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.

A novel selective GABA(A) alpha1 receptor agonist displaying sedative and anxiolytic-like properties in rodents

COSTA, BARBARA;MARTINI, CLAUDIA;
2005

Abstract

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.
Selleri, S; Bruni, F; Costagli, C; Costanzo, A; Guerrini, G; Ciciani, G; Gratteri, P; Besnard, F; Costa, Barbara; Montali, M; Martini, Claudia; Fohlin, J; DE SIENA, G; Aiello, Pm
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11568/203907
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