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[Arg14,Lys15] Nociceptin

Names

[ CAS No. ]:
236098-40-1

[ Name ]:
[Arg14,Lys15] Nociceptin

[Synonym ]:
phe-gly-gly-phe-thr-gly-ala-arg-lys-ser-ala-arg-lys-arg-lys-asn-gln

Biological Activity

[Description]:

[Arg14,Lys15]Nociceptin is a highly potent and selective NOP receptor agonist, with an EC50 of 1 nM. [Arg14,Lys15]Nociceptin displays high selectivity over opioid receptors, with IC50s of 0.32, 280, >10000 and 1500 nM for NOP (ORL1; OP4), μ, δ and κ receptors, respectively[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Opioid Receptor
Signaling Pathways >> Neuronal Signaling >> Opioid Receptor
Research Areas >> Neurological Disease

[In Vitro]

[Arg14,Lys15]Nociceptin is about 30-fold more potent than Nociceptin (NC) and produces longer lasting effects[2].

[In Vivo]

In in vivo experiments, [Arg14,Lys15]Nociceptin mimics the effects of NC, producing, after intracerebroventricular administration, pronociceptive effects in the tail-withdrawal assay and inhibiting the locomotor activity of the mice[2].

[References]

[1]. Okada K, Sujaku T, Chuman Y, et al. Highly potent nociceptin analog containing the Arg-Lys triple repeat. Biochem Biophys Res Commun. 2000;278(2):493-498.

[2]. Rizzi D, Rizzi A, Bigoni R, et al. [Arg(14),Lys(15)]nociceptin, a highly potent agonist of the nociceptin/orphanin FQ receptor: in vitro and in vivo studies. J Pharmacol Exp Ther. 2002;300(1):57-63.

Chemical & Physical Properties

[ Molecular Formula ]:
C82H137N31O22

[ Molecular Weight ]:
1909.16000

[ Exact Mass ]:
1908.06000

[ PSA ]:
919.32000

[ LogP ]:
1.29430

Safety Information

[ Safety Phrases ]:
22-24/25

[ WGK Germany ]:
3

Related Compounds