Opiate analgesia

Evidence for mediation by a subpopulation of opiate receptors

G. W. Pasternak, S. R. Childers, Solomon H Snyder

Research output: Contribution to journalArticle

Abstract

Naloxazone, a hydrazone derivative of the opiate antagonist naloxone, has a high affinity for opiate receptor binding sites. Naloxazone injections reduce opiate receptor binding to extensively washed mouse brain membranes for more than 24 hours, suggesting that the effect is irreversible. High-affinity binding sites are abolished by this treatment, whereas low-affinity sites are unaffected. Naloxazone treatment blocks the analgesic effects of morphine for at least 24 hours but does not prevent death from high doses of morphine. Thus analgesic but nonlethal opiate effects may be mediated by the high-affinity subpopulation of opiate receptors.

Original languageEnglish (US)
Pages (from-to)514-516
Number of pages3
JournalScience
Volume208
Issue number4443
StatePublished - 1980

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Opiate Alkaloids
Opioid Receptors
Analgesia
Morphine
Analgesics
Binding Sites
Hydrazones
Naloxone
Injections
Membranes
Brain
Therapeutics
naloxazone

ASJC Scopus subject areas

  • General

Cite this

Opiate analgesia : Evidence for mediation by a subpopulation of opiate receptors. / Pasternak, G. W.; Childers, S. R.; Snyder, Solomon H.

In: Science, Vol. 208, No. 4443, 1980, p. 514-516.

Research output: Contribution to journalArticle

Pasternak, GW, Childers, SR & Snyder, SH 1980, 'Opiate analgesia: Evidence for mediation by a subpopulation of opiate receptors', Science, vol. 208, no. 4443, pp. 514-516.
Pasternak, G. W. ; Childers, S. R. ; Snyder, Solomon H. / Opiate analgesia : Evidence for mediation by a subpopulation of opiate receptors. In: Science. 1980 ; Vol. 208, No. 4443. pp. 514-516.
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