Pharmacological studies on triazine derivatives V Sedative and neuroleptic actions of 2-amino-4-[4-(2-hydroxyethyl)-piperazin-1-yl]-6-trifluoromethyl-s-triazine (TR-10).
Pharmacological properties of 2 amino-4-[4-(2-hydroxyethyl)-piperazin-1-yl]-6-trifluoromethyl-s-triazine (TR-10) were investigated in mice and rats. Chlorpromazine served as a reference compound. Tr-10 expressed in general the pharmacological profiles as neuroleptic ascertained by anti-methamphetamine activity, supression of conditioned avoidance response, taming effects, decrease in exploratory behavior and cataleptogenic activity. Among these effects, anti-methamphetamine action was most potent. Different from chlorpromazine, TR-10 showed a similar pharmacological activity pattern in the intraperitoneal and oral routes of administration as depicted from ED50/LD50 values. Although the effects relevant to neuroleptics were less potent than chlorpromazine, such were seen with TR-10 at lower doses than those causing muscle relaxation. TR-10 significantly depressed the spontaneous motor activity but showed no anti-convulsant action in mice. Hypothermic action, potentiating effects of hypnotics and alpha-adrenergic blocking action, characteristic to chlorpromazine, were very weak for TR-10. TR-10 also showed low toxicity in mice (LD50 = 820 mg/kg p.o., 465 mg/kg i.p.) compared with that of chlorpromazine (LD50 = 370 mg/kg p.o., 228 mg/kg i.p.).
D000085:Acetates / Q000037:antagonists & inhibitors; D000317:Adrenergic alpha-Antagonists; D000374:Aggression / Q000187:drug effects; D000818:Animals; D000927:Anticonvulsants; D001362:Avoidance Learning / Q000187:drug effects; D001831:Body Temperature / Q000187:drug effects; D002375:Catalepsy / Q000139:chemically induced; D002746:Chlorpromazine / Q000494:pharmacology; D005106:Exploratory Behavior / Q000187:drug effects; D006801:Humans; D006993:Hypnotics and Sedatives; D008297:Male; D008694:Methamphetamine / Q000037:antagonists & inhibitors; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D009125:Muscle Relaxants, Central; D051381:Rats; D012890:Sleep / Q000187:drug effects; D013239:Stereotyped Behavior / Q000187:drug effects; D014149:Tranquilizing Agents; D014227:Triazines / Q000494:pharmacology* / Q000633:toxicity
D000085:Acetates; D000317:Adrenergic alpha-Antagonists; D000927:Anticonvulsants; D006993:Hypnotics and Sedatives; D009125:Muscle Relaxants, Central; D014149:Tranquilizing Agents; D014227:Triazines; D008694:Methamphetamine; D002746:Chlorpromazine