new series of 5-HT(1A) receptor agonists was identified and shown to have high potency and/or high selectivity. Of these, compound 13, which combines high selectivity (5-HT(1A)/alpha(1)=151) and good agonist potency (pD(2)=7.82; E(max)=76), was found to be the most interesting.

CiteXplore: 20185311

DOI: 10.1016/j.bmcl.2010.01.030