380620-88-2

380620-88-2 structure

Name: [(pF)Phe4]Nociceptin(1-13)NH2
Chemical Name: [(pF)Phe4]Nociceptin(1-13)NH2
CAS Number: 380620-88-2
Molecular Formula: C₆₁H₉₉FN₂₂O₁₅
Molecular Weight: 1471.54000
Catalog: Signaling Pathways GPCR/G Protein Opioid Receptor
Create Date: 2017-07-21 23:42:23
Modify Date: 2024-02-05 13:06:01
[(pF)Phe4]Nociceptin(1-13)NH2 is a highly potent and selective NOP (OP4) agonists, with a pKi of 10.68 and a pEC50 of 9.31. [(pF)Phe4]Nociceptin(1-13)NH2 displays high selectivity over δ, κ, and μ opioid receptors (>3000 fold)[1][2].

Name	[(pF)Phe4]Nociceptin(1-13)NH2
Synonyms	phe-gly-gly-pfluorophe-thr-gly-ala-arg-lys-ser-ala-arg-lys-nh2 m.w. 1399.60 c61h99fn22o15

Description	[(pF)Phe4]Nociceptin(1-13)NH2 is a highly potent and selective NOP (OP4) agonists, with a pKi of 10.68 and a pEC50 of 9.31. [(pF)Phe4]Nociceptin(1-13)NH2 displays high selectivity over δ, κ, and μ opioid receptors (>3000 fold)[1][2].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Opioid Receptor Signaling Pathways >> Neuronal Signaling >> Opioid Receptor Research Areas >> Neurological Disease
In Vivo	In unanaesthetised normotensive mice, bolus intravenous injection of 100 nmol/kg of [(pF)Phe4]Nociceptin(1-13)NH2 decreases mean blood pressure and heart rate; these effects are longer lasting than those elicited by the same dose of NC(1-13)NH2. I.c.v. administration of [(pF)Phe4]Nociceptin(1-13)NH2 dose-dependently stimulated feeding in rats, and is about tenfold more potent than NC(1-13)NH2[2].
References	[1]. Rizzi A, et al. Pharmacological characterisation of [(pX)Phe4]nociceptin(1-13)NH2 analogues. 2. In vivo studies. Naunyn Schmiedebergs Arch Pharmacol. 2002;365(6):450-456. [2]. Bigoni R, et al. Pharmacological characterisation of [(pX)Phe4]nociceptin(1-13)amide analogues. 1. In vitro studies. Naunyn Schmiedebergs Arch Pharmacol. 2002;365(6):442-449. [3]. Guerrini R, et al. Structure-activity studies of the Phe(4) residue of nociceptin(1-13)-NH(2): identification of highly potent agonists of the nociceptin/orphanin FQ receptor. J Med Chem. 2001;44(23):3956-3964.