ID | 32199 |
JaLCDOI | |
フルテキストURL | |
著者 |
Takayama, Haruhiko
Okayama University
Ogawa, Norio
Okayama University
Hirata, Hiroshi
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
|
出版物タイトル |
Acta Medica Okayama
|
発行日 | 1991-10
|
巻 | 45巻
|
号 | 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 |
英語
|
論文のバージョン | publisher
|
査読 |
有り
|
PubMed ID | |
Web of Science KeyUT |