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Synthesis and opioid activity of new fentanyl analogs.

机译：新型芬太尼类似物的合成及其阿片类药物活性。

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摘要

Three new fentanyl analogs (compounds 3-4-5) have been synthesized and evaluated for antinociceptive properties using the writhing test. The analgesic property of the active compound, N-[1-phenylpyrazol-3-yl]-N-[1-(2-phenethyl)-4-piperidyl)] propenamide (compound 4), was tested using the hot plate test in mice. Its opioid agonistic activity was characterized using three isolated tissues: guinea pig ileum, mouse vas deferens, and rabbit vas deferens. Compound 4 was as effective as fentanyl or morphine and it showed less antinociceptive potency than fentanyl but it was more potent than morphine. The duration of the antinociception was similar to that of fentanyl. This compound inhibited the electrically evoked contractions of myenteric plexus-longitudinal muscle strips of guinea pig ileum and of mouse vas deferens but not those of rabbit vas deferens. These effects could be reversed by micro selective antagonists (naloxone and/or CTOP) but not by the delta selective antagonist naltrindole, thus indicating that the compound acted as a micro opioid agonist. Finally, the binding data confirmed that compound 4 had high affinity and selectivity for the micro-receptor.
机译：合成了三种新的芬太尼类似物（化合物3-4-5），并使用扭体试验评估了其抗伤害感受性。活性化合物N- [1-苯基吡唑-3-基] -N- [1-（2-苯乙基）-4-哌啶基）]丙烯酰胺（化合物4）的镇痛特性通过热板试验在老鼠。其阿片样物质的激动活性用三种分离的组织来表征：豚鼠回肠，小鼠输精管和兔输精管。化合物4与芬太尼或吗啡一样有效，并且其抗伤害感受力比芬太尼低，但比吗啡更有效。抗伤害感受的持续时间与芬太尼相似。该化合物抑制豚鼠回肠和小鼠输精管的肌间神经丛-纵肌条的电诱发收缩，但不抑制兔输精管的电诱发收缩。这些作用可以被微选择拮抗剂（纳洛酮和/或CTOP）逆转，但不能被δ选择性拮抗剂纳曲酮逆转，因此表明该化合物起微阿片样物质激动剂的作用。最后，结合数据证实化合物4对微受体具有高亲和力和选择性。

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