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ID 14515
Eprint ID
14515
フルテキストURL
Thumnail 103_281.pdf 664 KB
タイトル(別表記)
Pharmacological specificity of antipsychotic, antiischemic and some other drugs for σ receptors labeled with [(3)H] haloperidol
著者
図子 義文 岡山大学医学部神経精神医学教室
抄録
Pharmacological specificity of several classes of drugs such as antipsychotics and antiischemic agents was assessed for σ receptors labeled with [(3)H] haloperidol. Specific binding of [(3)H] haloperidol in the presence of 25 nM spiperone was saturable and high affinity )Kd=1.96±1.31 nM, Bmax=2.37±0.27pmol/mg of protein;n=8). Among the 29 antipsychotics tested in inhibition studies, bromperidol and haloperidol were the most potent inhibitors (Ki=0.9nM, 1.0nM, respectively). The conventional antipsychotics moperone, timiperone etc. and the novel promising drugs YM-09151, Y-516, BMY-14802 and remoxipride potently inhibited [(3)H] haloperidol binding with the Ki in the range of low to moderate nanomolar. On the other hand, among the other 27 drugs tested, the antispasmodics eperisone and tolperisone, the antiischemic agents ifenprodil, the Ca(2+) antagonist flunarizine and cinnarizine, and the antitussives carbetapentane, cloperastine and dextromethorphan, were especially potent inhibitors. These results, taken together with the evidence that the antiischemic agents ifenprodil and dextromethorphan antagozine NMDA responses and NMDA receptor complex is a possible site of action for neuroprotective agents, strongly suggest that σ receptors may be potential sites of action for antiischemic as well as antipsychotic drugs, i.e., σ receptors mediate the neuroprotective effects of certain antiischemic agents by affecting the NMDA receptor complex.
キーワード
sigma receptors
antipsychotics
ifenprodil
dextromethorophan
eperisone
備考
原著
発行日
1991
出版物タイトル
岡山医学会雑誌
出版物タイトル(別表記)
Journal of Okayama Medical Association
103巻
4号
出版者
岡山医学会
出版者(別表記)
Okayama Medical Association
開始ページ
281
終了ページ
292
ISSN
0030-1558
NCID
AN00032489
資料タイプ
学術雑誌論文
オフィシャル URL
https://www.jstage.jst.go.jp/article/joma1947/103/4/103_4_281/_article/-char/ja/
関連URL
http://www.okayama-u.ac.jp/user/oma/
言語
Japanese
著作権者
岡山医学会
論文のバージョン
publisher
査読
有り
Eprints Journal Name
joma