Ac-RYYRIK-NH2 TFA

Names

[ CAS No. ]:
200959-48-4

[ Name ]:
Ac-RYYRIK-NH2 TFA

[Synonym ]:
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

Biological Activity

[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.