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[Phe1psi(CH2-NH)Gly2]nociceptin-(1-13)-NH2 is an agonist of the nociceptin (ORL1) receptor.

作者信息

Butour J L, Moisand C, Mollereau C, Meunier J C

机构信息

Unité de Neuropharmacologie Moléculaire, Institut de Pharmacologie et de Biologie Structurale, C.N.R.S. UPR 9062, Toulouse, France.

出版信息

Eur J Pharmacol. 1998 May 15;349(1):R5-6. doi: 10.1016/s0014-2999(98)00273-8.

DOI:10.1016/s0014-2999(98)00273-8
PMID:9669489
Abstract

[Phe1psi(CH2-NH)Gly2]nociceptin-(1-13)-NH2, a pseudopeptide analog of nociceptin, has been shown to be a selective 'antagonist' of the nociceptin receptor in the isolated guinea pig ileum and mouse vas deferens preparations (Guerrini et al., 1998. Br. J. Pharmacol. 123, 163-165). However, in recombinant chinese hamster ovary cells expressing the human nociceptin receptor, we find that the pseudopeptide is a potent (IC50 = 7.5 nM) and fully efficacious inhibitor of forskolin-induced accumulation of cAMP, thus behaving as a pure 'agonist' rather than an antagonist of the receptor. The contrary behaviour of the pseudopeptide in smooth muscle and transformed cells may suggest that different nociceptin receptor types are being addressed in the two systems.

摘要

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1
[Phe1psi(CH2-NH)Gly2]nociceptin-(1-13)-NH2 is an agonist of the nociceptin (ORL1) receptor.
Eur J Pharmacol. 1998 May 15;349(1):R5-6. doi: 10.1016/s0014-2999(98)00273-8.
2
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4
[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.[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。
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[Phe1phi(CH2-NH)Gly2]nociceptin-(1-13)-NH2 acts as a partial agonist at ORL1 receptor endogenously expressed in mouse N1E-115 neuroblastoma cells.
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In vitro characterization of Ac-RYYRWK-NH(2), Ac-RYYRIK-NH(2) and [Phe1Psi(CH(2)-NH)Gly2] nociceptin(1-13)NH(2) at rat native and recombinant ORL(1) receptors.大鼠天然和重组的阿片受体（ORL(1)）上Ac-RYYRWK-NH(2)、Ac-RYYRIK-NH(2)及[Phe1Psi(CH(2)-NH)Gly2] 孤啡肽(1-13)NH(2)的体外特性研究
Neuropeptides. 2001 Oct-Dec;35(5-6):244-56. doi: 10.1054/npep.2001.0882.
7
Antagonistic effects of [Nphe1]nociceptin(1-13)NH2 on nociceptin receptor mediated inhibition of cAMP formation in Chinese hamster ovary cells stably expressing the recombinant human nociceptin receptor.[Nphe1] 孤啡肽（1-13）NH2 对稳定表达重组人孤啡肽受体的中国仓鼠卵巢细胞中孤啡肽受体介导的 cAMP 生成抑制作用的拮抗效应
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8
Evidence that [Phe1 psi(CH2-NH)Gly2]nociceptin-(1-13)-NH2, a peripheral ORL-1 receptor antagonist, acts as an agonist in the rat spinal cord.[苯丙氨酸1 ψ(CH2-NH)甘氨酸2]孤啡肽-(1 - 13)-NH2作为一种外周ORL - 1受体拮抗剂，在大鼠脊髓中起激动剂作用的证据。
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[Phe1psi(CH2-NH)Gly2]nociceptin-(1-13)-NH2 acts as an agonist of the orphanin FQ/nociceptin receptor in vivo.[苯丙氨酸1ψ(CH2 - NH)甘氨酸2]孤啡肽-(1 - 13)-NH2在体内作为孤啡肽/痛敏肽受体的激动剂。
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