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Pharmacological Properties of SM-3997: A New Anxioselective Anxiolytic Candidate

Pharmacological properties of SM-3997 (3aα,4β,7β,7aα-hexahydro-2-(4-(4-(2-pyrimidinyl)-1 -piperazinyl)-butyl)-4,7-methano-1 H-isoindole-1,3(2H)-dione dihydrogen citrate) have been examined in rats and mice. SM-3997 showed a dose-related anticonflict activity in rats in a water lick conflict paradigm...

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Published in:Japanese journal of pharmacology 1987, Vol.45 (4), p.493-500
Main Authors: SHIMIZU, Hiroshi, HIROSE, Akira, TATSUNO, Tohru, NAKAMURA, Mitsutaka, KATSUBE, Junki
Format: Article
Language:English
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Summary:Pharmacological properties of SM-3997 (3aα,4β,7β,7aα-hexahydro-2-(4-(4-(2-pyrimidinyl)-1 -piperazinyl)-butyl)-4,7-methano-1 H-isoindole-1,3(2H)-dione dihydrogen citrate) have been examined in rats and mice. SM-3997 showed a dose-related anticonflict activity in rats in a water lick conflict paradigm, and it had no effect on water consumption in a spontaneous water drinking test. The potency of SM-3997 appeared to be equal to that of buspirone and about one-half that of diazepam. No tolerance to the anticonflict activity of SM-3997 was observed following 5 and 10 consecutive days of treatment. Unlike diazepam, SM-3997 had no anticonvulsant effect and had very weak muscle relaxant and hypnotic effects. On the other hand, SM-3997 and buspirone exhibited dopamine antagonistic action, although the potency of SM-3997 was less than one fourth that of buspirone. These results show that SM-3997 is a new anxioselective anxiolytic agent which is weaker than buspirone in the dopaminergic neuron system.
ISSN:0021-5198
1347-3506
DOI:10.1016/S0021-5198(19)43370-2