Behavioural effects of PK 8165 that are not mediated by benzodiazepine binding sites.
The phenylquinoline, PK 8165 (5-25 mg/kg), produced dose-related reductions in locomotor activity, rearing and exploratory head-dipping in a holeboard. Neither Ro 15-1788 (1, 10 or 20 mg/kg) nor CGS 8216 (1 or 10 mg/kg) was able to reverse the reductions in locomotor activity or rearing. This suggests that at least some of the behavioural effects of PK 8165 are not mediated by a site on the GABA-benzodiazepine receptor complex. This conclusion is supported by the recent report [9] that, whereas PK 8165 potently displaces benzodiazepines from their binding site in vitro, it is without effect in vivo.
D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects*; D001570:Benzodiazepinones / Q000494:pharmacology; D005106:Exploratory Behavior / Q000187:drug effects; D005442:Flumazenil; D008297:Male; D009043:Motor Activity / Q000187:drug effects; D011720:Pyrazoles / Q000494:pharmacology; D011804:Quinolines / Q000037:antagonists & inhibitors / Q000494:pharmacology*; D051381:Rats; D011963:Receptors, GABA-A / Q000502:physiology
D001570:Benzodiazepinones; D011720:Pyrazoles; D011804:Quinolines; D011963:Receptors, GABA-A; D005442:Flumazenil; C033830:2-phenylpyrazolo(4,3-c)quinolin-3(5H)-one; C030078:pipequaline