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Science 2 May 1980:
Vol. 208. no. 4443, pp. 514 - 516
DOI: 10.1126/science.6245448
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Articles

Science, Vol 208, Issue 4443, 514-516
Copyright © 1980 by American Association for the Advancement of Science

articles

Opiate analgesia: evidence for mediation by a subpopulation of opiate receptors

GW Pasternak, Childers SR, and SH Snyder

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.


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K. Chang, A Lillian, E Hazum, P Cuatrecasas, and J. Chang (1981)
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