Stereospecific effects of opiate antagonists on superficial and deep nociception and on motor activity suggest involvement of endorphins on different opioid receptors

It is known that various opiate antagonists enhance stereospecifically reactions to superficial nociceptive stimuli (e.g. in the hot plate test) suggesting the involvement of endogenous ligands in these reactions. In mice and rats the writhing responses to deep nociceptive stimuli (intraperitoneal test) were also enhanced stereospecifically by (-) naloxone, Mr 2266 and GPA 2163 but some other antagonists (naltrexone, levallorphan, diprenorphine) were inactive probably as a consequence of interfering agonist (antinociceptive) properties. An another antagonist, (-) Win 44441 suggested to bind principally with κ receptors did not enhance either superficial or deep nociception indicating that the former antagonists are probably interfering with endorphins at the level of μ receptors. The motor reaction of mice to a novel environment was stereospecifically depressed by opioid antagonists including (-) Win 44441 suggesting an involvement of endorphins at the level of κ receptors ; Mr 2266 and GPA 2163 were ineffective in this test and hyperalgesic in the two antinociceptive tests ; they might be relatively pure μ antagonists.