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Antinociceptive studies of the optical isomers of N-allylnormetazocine (SKF 10,047)

1983; Elsevier BV; Volume: 91; Issue: 2-3 Linguagem: Inglês

10.1016/0014-2999(83)90476-4

1879-0712

Mario D. Aceto, Everette L. May,

Pain Mechanisms and Treatments

In the mouse tail-flick test, neither the racemate of N-allylnormetazocine (NANM) nor its optical isomers showed antinociceptive activity. However, all three antagonized morphine's tail-flick effects. In the phenylquinone test in mice, the racemate and (−)-isomer of NANM showed agonist activity and antagonized morphine-induced antinociception. The (+)-isomer was inactive. The opioid antagonist, naloxone was effective versus morphine alone in the tail-flick and versus morphine, and (±)- and (−)-NANM in the phenylquinone test. Yohimbine, the α2-receptor blocker, antagonized morphine in the tail-flick test. In the phenylquinone test, yohimbine was effective versus (±)- and (−)-NANM, but showed no activity versus morphine. The results suggest that morphine and NANM are acting at different sites. In addition, different α2-adrenoceptors appear to be involved. Some implications regarding the analgesic and psychotomimetic properties of NANM are discussed.