Discovery of a new series of 5-HT1A receptor agonists.
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.
Franchini
Silvia
S
Dipartimento di Scienze Farmaceutiche, Università degli Studi di Modena e Reggio Emilia, Modena, Italy.
Prandi
Adolfo
A
Sorbi
Claudia
C
Tait
Annalisa
A
Baraldi
Annamaria
A
Angeli
Piero
P
Buccioni
Michela
M
Cilia
Antonio
A
Poggesi
Elena
E
Fossa
Paola
P
Brasili
Livio
L
D055808:Drug Discovery; D058825:Serotonin 5-HT1 Receptor Agonists
D058825:Serotonin 5-HT1 Receptor Agonists