ANTI-NOCICEPTIVE STUDIES OF THE OPTICAL ISOMERS OF N-ALLYLNORMETAZOCINE (SKF 10,047)
ANTI-NOCICEPTIVE STUDIES OF THE OPTICAL ISOMERS OF N-ALLYLNORMETAZOCINE (SKF 10,047)
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DOI：
10.1016/0014-2999(83)90476-4
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发表时间：
1983-01-01
影响因子：
5
通讯作者：
MAY, EL
中科院分区：
文献类型：
--
作者：
ACETO, MD;MAY, EL
在小鼠甩尾试验中，N-烯丙基去甲甲唑辛（NANM）的消旋体及其光学异构体均未显示出抗伤害活性。3种药物均能拮抗吗啡的甩尾效应。在小鼠苯醌实验中，NANM的外消旋体和（-）异构体表现出激动剂活性，并拮抗吗啡诱导的抗伤害作用。（+）-异构体无活性。阿片样物质拮抗剂纳洛酮在甩尾中与单独的吗啡相比是有效的，并且与吗啡相比是有效的，并且（±）-和（-）-NANM在苯醌试验中。育亨宾，α 2-受体阻断剂，在甩尾试验中拮抗吗啡。在苯基醌试验中，育亨宾对（. ±.）-和（-）-NANM，但对吗啡没有显示活性。吗啡和NANM显然作用于不同的部位。不同的α 2-肾上腺素受体似乎参与其中。关于NANM的镇痛和拟精神病性质的一些影响进行了讨论。
In the mouse tail-flick test, neither the racemate of N-allylnormetazocine (NANM) nor its optical isomers showed antinociceptive activity. All 3 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 vs. morphine alone in the tail-flick and vs. 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 vs. (.+-.)- and (-)-NANM, but showed no activity vs. morphine. Morphine and NANM are apparently acting at different sites. Different .alpha.2-adrenoceptors appear to be involved. Some implications regarding the analgesic and psychotomimetic properties of NANM are discussed.