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ID 32199
JaLCDOI
フルテキストURL
著者
Takayama, Haruhiko Okayama University
Ogawa, Norio Okayama University
Asanuma, Masato Okayama University
Hirata, Hiroshi Okayama University
Ogura, Toshio Okayama University
Ota, Zensuke Okayama University
抄録

To gain further insight into the central nervous system (CNS)-action of beta-adrenergic blocking agents (beta-blockers), we examined the effects of various kinds of beta-blockers on opioid receptors (Op-Rs) using radiolabeled receptor assay (RRA). We demonstrated that beta-blockers are competitively bound to Op-Rs in the CNS. Sodium index of beta-blockers in [3H]naloxone binding study indicated that beta-blockers had the mixed agonist-antagonist activity of opiates. The relative potency of beta-blockers in opioid RRA was negatively correlated with their membrane stabilizing activity. Neither beta-blocking activity nor intrinsic sympathomimetic activity was correlated with IC50 values of beta-blockers in opioid RRA. While it is widely accepted that beta-blockers have a tranquilizing activity, a part of the tranquilizing action of beta-blockers may be mediated through Op-Rs in the CNS. Although beta-blockers may have effects on their own receptors (beta-receptors) in the CNS, the more precise mechanisms of central action of these drugs must be further investigated.

キーワード
?-blocker
opioid receptor
membrane stabilizing activity
sodium index
Amo Type
Article
発行日
1991-10
出版物タイトル
Acta Medica Okayama
45巻
5号
出版者
Okayama University Medical School
開始ページ
295
終了ページ
299
ISSN
0386-300X
NCID
AA00508441
資料タイプ
学術雑誌論文
言語
English
論文のバージョン
publisher
査読
有り
PubMed ID
Web of Sience KeyUT