In our pursuit to identify selective ligands for Bz/GABA(A) receptor subtypes, a novel pyrazolo[1,5-a]pyrimidine derivative (4), the azaisostere of zolpidem, was synthesized and evaluated in vitro on bovine brain homogenate and on recombinant benzodiazepine receptors (alphaxbeta2/3gamma2, x = 1-3, 5) expressed in HEK293 cells. Compound 4 displayed affinity only for alpha1beta2gamma2 subtype (K(i) = 31 nM), and in an in-depth, in vivo study it revealed sedative and anxiolytic-like properties without any amnesic and myorelaxant effects in rodents.
Autori interni: | |
Autori: | SELLERI S; BRUNI F; COSTAGLI C; COSTANZO A; GUERRINI G; CICIANI G; GRATTERI P; BESNARD F; COSTA B; MONTALI M; MARTINI C; FOHLIN J; DE SIENA G; AIELLO PM |
Titolo: | A novel selective GABA(A) alpha1 receptor agonist displaying sedative and anxiolytic-like properties in rodents |
Anno del prodotto: | 2005 |
Appare nelle tipologie: | 1.1 Articolo in rivista |
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