Selleri, Silvia Bruni, Fabrizio Costagli, Camilla Costanzo, Annarella Guerrini, Gabriella Ciciani, Giovanna Gratteri, Paola Besnard, François Costa, Barbara Montali, Marina Martini, Claudia Fohlin, Jonna De Siena, Gaetano Aiello, Petra Malmberg A Novel Selective GABA<sub>A</sub> α1 Receptor Agonist Displaying Sedative and Anxiolytic-like Properties in Rodents In our pursuit to identify selective ligands for Bz/GABA<sub>A</sub> receptor subtypes, a novel pyrazolo[1,5-<i>a</i>]pyrimidine derivative (<b>4</b>), the azaisostere of zolpidem, was synthesized and evaluated in vitro on bovine brain homogenate and on recombinant benzodiazepine receptors (αxβ2/3γ2, <i>x </i>= 1−3, 5) expressed in HEK293 cells. Compound <b>4</b> displayed affinity only for α1β2γ2 subtype (<i>K</i><sub>i</sub> = 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. nM;vivo study;rodent;ligand;benzodiazepine;K i;affinity;amnesic;zolpidem;receptor subtypes;Properties;Bz;HEK 293 cells;pursuit;brain homogenate;pyrazolo;azaisostere;α1 Receptor Agonist;Compound 4;Sedative;sedative;α1β2γ2 subtype;Rodent;pyrimidine;myorelaxant effects;GABA 2005-10-20
    https://acs.figshare.com/articles/journal_contribution/A_Novel_Selective_GABA_sub_A_sub_1_Receptor_Agonist_Displaying_Sedative_and_Anxiolytic_like_Properties_in_Rodents/3261715
10.1021/jm058002n.s001