Folia Pharmacologica Japonica
Online ISSN : 1347-8397
Print ISSN : 0015-5691
ISSN-L : 0015-5691
Pharmacology of N-methyl-9, 10-ethanoanthracene-9(1OH)-methylamine hydrochloride (benzoctamine), a new psychotropic agent. Part 1. Effects on the central nervous system.
Kazuo TAKAHAMATakeshi MIYATAYoshitoshi KASÉ
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1977 Volume 73 Issue 2 Pages 151-176

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Abstract
Tranquilizing and other related actions of benzoctamine (Benz), N-methyl-9, 10-ethanoanthracene-9(10 H)-methylamine hydrochloride were studied in comparison with those of chlorpromazine (CPZ) and chlordiaze-poxide (CDP). Toxic symptoms in mice and rats were due to CNS depression. This agent was 4.2 times (s.c.) and 6.1 times (i.p.) as toxic as CDP in mice, 3.8 times (i.p.) more toxic than CDP in rats; 1.9 times, equally and about half as toxic as CPZ, respectively. A potent muscle relaxant action was demonstrated in mice, and a decerebrate rigidity in cats was depressed with Benz. Tonic extension of mice induced by electro-shock was suppressed but chemo-shock was not inhibited. Discriminative and non-discriminative conditioned avoidance responses were depressed in rats. Benz suppressed both fighting behavior in mice and hyperemotionality in rats due to olfactory bulb ablation or long-term isolation; the effects were 1/4 to 1/2 of those of CPZ; 4 to 5 times and 1/2 to 1 time as potent as those of CDP in suppressing effects on fighting behavior and hyperemotionality, respectively. Hyperactivity caused by amphetamine or morphine was reduced, but amphetamine hyperactivity was facilitated in small doses. Benz did not antagonize hypothermia nor ptosis caused by reserpine in rats and apomorphine-induced vomiting was not inhibited in dogs. In small doses, depressing EEG patterns appeared at the limbic system; in large doses, the depression extended to the neocortex and mid-brain reticular formation. EEG arousal response was also depressed. Generally speaking, the effects of Benz on EEG were similar to those of CDP in small doses and those of CPZ in large doses. Thus Benz is a new type of tranquilizer with a potent muscle-relaxant action, and cannot be categorized with major or minor tranquilizers.
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