ID | 32199 |
JaLCDOI | |
FullText URL | |
Author |
Takayama, Haruhiko
Ogawa, Norio
Hirata, Hiroshi
Ota, Zensuke
|
Abstract | 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. |
Keywords | ?-blocker
opioid receptor
membrane stabilizing activity
sodium index
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Amo Type | Article
|
Publication Title |
Acta Medica Okayama
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Published Date | 1991-10
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Volume | volume45
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Issue | issue5
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Publisher | Okayama University Medical School
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Start Page | 295
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End Page | 299
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ISSN | 0386-300X
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NCID | AA00508441
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Content Type |
Journal Article
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language |
English
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File Version | publisher
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Refereed |
True
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PubMed ID | |
Web of Science KeyUT |