nociceptin

Nociceptin (Orphanin FQ) is a 17-amino-acid polypeptide that is structurally related to the opioid peptide dynorphin A.

Nociceptin (1-7) acetate is a potent agonist of opioid receptor-like 1 (ORL1) receptor. Nociceptin (1-7) combines with nociceptin reduces hyperalgesia and has antinociceptive activity.

Nociceptin (1-13), amide is a potent agonist Opioid receptor-like1 (ORL1) receptor with a pEC50 of 7.9 for mouse vas deferens and a Ki of 0.75 nM for binding to rat forebrain membranes.

[(pF)Phe4]Nociceptin(1-13)NH2 acetate is a selective agonist of NOP receptor with a pKi of 10.68 and a pEC50 of 9.31. [(pF)Phe4]Nociceptin(1-13)NH2 acetate displays high selectivity over δ, κ, and μ opioid receptors (>3000 fold).

Potent agonist of the nociceptin (ORL1) receptor, demonstrated both in vitro and in vivo. Selective, competitive antagonism at the nociceptin receptor has also been reported (pA2 = 7.02 and 6.75 in the guinea pig ileum and mouse vas deferens respectively)

Selective and competitive nociceptin receptor antagonist, devoid of any agonist activity. Binds selectively to recombinant nociceptin receptors (pKi = 8.4), and competitively antagonizes the actions of nociceptin in vitro and in vivo.

Highly potent and selective nociceptin/orphanin FQ receptor (OP4) agonist peptide (pKi = 10.68; pEC50 = 9.80). Displays > 8000-fold selectivity over δ, κ, and μ opioid receptors and has relatively long lasting pronociceptive, hypotensive, negative inotrop

Bioactive metabolite of nociceptin, antagonist of nociceptin-induced hyperalgesia

[Nphe1]Nociceptin(1-13)NH2 is a novel endogenous ligand for the nociceptin/orphanin FQ (NC) receptor, acting as a selective and competitive antagonist without any agonist effects. It binds specifically to recombinant nociceptin receptors with high affinity (pKi=8.4) and effectively blocks nociceptin's ability to inhibit cyclic AMP accumulation in CHO cells (pA2=6.0), showcasing potential as an analgesic agent.

Nociceptin (1-13), amide TFA, a potent ORL1 receptor (opioid receptor-like 1 receptor, OP4) agonist, exhibits a pEC50 of 7.9 in mouse vas deferens and a Ki of 0.75 nM for rat forebrain membrane binding [1] [2].

Nociceptin (1-7) TFA, the N-terminal bioactive fragment of nociceptin, serves as a potent ORL 1 (NOP) receptor agonist, exhibiting antinociceptive properties. Its combination with nociceptin effectively reduces hyperalgesia in vivo [1].

[Arg14,Lys15]Nociceptin TFA is a potent and selective agonist for the NOP receptor (ORL1; OP4), with an EC50 of 1 nM. It shows significant selectivity against opioid receptors, with IC50 values of 0.32 nM for NOP, and 280, >10000, and 1500 nM for μ, δ, and κ receptors, respectively [1].

Highly potent and selective NOP receptor agonist (EC50 = 1 nM). Displays > 875-fold selectivity over opioid receptors (IC50 values are 0.32, 280, > 10000 and 1500 for NOP, μ, δ and κ receptors respectively). Longer lasting and 30-fold more potent than noc

Nociceptin (1-13), amide is a potent ORL1 (OP4) receptor agonist, exhibiting a pEC50 of 7.9 in mouse vas deferens and a Ki of 0.75 nM for rat forebrain membrane binding.

Ac-RYYRIK-NH2 acetate is an agonist at nociceptin/orphanin FQ(noc/OFQ) receptors, affecting spontaneous locomotor activity. Ac-RYYRIK-NH2 acetate is a partial agonist on ORL1 transfected in CHO cells, antagonizes the stimulation of [35S]-GTPgammaS binding to G proteins by noc/OFQ in membranes and sections of rat brain.

Ac-RYYRWK-NH2 acetate is a potent partial agonist of the nociceptin receptor(NOP), which is the endogenous ORL1 receptor agonist.

Orphanin FQ(1-11) acetate(178249-41-7 free base) is a peptide fragment containing amino acids 1-11 of Nociceptin. Orphanin FQ(1-11) acetate(178249-41-7 free base) is a potent agonist of the ORL1/KOR-3 receptor (Ki = 55 nM) and displays no affinity for opioid receptors, including μ, δ, κ1 and κ3 receptors (Ki >1000 nM). Orphanin FQ(1-11) acetate(178249-41-7 free base) displays analgesic properties in CD-1 mice.

UFP101 is a synthetic peptide that functions as an antagonist of the nociceptin receptor, demonstrating high affinity with a Ki of 0.06 nM in CHO cells expressing the human receptor. It exhibits selectivity for the nociceptin receptor over the κ-opioid receptor, with a Ki of 204 nM in CHO cells expressing the rat receptor. The compound effectively inhibits GTPγS release from the nociceptin receptor in CHO cell membranes, with an EC50 of 1.86 nM. When administered intracerebroventricularly at a dose of 10 nmol/animal, UFP101 prolongs the latency to tail withdrawal in the tail-flick test in mice, indicating its potential as an analgesic. Additionally, at doses of 0.003, 0.03, and 0.3 mg/kg, UFP101 enhances survival in a sepsis mouse model induced by cecal ligation and puncture, suggesting potential therapeutic applications in sepsis management.

Potent, selective and competitive silent antagonist for the NOP opioid receptor. Binds to NOP with high affinity (pKi = 10.24) and displays > 3000-fold selectivity over δ, μ and κ opioid receptors. Antinociceptive and opposes the action of nociceptin in v

endogenous peptide used to block nociceptin-induced allodynia and hyperalgesia

Nocistatin (human) TFA inhibits the allodynia and hyperalgesia induced by nociceptin and mitigates pain triggered by prostaglandin E2 [1].

Nocistatin, an endogenous neuropeptide, serves as a ligand for the orphan opioid receptor-like receptor and functionally antagonizes the neuropeptide nociceptin/orphanin FQ (Noc/OFQ). It inhibits 5-HT release through a G i/o protein-mediated pathway and blocks nociceptin-induced allodynia and hyperalgesia [1] [2].

Ac-RYYRWK-NH2 is a highly effective and specific partial agonist for the nociceptin receptor (NOP). It demonstrates a remarkable affinity for rat cortical membranes ORL1, with [3H]Ac-RYYRWK-NH2 exhibiting a Kd value of 0.071 nM. However, it shows negligible affinity towards μ-, κ-, or δ-opioid receptors.

High affinity ligand for the NOP site (Ki = 1.5 nM). Antagonizes nociceptin-stimulated GTP binding in rat brain and the chronotropic effect of nociceptin on rat cardiomyocytes. However, displays potent agonist properties in vivo, inhibiting locomotor acti

Ac-RYYRIK-NH2 TFA acts as both a potent partial agonist for ORL1 when transfected in CHO cells (K d = 1.5 nM) and an endogenous ligand of ORL1. Moreover, it serves as a specific antagonist that inhibits G protein activation and competitively blocks the stimulation of [35S]-GTPγS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in rat brain membranes and sections [1].

Orphanin FQ(1-11) TFA, a fragment of orphanin FQ or nociceptin (OFQ N), acts as a powerful NOP receptor (ORL-1; OP4) agonist with a K i of 55 nM. It lacks affinity for μ, δ, κ1, and κ3 receptors (K i >1000 nM), demonstrating specificity, and exhibits analgesic properties in CD-1 mice [1] [2].

Orphanin FQ(1-11) is a peptide fragment containing amino acids 1-11 of Nociceptin. Orphanin FQ(1-11) is a potent agonist of the ORL1/KOR-3 receptor (Ki = 55 nM) and displays no affinity for opioid receptors, including μ, δ, κ1 and κ3 receptors (Ki >1000 nM). Orphanin FQ(1-11) displays analgesic properties in CD-1 mice.

LIH383 is a peptide agonist specifically designed to activate the chemokine (C-X-C motif) receptor 7 (CXCR7), which functions both as a chemokine and an opioid peptide scavenger receptor. Demonstrating a high selectivity, LIH383 activates CXCR7 with an effective concentration (EC50) of 0.61 nM, showing significantly lower affinity towards μ-, δ-, and κ-opioid receptors, as well as the nociceptin opioid peptide (NOP) receptor, even at concentrations of 3 µM in β-arrestin recruitment assays. Furthermore, at a concentration of 3 µM, LIH383 effectively inhibits the uptake of opioid peptides by CXCR7, a process normally induced by dynorphin A, a non-selective opioid receptor agonist, in U87-ACKR3 cells.

Blocker of nociceptin-induced allodynia and hyperalgesia