Starting from compounds previously identified as a1-adrenoceptor antagonists that were also found to bind to the 5-HT1A receptor, in an attempt to separate the two activities, a new series of 5-HT1A receptor agonists was identified and shown to have high potency and/or high selectivity. Of these, compound 13, which combines high selectivity (5-HT1A/a1 = 151) and good agonist potency (pD2 = 7.82; Emax = 76), was found to be the most interesting.
Discovery of a new series of 5-HT1A receptor agonists
FOSSA, PAOLA;
2010-01-01
Abstract
Starting from compounds previously identified as a1-adrenoceptor antagonists that were also found to bind to the 5-HT1A receptor, in an attempt to separate the two activities, a new series of 5-HT1A receptor agonists was identified and shown to have high potency and/or high selectivity. Of these, compound 13, which combines high selectivity (5-HT1A/a1 = 151) and good agonist potency (pD2 = 7.82; Emax = 76), was found to be the most interesting.
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