[Arg14,Lys15]Nociceptin TFA

[Arg14,Lys15]Nociceptin TFA;

[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 TFAamp;;

[Arg14,Lys15]Nociceptin TFA Chemical Structure

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生物活性

[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[1].

体外研究
(In Vitro)

[Arg14,Lys15]Nociceptin TFA is about 30-fold more potent than Nociceptin (NC) and produces longer lasting effects[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

In in vivo experiments, [Arg14,Lys15]Nociceptin TFA mimics the effects of NC, producing, after intracerebroventricular administration, pronociceptive effects in the tail-withdrawal assay and inhibiting the locomotor activity of the mice[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

2023.18

Formula

C84H138F3N31O24

Sequence Shortening

FGGFTGARKSARKRKNQ

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

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.

    [2]. Rizzi D, Rizzi A, Bigoni R, et al. [Arg(14),Lys(15)]nociceptin, a highly potent agonist of the nociceptin/orphanin FQ receptor: in vitro and in vivo studies. J Pharmacol Exp Ther. 2002;300(1):57-63.