Aceto M D, May E L
Eur J Pharmacol. 1983 Jul 22;91(2-3):267-72. doi: 10.1016/0014-2999(83)90476-4.
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 alpha 2-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 alpha 2-adrenoceptors appear to be involved. Some implications regarding the analgesic and psychotomimetic properties of NANM are discussed.
在小鼠甩尾试验中，N - 烯丙基去甲左啡诺（NANM）的消旋体及其光学异构体均未表现出抗伤害感受活性。然而，这三种物质均能拮抗吗啡的甩尾效应。在小鼠苯醌试验中，NANM的消旋体和（-）-异构体表现出激动剂活性，并拮抗吗啡诱导的抗伤害感受。（+）-异构体无活性。阿片类拮抗剂纳洛酮在甩尾试验中对单独使用的吗啡有效，在苯醌试验中对吗啡、（±）-和（-）-NANM有效。α2 - 受体阻滞剂育亨宾在甩尾试验中拮抗吗啡。在苯醌试验中，育亨宾对（±）-和（-）-NANM有效，但对吗啡无活性。结果表明，吗啡和NANM作用于不同位点。此外，似乎涉及不同的α2 - 肾上腺素能受体。文中讨论了有关NANM的镇痛和拟精神病特性的一些影响。
