Opioid Receptor

AT-121 is a dual μ-opioid and neuropeptide receptor partial agonist (Kis 16.49 and 3.67 nM, respectively). It stimulates [35S]GTPγS binding to cell membranes expressing either μ-opioid receptors or neuropeptide receptors (EC50s of 19.6 and 34.7 nM, respectively.) AT-121 (0.003-0.03 mg/kg) reduced capsaicin-induced thermal anisocoria in a dose-dependent manner, but did not increase scratching activity in rhesus monkeys. In rhesus monkey drug self-administration tests, AT-121 at doses of 0.3 to 10 μg/kg per injection lacked reinforcing effects (a potential marker of abuse) and did not reduce the reinforcing effects of food pellets.AT-121 (0.01 or 0.03 mg/kg) did not induce hyperalgesia, a marker of tolerance, in rhesus monkeys.AT-121 is a safe non-addictive pain reliever with anti-injury and analgesic effects.

ZT 52656A is a selective agonist of kappa opioid, and used for the prevention or alleviation of pain in the eye.

Apitegromab (SRK-015) is a new myostatin inhibitor, an antibody targeting myostatin precursor, which can be used to study neuromuscular diseases including spinal muscular atrophy.

Difelikefalin acetate (CR 845 acetate) is a peripherally restricted kappa opioid receptor agonist. CR845 exhibit low P450 CYP inhibition and low penetration into the brain.

Salvinorin A is a non-nitrogenous κ-opioid selective agonist.

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.

DuP 747 HCl is a selective kappa agonist with analgesic activity.DuP 747 consists of two conformations.

Norbinaltorphimine dihydrochloride is a selective and potent κ opioid receptor antagonist that induces itch-associated responses in mice.

CTAP(TFA) (103429-32-9 free base) is a potent, highly selective, and brain-penetrant antagonist of the μ-opioid receptor with IC50 of 3.5 nM. It displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP(TFA） (103429-32-9 free base) can be used for the study of L-DOPA-induced dyskinesia (LID)

Faxeladol, a potent adrenergic absorption inhibitor and serotonin reuptake inhibitor, is a small-molecule Opioid receptor agonist that can be used to study neurological disorders.

Amentoflavone (3',8''-Biapigenin), as a potent inhibitor of CYP3A4 and CYP2C9, can interact with many other medications. CYP3A4 and CYP2C9 are proteins used for drug metabolism in the body. Amentoflavone also is an inhibitor of human cathepsin B. It has antimalarial activity in trials significant affinities towards the Delta-1, kappa opioid receptors (as an antagonist) and binds to benzodiazepine receptors. Amentoflavone may be a potential lead for a new type of anti-inflammatory agents having the dual inhibitory activity of group II phospholipase A2 and cyclooxygenase. Amentoflavone and quercetin differentially exerted suppression of PGE2 biosynthesis via downregulation of COX-2/iNOS expression.

SNC 80 (NIH 10815) is a potent, highly selective and non-peptide δ-opioid receptor agonist, Ki = 1.78 nM, IC50 = 2.73 nM. SNC80 also selectively activates μ-δ heteromer in HEK293 cells with an EC50 of 52.8 nM. SNC80 shows antinociceptive, antihyperalgesic and antidepressant‐like effects. SNC80 has the potential for multiple headache disorders treatment.

DAMGO (DAGO) is an opioid receptor agonist with the ability to affect the locomotive activity in rodents. Possible analgesic agent due to μ-opiod receptor interaction.

[Leu5]-Enkephalin (Leu-enkephalin) is an endogenous neuropeptide involved in nociception and an agonist of δ-opioid and μ-opioid receptors (Kis = 4.0 and 3.4 nM, respectively)

Naloxegol oxalate (NKTR-118) is a peripherally-selective opioid antagonist for the treatment of opioid-induced constipation.

Progesterone is a steroid hormone that regulates the menstrual cycle and is essential for pregnancy. It is also commonly used to induce melasma models.

Samidorphan HCl is an orally active and highly potent modulator of the opioid system that binds to μ‐opioid, κ‐opioid, and delta-opioid receptors. Samidorphan HCl is a novel μ-opioid receptor antagonist, a partial agonist for k-opioid and delta-opioid receptors. Samidorphan HCl can be used to prevent and treat schizophrenia.

Matrine (Vegard), an alkaloid isolated from the Sophora genus, acts as a kappa opioid receptor agonist.

Harmane (Loturine) is a bio-active β-Carboline and monoamine oxidase inhibitor found in coffee and tobacco smoke.

GR103545 is a selective agonist of the κ-opioid receptor, which is a radiotracer that can be used as in vivo imaging.

ADL-5747 (ADL-5747 (free base)) (free base) is a delta opioid receptor agonist used in the treatment of neurological disorders, skin and musculoskeletal disorders, and may be used in the study of postherpetic neuralgia, knee osteoarthritis and pain.

Dynorphin A is an endogenous opioid peptide and a κ-opioid receptor (KOR) agonist, with some agonistic activity on μ- and δ-opioid receptors. It primarily functions as a neurotransmitter and regulator in the central and peripheral nervous systems, exerting analgesic and mood-regulating effects.

6'-GNTI dihydrochloride is a κ-opioid receptor (KOR) agonist that favors activation of G-protein-mediated signaling over recruitment of β-aspirin 2. 6'-GNTI dihydrochloride only activates the Akt pathway in striatal neurons.