[苯丙氨酸1脯氨酸（CH2-NH）甘氨酸2]-孤啡肽-（1-13）NH2，一种推测的孤啡肽受体拮抗剂，在大鼠脊髓中是一种强效且稳定的激动剂。

[Phe1psi(CH2-NH)Gly2]-nociceptin-(1-13)NH2, a proposed antagonist of the nociceptin receptor, is a potent and stable agonist in the rat spinal cord.

作者信息

Xu I S, Wiesenfeld-Hallin Z, Xu X J

机构信息

Department of Medical Laboratory Sciences and Technology, Huddinge University Hospital, Karolinska Institute, Sweden.

出版信息

Neurosci Lett. 1998 Jun 19;249(2-3):127-30. doi: 10.1016/s0304-3940(98)00411-x.

DOI:10.1016/s0304-3940(98)00411-x

PMID:9682833

Abstract

[Phe1psi(CH2-NH)Gly2]-nociceptin-(1-13)NH2 is an nociceptin analogue which has been shown to be a selective antagonist of the nociceptin receptor in peripheral tissues. We now report that intrathecal [Phe1psi(CH2-NH)Gly2]-nociceptin-(1-13)NH2 produced a dose-dependent depression of the nociceptive flexor reflex in rats, an effect that is similar to nociceptin. The duration of depression produced by [Phe1psi(CH2-NH)Gly2]-nociceptin-(1-13)NH2 was significantly more prolonged than by nociceptin. The reflex depressive effect of nociceptin was not blocked by [Phe1psi(CH2-NH)Gly2]-nociceptin-(1-13)NH2. The results indicated that the proposed nociceptin receptor antagonist [Phe1psi(CH2-NH)Gly2]-nociceptin-(1-13)NH2 is a potent agonist in rat spinal cord and more resistant to enzymatic degradation compared to nociceptin.

摘要

[苯丙氨酸1ψ(CH2-NH)甘氨酸2]-孤啡肽-(1-13)NH2是一种孤啡肽类似物，已被证明是外周组织中孤啡肽受体的选择性拮抗剂。我们现在报告，鞘内注射[苯丙氨酸1ψ(CH2-NH)甘氨酸2]-孤啡肽-(1-13)NH2可使大鼠伤害性屈肌反射产生剂量依赖性抑制，这一效应与孤啡肽相似。[苯丙氨酸1ψ(CH2-NH)甘氨酸2]-孤啡肽-(1-13)NH2产生的抑制持续时间比孤啡肽显著延长。孤啡肽的反射抑制作用未被[苯丙氨酸1ψ(CH2-NH)甘氨酸2]-孤啡肽-(1-13)NH2阻断。结果表明，所提出的孤啡肽受体拮抗剂[苯丙氨酸1ψ(CH2-NH)甘氨酸2]-孤啡肽-(1-13)NH2在大鼠脊髓中是一种强效激动剂，并且与孤啡肽相比更耐酶降解。