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首页> 外文期刊>CNS drug reviews >RB101-mediated protection of endogenous opioids: potential therapeutic utility?
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RB101-mediated protection of endogenous opioids: potential therapeutic utility?

机译：RB101介导的内源性阿片样物质的保护：潜在的治疗用途？

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摘要

The endogenous opioids met- and leu-enkephalin are inactivated by peptidases preventing the activation of opioid receptors. Inhibition of enkephalin-degrading enzymes increases endogenous enkephalin levels and stimulates robust behavioral effects. RB101, an inhibitor of enkephalin-degrading enzymes, produces antinociceptive, antidepressant, and anxiolytic effects in rodents, without typical opioid-related negative side effects. Although enkephalins are not selective endogenous ligands, RB101 induces these behaviors through receptor-selective activity. The antinociceptive effects of RB101 are produced through either the mu-opioid receptor alone or through activation of both mu- and delta-opioid receptors; the antidepressant-like and anxiolytic effects of RB101 are mediated only through the delta-opioid receptor. Although little is known about the effects of RB101 on other physiologically and behaviorally relevant peptides, these findings suggest that RB101 and other inhibitors of enkephalin-degrading enzymes may have potential as novel therapeutic compounds for the treatment of pain, depression, and anxiety.
机译：内源性阿片类药物甲氨蝶呤和亮氨酸脑啡肽被肽酶灭活，阻止了阿片受体的活化。抑制脑啡肽降解酶会增加内源性脑啡肽水平，并刺激强大的行为效果。 RB101是脑啡肽降解酶的抑制剂，可在啮齿动物中产生镇痛，抗抑郁和抗焦虑作用，而没有典型的与阿片类药物相关的负面副作用。尽管脑啡肽不是选择性的内源性配体，但RB101通过受体选择性活性诱导这些行为。 RB101的抗伤害作用是通过单独的阿片受体或通过激活阿片和阿片受体共同产生的。 RB101的抗抑郁药和抗焦虑药仅通过δ阿片受体介导。尽管对RB101对其他生理和行为相关肽的作用了解甚少，但这些发现表明RB101和其他脑啡肽降解酶抑制剂可能具有作为治疗疼痛，抑郁和焦虑症的新型治疗化合物的潜力。

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