NOP Receptor/ORL1 Agonist

MCOPPB trihydrochloride is a NOP/ORL1 G protein-coupled receptor agonist and autophagy inhibitor that can cross the blood-brain barrier. MCOPPB trihydrochloride clears senescent cells, regulates locomotion, lipid storage and immune responses, and inhibits fibrosis and angiogenesis. MCOPPB trihydrochloride blocks autophagic flux, induces changes in locomotion and lipid storage, and activates the stress-responsive immune transcription network, thereby improving post-infarction cardiac function and exerting anxiolytic effects. MCOPPB trihydrochloride can be applied to research fields such as aging-related diseases and ischemic heart failure.

BPR1M492 is a brain-penetrant μ-opioid receptor (MOR) agonist an in vitro EC₅₀ of 0.93 nM in the cAMP inhibition assay and 0.004 nM in the FLIPR Ca²⁺ assay without a clear signaling bias between cAMP and β-arrestin-2 pathway. BPR1M492 is a cAMP-biased nociceptin-orphanin FQ opioid peptide agonist. BPR1M492 is a weak cAMP-biased δ/κ-opioid receptor agonist. BPR1M492 demonstrates potent in vivo antinociception and can be used for pain research.

Ro 64-6198 is a potent, selective, nonpeptide, high-affinity, high cellular permeability and brain penetration N/OFQ receptor (NOP) agonist with an EC₅₀ value of 25.6 nM. Ro 64-6198 is at least 100 times more selective for the NOP receptor over the classic opioid receptors. Ro 64-6198 can be used for stress and anxiety, addiction, neuropathic pain, cough, and anorexia.

Nociceptin (1-13), amide TFA is a potent ORL1 receptor (opioid receptor-like 1 receptor, OP4) agonist with a pEC₅₀ of 7.9 for mouse vas deferens and a K_i of 0.75 nM for binding to rat forebrain membranes.

MT-7716 hydrochloride (W-212393 hydrochloride) is a selective non-peptide nociceptin receptor (NOP) agonist and promising potential treatment drug for alcohol abuse and relapse prevention.

Lexanopadol (GRT-6006) is a μ-opioid receptor and nociceptor receptor (ORL-1 receptor) agonist. Lexanopadol can be used to study pain.

Nociceptin (1-13)，amide is a potent ORL1 receptor (opioid receptor-like 1 receptor，OP4) agonist with a pEC₅₀ of 7.9 for mouse vas deferens and a K_i of 0.75 nM for binding to rat forebrain membranes.

[(pF)Phe4]Nociceptin(1-13)NH2 TFA is a highly potent and selective NOP receptor (OP4) agonist, with a pK_i of 10.68 and a pEC₅₀ of 9.31. [(pF)Phe4]Nociceptin(1-13)NH2 TFA displays high selectivity over δ, κ, and μ opioid receptors (>3000 fold).

MT-7716 free base (W-212393) is a selective non-peptide nociceptin receptor (NOP) agonist and promising potential treatment drug for alcohol abuse and relapse prevention.

Nociceptin (1-7) is the N-terminal bioactive fragment of nociceptin (HY-P0183). Nociceptin (1-7) is a potent ORL₁ (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) combines with nociceptin reduces hyperalgesia in vivo.

ZP 120C is a potent and partial ORL1 receptor agonist. ZP 120C inhibits electrically induced contraction. ZP 120C can be used in the research of hyponatremia/hypokalemia.

Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP), [³H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a K_d of 0.071 nM, but has no affinity for μ-, κ- or δ-opioid receptors.

Nociceptin (1-7) TFA is the N-terminal bioactive fragment of nociceptin (HY-P0183). Nociceptin (1-7) TFA is a potent ORL₁ (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) TFA combines with nociceptin reduces hyperalgesia in vivo.

MOR agonist-5 is a selective and potent mu-opioid receptor (MOR) agonist with an EC₅₀ of 0.25 nM. MOR agonist-5 shows an EC₅₀ of 10 nM for DOR and >10000 nM for KOR and NOR. MOR agonist-5 exerts significant antinociceptive activity. MOR agonist-5 can be used for the research of pain.