κ-opioid receptor

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.

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.

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.

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.

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.

BRL 52537 hydrochloride is a selective and specific KOR agonist which has been implicated in neuroprotection from ischemic neuronal injury[1]. It is used for research into potential treatments for stroke and heart attack as well as more general brain rese

GR 89696 fumarate is a highly selective κ2 opioid receptor agonist (IC50 = 0.04nM) with anti-pruritchy, anti-injury and neuroprotective effects.

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

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.

Asimadoline (EMD-61753) is a proprietary small molecule therapeutic, originally discovered by Merck KGaA of Darmstadt, Germany. Asimadoline was originally developed to treat peripheral pain such as arthritis. Asimadoline is an orally administered agent that acts as a kappa opioid receptor agonist. It has shown encouraging clinical efficacy for the treatment of IBS in a barostat study in IBS patients and has the potential for treating other gastrointestinal diseases.

Asimadoline hydrochloride (EMD-61753 hydrochloride) is a κ-opioid receptor agonist potentially for the treatment of pruritus. Asimadoline hydrochloride has also been shown to be used in the treatment of irritable bowel syndrome.

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.

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

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.

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.

Aticaprant (CERC-501) is a potent and centrally-penetrant antagonist of the kappa-opioid receptor (Ki: 0.807 nM).[2]

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

μ/κ/δopioid receptor agonist1 is an agonist for the μ opioid receptor (MOR), κ opioid receptor (KOR), and δ opioid receptor (DOR). It produces potent and long-lasting analgesic effects in the tail flick test through peripheral MOR and KOR activation.

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