nociceptin

Bioactive metabolite of nociceptin, antagonist of nociceptin-induced hyperalgesia

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

[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].

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].

[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 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.

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.

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

[(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).

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

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.

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)

MT-7716 free base is a selective non-peptide agonist of nociceptin receptor (NOP). It is used for promising potential treatment drugs for alcohol abuse and relapse prevention.

Ro 64-6198 is a nonpeptide, high-affinity, and brain penetration N/OFQ receptor (NOP) agonist (EC50: 25.6 nM). Ro 64-6198 is at least 100 times more selective for the NOP receptor over the classic opioid receptors.

MCOPPB triHydrochloride (MCOPPB 3HCl) is a nociceptin receptor agonist.

BAN ORL 24 is a highly potent nociceptin/orphan FQ (N/OFQ) receptor (NOP) antagonist that can be used to study neurological diseases.

SCH-486757 is an agonist of nociceptin-1 (NOP1) and orphanin FQ peptide receptors and is used in the study of cough.

MT-7716 hydrochloride is a selective agonist of non-peptide nociceptin receptor (NOP)

LY2940094 (LY-2940094) decreases ethanol self-administration in animal models. LY2940094 is an effective, selective, and orally available nociceptin receptor antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM).

AT-090 is an innovative and highly selective agonist for nociceptin/orphanin FQ peptide receptors (NOP receptors).

NOP antagonist 1 (Compound (-)-31) is an antagonist of the nociceptin/orphanin FQ peptide receptor (NOP) with a Kb value of 8.65 nM. It is applicable in research related to neuropsychiatric disorders.

MCOPPB is a potent and selective agonist for the nociceptin receptor with a pKi of 10.07, much weaker activity at other opioid receptors. In animal studies, MCOPPB produces potent anxiolytic effects, with no inhibition of motor or memory function, and onl