Ac-RYYRWK-NH2 TFA

Names

[ Name ]:
Ac-RYYRWK-NH2 TFA

Biological Activity

[Description]:

Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP), [3H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a Kd of 0.071 nM, but has no affinity for µ-, κ- or δ-opioid receptors[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Opioid Receptor

Signaling Pathways >> Neuronal Signaling >> Opioid Receptor

Research Areas >> Neurological Disease

[In Vitro]

[3H]ac-RYYRWK-NH2 binding to rat cortical membranes revealed a single high affinity site for [3H]ac-RYYRWK-NH2 (Kd=0.071 nM)[1]. Naloxone benzoylhydrazone displaced [3H]acRYYRWK-NH2 binding to rat cortical membranes (Ki=104 nM) and human ORL1 (Ki=136 nM) as well as [125I]Tyr14-NC-OH to ORL1 (Ki=37 nM) has no affinity for µ-, κ- or δ-opioid receptors[1].

[References]

[1]. 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.

[2]. M Ho, et al, Characterization of the ORL(1) receptor on adrenergic nerves in the rat anococcygeus muscle. Br J Pharmacol. 2000 Sep;131(2):349-55.

Chemical & Physical Properties

[ Molecular Formula ]:
C₅₁H₇₀F₃N₁₅O₁₁

[ Molecular Weight ]:
1126.19

Related Compounds

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