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.

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

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.

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.

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.

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

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.

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.

(-)-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.

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

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

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.

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.

ICI 204,448 is a potent κ-opioid agonist with potential analgesic activity for the study of neurological diseases.

[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.

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

JDTic is a powerful antagonist of kappa-opioid receptors (KOR), effectively inhibiting the antinociceptive effects induced by the κ-agonist U50, 488.

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

Alvimopan (LY 246736) is a synthetic trans-3, 4-dimethyl-4-(3-hydroxyphenyl) piperidine with peripherally selective opioid mu receptor antagonist activity. Alvimopan is a selective and competitive antagonist at mu-opioid receptors, found in myenteric and submucosal neurons and the immune cells of the lamina propria in the human gut. Upon administration, this agent binds to mu-opioid receptors in the gut, thereby reversing opioid-related disturbances in gut motility. Alvimopan is approximately three to nine times more potent than naloxone.

BTRX-335140 (CYM-53093) is a potent and selective orally active κ-opioid receptor (KOR) antagonist with antagonistic activity against κOR, μOR, and δOR with IC50 values of 0.8, 110, and 6500 nM, respectively.

DPI-3290 is a specific agonist of opioid receptors (Ki: 0.18 nM, 0.46 nM, and 0.62 nM for δ-, μ-, and κ-opioid receptors, respectively) with potent antinociceptive activity. DPI-3290 is one of a series of novel centrally acting agents.

Tonazocine, a non-peptide compound, primarily functions as a partial δ-opioid receptor agonist, with additional properties of a μ-receptor antagonist and weak κ-receptor agonist activity.

Norbuprenorphine, the primary active metabolite of buprenorphine, is a potent agonist of the μ, δ, and κ opioid receptors. It is the only known active metabolite of buprenorphine.

Norbuprenorphine HCl is a primary active metabolite of buprenorphine, serving as an effective agonist for the μ, δ, and κ opioid receptors.