[Nphe1]Nociceptin(1-13)NH2 (TFA)

[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2?binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent[1].

OC(C(F)(F)F)=O.NCCCC[C@@H](C(N)=O)NC([C@H](CCCNC(N)=N)NC([C@H](C)NC([C@H](CO)NC([C@H](CCCCN)NC([C@H](CCCNC(N)=N)NC([C@H](C)NC(CNC([C@H]([C@H](O)C)NC([C@@H](NC(CNC(CNC(CNCC1=CC=CC=C1)=O)=O)=O)CC2=CC=CC=C2)=O)=O)=O)=O)=O)=O)=O)=O)=O

[1]Y Hashimoto, et al. Antagonistic effects of [Nphe1]nociceptin(1-13)NH2 on nociceptin receptor mediated inhibition of cAMP formation in Chinese hamster ovary cells stably expressing the recombinant human nociceptin receptor|[2]G Calo', et al. Characterization of [Nphe(1)]nociceptin(1-13)NH(2), a new selective nociceptin receptor antagonist. Br J Pharmacol. 2000 Mar;129(6):1183-93.