[(pF)Phe4]Nociceptin(1-13)NH2

发表于由

[(pF)Phe4]Nociceptin(1-13)NH2;

[(pF)Phe4]Nociceptin(1-13)NH2 是一种高效、选择性的 NOP 受体 (OP4) 激动剂，pKi 为 10.68，pEC50 为 9.31。[(pF)Phe4]Nociceptin(1-13)NH2 对 δ、κ 和 μ 阿片受体具有较高的选择性 (>3000 倍)。

[(pF)Phe4]Nociceptin(1-13)NH2amp;;

[(pF)Phe4]Nociceptin(1-13)NH2 Chemical Structure

CAS No. : 380620-88-2

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生物活性

[(pF)Phe4]Nociceptin(1-13)NH2 is a highly potent and selective NOP receptor (OP4) agonist, with a pKi of 10.68 and a pEC50 of 9.31. [(pF)Phe4]Nociceptin(1-13)NH2 displays high selectivity over δ, κ, and μ opioid receptors (>3000 fold)[1][2].

体内研究
(In Vivo)

In unanaesthetised normotensive mice, bolus intravenous injection of 100 nmol/kg of [(pF)Phe4]Nociceptin(1-13)NH2 decreases mean blood pressure and heart rate; these effects are longer lasting than those elicited by the same dose of NC(1-13)NH2. I.c.v. administration of [(pF)Phe4]Nociceptin(1-13)NH2 dose-dependently stimulated feeding in rats, and is about tenfold more potent than NC(1-13)NH2[2].

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

1399.58

Formula

C61H99FN22O15
CAS 号

380620-88-2
Sequence Shortening

FGG{Phe(4-F)}TGARKSARK-NH2
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]. Rizzi A, et al. Pharmacological characterisation of [(pX)Phe4]nociceptin(1-13)NH2 analogues. 2. In vivo studies. Naunyn Schmiedebergs Arch Pharmacol. 2002;365(6):450-456.

    [2]. Bigoni R, et al. Pharmacological characterisation of [(pX)Phe4]nociceptin(1-13)amide analogues. 1. In vitro studies. Naunyn Schmiedebergs Arch Pharmacol. 2002;365(6):442-449.

    [3]. Guerrini R, et al. Structure-activity studies of the Phe(4) residue of nociceptin(1-13)-NH(2): identification of highly potent agonists of the nociceptin/orphanin FQ receptor. J Med Chem. 2001;44(23):3956-3964.