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| | [(PF)PHE4]nociceptin(1-13)NH2 Basic information |
| | [(PF)PHE4]nociceptin(1-13)NH2 Chemical Properties |
| 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 |
| | [(PF)PHE4]nociceptin(1-13)NH2 Usage And Synthesis |
| 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 |
| | [(PF)PHE4]nociceptin(1-13)NH2 Preparation Products And Raw materials |
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