Dopamine Receptor Affinities in Vitro and Stereotypic Activities in Vivo of Cabergoline in Rats
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概要
- 論文の詳細を見る
An ergot alkaloid derivative, cabergoline, and its metabolites were investigated for their affinities for dopamine D_1 and D_2 receptors in rat striatum in vitro in comparison with those of bromocriptine and pergolide. The affinity for D_1 receptors was in the following order : pergolide>des-dimethylaminopropyl cabergoline (FCE21904)>cabergoline≧bromocriptine≧des-methyl cabergoline (FCE27395)≧des-ethylcarbamoyl cabergoline (FCE21590). From the effects of GTP on these affinities for the D_1 receptor, cabergoline, some of its metabolites, and pergolide were characterized as agonists in contrast to bromocriptine which was classified as an antagonist. The affinity for D_2 receptors was ranked as follows : pergolide≧cabergoline≧FCE27395≧FCE21904>bromocriptine>FCE21590>carboxylic acid-type derivative of cabergoline (FCE21589). The affinity of each compound for the D_2 receptor was much higher than that for the D_1 receptor. The selectively of cabergoline for the D_2 receptor was higher than those of bromocriptine and pergolide. Furthermore, these ergot alkaloids were investigated for eliciting stereotypy after subcutaneous administration to normal rats. Pergolide potently induced stereotypy at doses of 0.5 and 1.0 mg/kg, cabergoline slightly induced it only at a high dose of 2.0 mg/kg, whereas bromocriptine did not induce it at any of the doses tested, 10-40 mg/kg. These results suggest that pharmacological properties of cabergoline for the D_1 and D_2 receptors differ from those of bromocriptine and pergolide.
- 公益社団法人日本薬学会の論文
- 1996-09-15
著者
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小島 政芳
Fuji Photo Film Co. Ltd. Ashigara Research Laboratories
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Arai Nobuhiko
Central Research Laboratories Kissei Pharmaceutical Co. Ltd.
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Arai Nobuhiko
キッセイ薬品工業
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Kojima Masami
Central Research Laboratory Kissei Pharmaceutical
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MIYAGI Masaharu
Pharmaceutical Laboratories, Kissei Pharmaceutical Co., Ltd.,
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Kojima M
Department Of Hospital Pharmacy Mie University School Of Medicine
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Itoh Fumiaki
Central Research Laboratories Kissei Pharmaceutical Co. Ltd.
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UJIIE Arao
Central Research Laboratories, Kissei Pharmaceutical Co., Ltd.
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Ujiie A
Central Research Laboratories Kissei Pharmaceutical Co. Ltd.
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Ujiie Arao
Central Research Laboratories Kissei Pharmaceutical Co. Ltd.
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TAYA Fumie
Central Research Laboratory, Kissei Pharmaceutical
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MIYAGI Masaharu
Central Research Laboratories, Kissei Pharmaceutical Co., Ltd.,
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ISAJI Masayuki
Central Research Laboratories, Kissei Pharmaceutical Co., Ltd.,
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Taya Fumie
Central Research Laboratory Kissei Pharmaceutical
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Isaji M
The 2nd Research Center Kissei Pharmaceutical Co. Ltd.
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Kojima M
Tokyo Pharmaceutical Research Center Pharmaceutical Technology Research Laboratories Daiichi Pharmac
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Itoh Fumiaki
Central Research Laboratory Kissei Pharmaceutical
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Miyagi M
Kumamoto Inst. Technol. Kumamoto Jpn
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