Zaleplon and triazolam: drug discrimination, plasma levels, and self-administration in baboons

Zaleplon is a chemically novel hypnotic that preferentially binds alpha (1) -subunit containing subtypes of the alpha beta gamma configuration of the g amma -aminobutyric acid (GABA)(A) receptor. Zaleplon and the non-subtype-se lective hypnotic triazolam occasioned 100% drug-appropriate responding in b aboons trained to discriminate lorazepam or pentobarbital from vehicle. Flu mazenil shifted the zaleplon generalization gradient at least five-fold to the right. A plasma elimination half-life of 6-8 h for oral 10 mg/kg zalepl on and 0.32 mg/kg triazolam was paralleled by discriminative control for 7 h. Zaleplon maintained self-injection greater than vehicle, as did comparis on doses of the similarly selective hypnotic zolpidem and triazolam. Concur rent food-maintained responding increased during self-injection of all thre e drugs. Preferential binding at this alpha (1)-containing GABA, subtype di d not diminish the benzodiazepine (Bzs)-like behavioral effects of zaleplon . (C) 2000 Elsevier Science Ireland Ltd. All rights reserved.