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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

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Selleri, S. et al.

Selleri, Bruni, Costagli, Costanzo, Guerrini, Ciciani, Gratteri, Besnard, Costa, Montali, Martini, Fohlin, De Siena, Aiello,

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

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.[1]

References

A novel selective GABA(A) alpha1 receptor agonist displaying sedative and anxiolytic-like properties in rodents. 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, P.M. J. Med. Chem. (2005) [Pubmed]

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