| Identification | Back Directory | [Name]
[(PF)PHE4]NOCICEPTIN(1-13)NH2 | [CAS]
380620-88-2 | [Synonyms]
M.W. 1399.60 C61H99FN22O15
[(PF)PHE4]NOCICEPTIN(1-13)NH2
PHE-GLY-GLY-PFLUOROPHE-THR-GLY-ALA-ARG-LYS-SER-ALA-ARG-LYS-NH2
L-Lysinamide, L-phenylalanylglycylglycyl-4-fluoro-L-phenylalanyl-L-threonylglycyl-L-alanyl-L-arginyl-L-lysyl-L-seryl-L-alanyl-L-arginyl- (9CI) | [Molecular Formula]
C61H99FN22O15 | [MDL Number]
MFCD03791318 | [MOL File]
380620-88-2.mol | [Molecular Weight]
1399.58 |
| Chemical Properties | Back Directory | [density ]
1.47±0.1 g/cm3(Predicted) | [storage temp. ]
Desiccate at -20°C | [form ]
Powder | [pka]
12.91±0.46(Predicted) | [Water Solubility ]
Soluble to 2 mg/ml in water | [Sequence]
H-Phe-Gly-Gly-Phe(4-F)-Thr-Gly-Ala-Arg-Lys-Ser-Ala-Arg-Lys-NH2 |
| Hazard Information | Back Directory | [Uses]
[(pF)Phe4]Nociceptin(1-13)NH2 is a highly potent and selective NOP receptor (OP4) agonist, 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]. | [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. DOI:10.1007/s00210-002-0549-7
[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. DOI:10.1007/s00210-002-0548-8
[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. DOI:10.1021/jm010221v |
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