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背景说明：[Arg14,Lys15]Nociceptin TFA 是一种高效、选择性的 NOP (ORL1; OP4) 受体激动剂，EC50为 1 nM。[Arg14,Lys15]Nociceptin TFA 对阿片受体具有较高的选择性，对 NOP、μ、δ 和 κ 受体的 IC50 值分别为 0.32、280、>10000 和 1500 nM。 [Arg14,Lys15]Nociceptin TFA is a highly potent and selective NOP receptor (ORL1; OP4) agonist, with an EC50 of 1 nM. [Arg14,Lys15]Nociceptin TFA displays high selectivity over opioid receptors, with IC50s of 0.32, 280, >10000 and 1500 nM for NOP, μ, δ and κ receptors, respectively.
In Vivo：In in vivo experiments, [Arg14,Lys15]Nociceptin mimics the effects of NC, producing, after intracerebroventricular administration, pronociceptive effects in the tail-withdrawal assay and inhibiting the locomotor activity of the mice.
In Vitro：[Arg14,Lys15]Nociceptin is about 30-fold more potent than Nociceptin (NC) and produces longer lasting effects.
参考文献：[1] Okada K, Sujaku T, Chuman Y, et al. Highly potent nociceptin analog containing the Arg-Lys triple repeat. Biochem Biophys Res Commun. 2000;278(2):493-498.
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