TY - JOUR
T1 - Opiate analgesia
T2 - Evidence for mediation by a subpopulation of opiate receptors
AU - Pasternak, Gavril W.
AU - Childers, Stephen R.
AU - Snyder, Solomon H.
PY - 1980/1/1
Y1 - 1980/1/1
N2 - 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.
AB - 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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U2 - 10.1126/science.6245448
DO - 10.1126/science.6245448
M3 - Article
C2 - 6245448
AN - SCOPUS:0019307228
SN - 0036-8075
VL - 208
SP - 516
EP - 518
JO - Science
JF - Science
IS - 4443
ER -