nociceptin receptor

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

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

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.

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).

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.

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

(±)-J-113397 is a potent and selective non-peptidyl ORL1 receptor antagonist (K(i): cloned human ORL1=1.8 nM). J-113397 inhibited nociceptin orphanin FQ-stimulated GTPγS binding to CHO cells expressing ORL1 with an IC50 value of 5.3 nM. J-113397 can be used for researching the physiological roles of nociceptin orphanin FQ [1].

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 (NOP) receptor antagonist

SR8993 is a highly selective, brain-penetrant agonist of the nociceptin receptor.

AT-076 is a noncompetitive antagonist of the κ-opioid receptor (Ki = 1.14 nM) and nociceptin receptor (Ki = 1.75 nM) and a competitive antagonist of the μ-opioid receptor (Ki = 1.67 nM) and δ-opioid receptor (Ki = 19.6 nM).

BU08028 is a mu opioid peptide (MOP) receptor and nociceptin-orphanin FQ peptide (NOP) receptor agonist.

LY-2940094, a nociceptin receptor antagonist, is used potentially for the treatment of major depressive disorder and alcoholism.

SB-612111 is a novel and potent human opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki = 0.33 nM). It exhibits selectivity for μ-, κ-, and δ-receptors with Ki values of 57.6 nM, 160.5 nM, and 2109 nM, respectively. SB-612111 effectively antagonizes the pronociceptive action of Nociceptin in an acute pain model[1].

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.

SB-612111 hydrochloride is a potent, novel orphan receptor for opioid receptors (ORL-1) antagonist with high affinity for hORL-1 and a Ki value of 0.33 nM. SB-612111 hydrochloride is able to act on mu-receptor (Ki: 57.6 nM), κ SB-612111 hydrochloride effectively antagonized the nociceptive effects of Nociceptin in an acute pain model.

[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].

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].

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.

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].

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.