κ-opioid

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.

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.

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

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.

Mianserin hydrochloride (Org GB 94) is a tetracyclic compound with antidepressant properties that blocks alpha-adrenergic, histamine H1, and certain serotonin receptors; it may cause drowsiness and hematological issues.

Progesterone (Pregn-4-ene-3,20-dione) is the major progestational steroid that is secreted primarily by the CORPUS LUTEUM and the PLACENTA. Progesterone acts on the UTERUS, the MAMMARY GLANDS and the BRAIN. It is required in EMBRYO IMPLANTATION; PREGNANCY maintenance, and the development of mammary tissue for MILK production.

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

Mirtazapine (6-Azamianserin) is a tetracyclic antidepressant with a somewhat unique mechanism of action. Mirtazapine therapy can be associated with transient asymptomatic elevations in serum aminotransferase levels and has been linked to rare instances of clinically apparent acute liver injury.

(-)-Menthol (Levomenthol) is a levo isomer of menthol, an organic compound made synthetically or obtained from peppermint or mint oils with flavoring and local anesthetic properties. When added to pharmaceuticals and foods, menthol functions as a fortifier for peppermint flavors. It also has a counterirritant effect on skin and mucous membranes, thereby producing a local analgesic or anesthetic effect.

Loperamide hydrochloride (ADL 2-1294) is a synthetic, piperidine derivative and opioid agonist with antidiarrheal activity.

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

ADL-5859 (ADL5859 Hydrochloride) is a selective δ-opioid receptor agonist ( Ki: 0.8 nM), selectivity against opioid receptor κ, μ, and little inhibition for the hERG channel.

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.

Dynorphin B (1-13) acetate acts as an agonist on opioid κ-receptor.

ICI 199,441 hydrochloride is a potent, selective agonist of κ-opioid receptor.

[DPro10] Dynorphin A (1-11)acetate,porcine is a highly potent κ-opioid receptor agonist with a Ki value of 0.13 nM. [DPro10] Dynorphin A (1-11), porcine is an n-alkylated derivative with analgesic activity.

Lumichrome is an endogenous compound in humans, produced by photodegradation of riboflavin. It utilizes a p53-dependent mechanism to inhibit growth and induce apoptosis in human lung cancer cells.

Porcine dynorphin A(1-13) acetate (Dynorphin A Porcine Fragment 1-13 acetate) is a potent, endogenous κ opioid receptor agonist and is antinociceptive at physiological concentrations. Exposure to dynorphin A (1-13) causes acute increases in [Ca2+]i in individual neurons similar to increases seen with acute NMDA treatment.

LY2795050 is a novel specific κ-Opioid Receptor antagonist (IC50: 0.72 nM).

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.

LY2444296 (FP3FBZ) is an orally active and selective antagonist of kappa opioid receptor(Ki = 1 nM).

Dynorphin A (1-10) acetate is an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) also blocks NMDA-activated current with an IC50 of 42.0 μM.

Porcine dynorphin A (1-13), a potent endogenous κ opioid receptor agonist, exhibits antinociceptive properties at physiological concentrations and induces acute increases in [Ca2+]i in neurons, akin to those observed with acute NMDA treatment.

Herkinorin is an opioid analgesic and an analogue of the natural product Salvinorin A. herkinorin is a μ-opioid agonist with more than 100x higher μ-opioid affinity and 50x lower κ-opioid affinity compared to Salvinorin A. Herkinorin is a semi-synthetic c