200959-48-4

200959-48-4 structure

Name: Ac-RYYRIK-NH2 TFA
Chemical Name: Ac-RYYRIK-NH2
CAS Number: 200959-48-4
Molecular Formula: C₄₄H₇₀N₁₄O₉
Molecular Weight: 939.115
Catalog: Signaling Pathways GPCR/G Protein Opioid Receptor
Create Date: 2019-02-17 11:41:10
Modify Date: 2024-01-03 13:20:30
Ac-RYYRIK-NH2 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].

Name	Ac-RYYRIK-NH2
Synonyms	L-Lysinamide, N-acetyl-N-(diaminomethylene)-L-ornithyl-L-tyrosyl-L-tyrosyl-N-(diaminomethylene)-L-ornithyl-L-isoleucyl- N-acetyl-N-(diaminomethylidene)-L-ornithyl-L-tyrosyl-L-tyrosyl-N-(diaminomethylidene)-L-ornithyl-L-isoleucyl-L-lysinamide Ac-RYYRIK amide AC-ARG-TYR-TYR-ARG-ILE-LYS-NH2 N-Acetyl-N-(diaminomethylene)-L-ornithyl-L-tyrosyl-L-tyrosyl-N-(diaminomethylene)-L-ornithyl-L-isoleucyl-L-lysinamide ACETYL-RYYRIK,AMIDE

Description	Ac-RYYRIK-NH2 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].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Opioid Receptor Signaling Pathways >> Neuronal Signaling >> Opioid Receptor Research Areas >> Neurological Disease
Target	Kd: 1.5 nM (ORL1 transfected in CHO cells)[1]
In Vivo	Ac-RYYRIK-NH2 (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].
References	[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.