nop receptor

Cebranopadol (GRT6005) is an analgesic NOP and opioid receptor agonist with Kis of 0.9 nM, 0.7 nM, 2.6 nM, 18 nM for human NOP, μ-opioid (MOP), κ-opioid (KOP) and δ-opioid (DOP) receptor, respectively.

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

Cerivastatin sodium (BAY W 6228 sodium) is an orally active and highly potent HMG-CoA reductase inhibitor with lipid-lowering activity that can reduce low-density lipoprotein cholesterol levels. Cerivastatin sodium has anticancer effects and can be used to study primary hyperlipidemia.

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

BPR1M97 is a mu opioid receptor (MOP) and neuropeptide-orphin FQ (NOP) receptor agonist with blood-brain barrier permeability and potency, with Kis values of 1.8 nM for MOP and 4.2 nM for NOP.BPR1M97 exhibits anti-injurious effects and antinociceptive effects.

SCH 221510 is an orally available, selective and potent NOP agonist with an EC50 of 12 nM and a Ki of 0.3 nM.SCH 221510 has anxiolytic activity and can be used to study neurological disorders.

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).

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.

NNC 63-0532 is a potentnociceptin receptor agonist, Ki=7.3 nM, EC50=305 nM.

NOP receptor antagonist

nociceptin orphanin FQ (NOP) receptor antagonist

SR14150 is a partial agonist of high-affinity NOP 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.

J-113397 is a potent and selective NOP receptor antagonist (IC50 = 2.3 nM).

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

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.

MT-7716 HCl hydrate is a NOP receptor agonist.

UFP-101 TFA is a potent, selective, and competitive N OFQ peptide (NOP) receptor antagonist with a pKi value of 10.24, showing over 3000-fold selectivity against δ, μ, and κ opioid receptors, and exhibits antidepressant-like effects [1] [2].

[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 (1-7) 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].