Ac-RYYRIK-NH2 TFA

发表于由

Ac-RYYRIK-NH2 TFA;

Ac-RYYRIK-NH2 TFA 是一种有效的 ORL1 部分激动剂，作为 ORL1 的内源性配体，在 CHO 细胞中 (Kd=1.5 nM)。Ac-RYYRIK-NH2 TFA 是 G 蛋白激活的特异性拮抗剂，竞争性拮抗 noc/OFQ 在大鼠脑膜和脑切面刺激 [35S]-GTPgS 结合 G 蛋白。

Ac-RYYRIK-NH2 TFAamp;;

Ac-RYYRIK-NH2 TFA Chemical Structure

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生物活性

Ac-RYYRIK-NH2 TFA is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain[1].

IC50 Target

Kd: 1.5 nM (ORL1 in CHO cells)[1]
体内研究
(In Vivo)

Ac-RYYRIK-NH2 TFA (intracerebroventricularly (i.c.v.)) inhibits spontaneous locomotor activity in mice with an ID50 of 0.07 nmol. Co-administration of noc/OFQ and Ac-RYYRIK-NH2 lead to additive effects in Male Swiss mice[1].

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

1053.13

Formula

C46H71F3N14O11
Sequence Shortening

Ac-RYYRIK-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]. H Berger, et al. Antagonism by acetyl-RYYRIK-NH2 of G protein activation in rat brain preparations and of chronotropic effect on rat cardiomyocytes evoked by nociceptin/orphanin FQ. Br J Pharmacol. 1999 Feb;126(3):555-8.

    [2]. H Berger, et al. The nociceptin/orphanin FQ receptor ligand acetyl-RYYRIK-amide exhibits antagonistic and agonistic properties.Peptides. 2000 Jul;21(7):1131-9.

    [3]. C T Dooley, et al. Binding and in vitro activities of peptides with high affinity for the nociceptin/orphanin FQ receptor, ORL1. J Pharmacol Exp Ther. 1997 Nov;283(2):735-41.