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.

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).

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.

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.

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].