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Vol. 285, Issue 2, 518-526, May 1998
Departments of Pharmacology and Psychology, University of Michigan,
Ann Arbor, Michigan
Naltrexone (NTX) exhibited approximately 3-fold higher affinity for
sites labeled by [3H]U69,593 (putative
1-selective ligand) than [3H]bremazocine
(non-selective ligand) in the presence of mu and delta receptor blockade in monkey brain membranes. This
led us to test an hypothesis that NTX could display in
vivo antagonist selectivity for 1-
versus non-1-mediated effects. Six opioid agonists were characterized by NTX apparent pA2 analysis in
a 50°C water tail-withdrawal assay in rhesus monkeys. Constrained NTX
pA2 values (95% confidence limits) were: alfentanil, 8.66 (8.47-8.85); ethylketocyclazocine, 7.97 (7.93-8.01); U69,593, 7.64 (7.49-7.79); U50,488, 7.55 (7.42-7.67); bremazocine, 6.92 (6.73-7.12); enadoline, 6.87 (6.69-7.05). Pretreatment with
clocinnamox, an irreversible mu antagonist, confirmed
that mu receptors were not involved in the
antinociception produced by the kappa agonists, U69,593,
U50,488, bremazocine and enadoline; however, both mu and
kappa receptors mediated the antinociceptive effects of
ethylketocyclazocine. The apparent NTX pA2 profile of
opioid agonists correlated highly with the radioligand binding studies,
which indicates that U69,593 and U50,488 produced antinociception by
acting on kappa-1 receptors, whereas bremazocine and
enadoline probably acted via non-kappa-1 receptors. This study provides further functional evidence of kappa opioid receptor multiplicity in primates and
suggests that NTX may be a useful tool to study this phenomenon
in vivo.
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