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Bioorg Med Chem Lett. 2010 Mar 15;20(6):2017-20. doi: 10.1016/j.bmcl.2010.01.030. Epub 2010 Feb 4.

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

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1
Dipartimento di Scienze Farmaceutiche, Università degli Studi di Modena e Reggio Emilia, Modena, Italy.

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.

PMID:
20185311
DOI:
10.1016/j.bmcl.2010.01.030
[Indexed for MEDLINE]

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