Pharmacological actions of SM-9018, a new neuroleptic drug with both potent 5-hydroxytryptamine2 and dopamine2 antagonistic actions.
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概要
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Pharmacological studies were undertaken to clarify the profile of cis-2-(4-(4-(1, 2-benzisothiazol-3-yl)-1-piperazinyl) butyl) hexahydro-1H-isoindole-1, 3-(2H)-dione hydrochloride (SM-9018), a new neuroleptic drug. SM-9018 had very high binding affinities for both 5-hydroxytryptamine<SUB>2</SUB> (5-HT<SUB>2</SUB>) and dopamine<SUB>2</SUB> (D<SUB>2</SUB>) receptors, unlike many other neuroleptics. SM-9018 also strongly inhibited 5-HT<SUB>2</SUB> receptor-mediated behavior such as tryptamine-induced clonic seizure and D<SUB>2</SUB> receptor-mediated behavior such as methamphetamine-induced hyperactivity, apomorphine-induced stereotypy and climbing behavior. SM-9018 possessed only a weak cataleptogenic activity, which may be clinically related to extrapyramidal side effects, despite its potent D<SUB>2</SUB> antagonistic activity. Moreover, SM-9018 induced weak central depressant effects such as inhibition of spontaneous locomotor activity and motor coordination, as compared with classical neuroleptics (haloperidol and chlorpromazine). These results suggest that SM-9018 is a new neuroleptic drug with both potent 5-HT<SUB>2</SUB> and D<SUB>2</SUB> antagonistic activities and with low cataleptogenic and central depressant activities.
著者
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SHIMIZU Hiroshi
Research Institute for Polymers and Textiles
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NAKAMURA Mitsutaka
Research and Development Center, Pharmaceuticals Division, Sumitomo Chemical Co., Ltd.
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Hirose Akira
Research Center For Advanced Science & Technology University Of Tokyo:dept.of Frontier Informati
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TANAKA Hiroyasu
Research Laboratories, Sumitomo Pharmaceuticals Co., Ltd.
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KATO Terufumi
Research Laboratories, Sumitomo Pharmaceuticals Co., Ltd.
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OHNO Yukihiro
Research Laboratories, Sumitomo Pharmaceuticals Co., Ltd.
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KATSUBE Junki
Research Laboratories, Sumitomo Pharmaceuticals Co., Ltd.
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SHIMIZU Hiroshi
Research Laboratories, Sumitomo Pharmaceuticals Co., Ltd.
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