Sedative effects of PK 9084 and PK 8165, alone and in combination with chlordiazepoxide.
1 The sedative effects in rats of two phenylquinolines, PK 9084 and PK 8165 (5-50 mg/kg), were examined in a holeboard: both when given alone and when given in conjunction with chlordiazepoxide (5 mg/kg). 2 Both phenylquinolines produced significant dose-related decreases in locomotor activity and rearing, with an ED50 about twice that for chlordiazepoxide. 3 When the phenylquinolines were combined with chlordiazepoxide the degree of sedation was equal to that seen with either drug given alone, whichever produced the greater sedation; the sedative effects of the two drugs were never additive. 4 PK 9084 (10 and 50 mg kg) significantly reduced rectal temperature, as did chlordiazepoxide (5 mg/kg), but there was no addition nor interaction of their effects. 5 Both phenylquinolines also reduced exploratory head-dipping, as did chlordiazepoxide, but in combination they antagonized each other's effects. 6 The classification of the phenylquinolines as non-sedative anxiolytics, acting as agonists at the benzodiazepine receptors needs revision.
D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects*; D001831:Body Temperature / Q000187:drug effects; D002707:Chlordiazepoxide / Q000494:pharmacology*; D004347:Drug Interactions; D005106:Exploratory Behavior / Q000187:drug effects; D006993:Hypnotics and Sedatives; D008297:Male; D009043:Motor Activity / Q000187:drug effects; D011804:Quinolines / Q000494:pharmacology*; D051381:Rats
D006993:Hypnotics and Sedatives; D011804:Quinolines; D002707:Chlordiazepoxide; C030079:PK 9084; C030078:pipequaline