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Vol. 292, Issue 2, 576-583, February 2000

Differential Antinociceptive Effects of Endomorphin-1 and Endomorphin-2 in the Mouse1

Leon F. Tseng, Minoru Narita, Chiaki Suganuma, Hirokazu Mizoguchi, Masahiro Ohsawa, Hiroshi Nagase and John P. Kampine

Department of Anesthesiology, Medical College of Wisconsin, Milwaukee, Wisconsin (L.F.T., M.N., C.S., H.M., J.P.K.); and Basic Research Laboratories, Toray Industries Inc., Kamakura, Japan (H.N.).

Two highly selective µ-opioid receptor agonists, endomorphin-1 and endomorphin-2, have been identified and postulated to be endogenous µ-opioid receptor ligands. We determined the antinociceptive effects of these two ligands at the supraspinal level in mice with the tail-flick and hot-plate responses. The i.c.v. injection of endomorphin-1 and -2 inhibited the tail-flick and hot-plate responses in a dose-dependent manner. The endomorphin-1 was found to be 3.3- and 2.4-fold more potent than endomorphin-2 in inhibiting the tail-flick and hot-plate responses, respectively. The antinociception induced by endomorphin-1 was blocked by i.c.v. pretreatment with the µ-opioid receptor antagonist beta -funaltrexamine but not by the kappa -opioid receptor antagonist nor-binaltorphimine, the delta 1-opioid antagonist 7-benzylidene naltrexamine, or the delta 2-opioid receptor antagonist naltriben. In contrast, the antinociception induced by endomorphin-2 was blocked by i.c.v. pretreatment with beta -funaltrexamine or nor-binaltorphimine but not by 7-benzylidene naltrexamine or naltriben. The inhibition of the tail-flick response induced by endomorphin-2 was blocked by pretreatment with an antiserum against dynorphin A(1-17) but not by antisera against Met-enkephalin, Leu-enkephalin, or beta -endorphin. None of these antisera reduced the endomorphin-1-induced tail-flick inhibition. We propose that endomorphin-1 produces antinociception by stimulating one type of µ-opioid receptor, whereas endomorphin-2 initially stimulates different µ-opioid receptors, which subsequently induce the release of dynorphins that act on kappa -opioid receptors to produce antinociception.

1 This work was supported in part by Grant DA03811 from the National Institutes of Health, National Institute on Drug Abuse (PI: L.F.T.). A preliminary report of some of the results was presented at the 28th Annual Meeting of the Society for Neuroscience, Los Angeles, CA, November 7-12, 1998 (Tseng et al., 1998).

0022-3565/00/2922-0576$03.00/0
THE JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
Copyright © 2000 by The American Society for Pharmacology and Experimental Therapeutics


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