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The relationship between binding of antipsychotic drugs and sigma psychotomimetic opiates to binding sites for the sigma agonist (+)-[3H]SKF 10,047 (N-allylnormetazocine) and to dopamine D2 sites was investigated. In guinea pig brain membranes, (+)-[3H]SKF 10,047 bound to a single class of sites with a Kd of 4 X 10(-8) M and a Bmax of 333 fmol/mg of(More)
Conflict behavior is a powerful tool to reveal relevant pharmacologic correlates of the therapeutically desirable properties of benzodiazepine antianxiety compounds. The predictability of its clinical effectiveness in psychoneuroses is very high, and important quantitative and qualitative differences between compounds in this chemical class can be shown(More)
8-Chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5-a][1,4]benzodiazepine (midazolam, Ro 21-3981, Dormicum) is an imidazobenzodiazepine whose salts are soluble and stable in aqueous solution. It has a quick onset and, due to rapid metabolic inactivation, a rather short duration of action in all species studied. Midazolam has a similar pharmacologic potency(More)
The purpose of the study was to develop a tooth pulp stimulation procedure in the awake, freely moving rat and to then quantitatively assess the analgesic effects of compounds reported to act on mu and/or kappa receptors. The mu receptor agonists produce a biphasic (primary and secondary slope) dose-response curve (DRC) whereas kappa agonist and mixed(More)
Dose-response profiles were determined for chlordiazepoxide, diazepam and N-desmethyldiazepam in a squirrel monkey punishment (conflict) procedure. The monkeys were trained to lever press under a food-maintained concurrent schedule consisting of an unpunished 6-minute variable interval (VI) schedule, and a 1.5-minute VI schedule, on which responses were(More)
The mechanism of action of benzodiazepines is considered from a behavioral pharmacology perspective, particularly with respect to methods that involve suppression of responding, such as the punishment-conflict model. Four biochemical hypotheses of current interrest are reviewed. 1) Several lines of evidence suggest that the benzodiazepine receptor in brain(More)