kappa opioid receptor

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

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

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

Dup 747 is an analgesic that binds with high affinity and selectivity to the kappa-opioid receptor.

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

22-Thiocyanatosalvinorin A (RB-64) is a potent selective agonist for the kappa-opioid receptor, exhibiting an EC50 value of 0.077 nM.

5′-Guanidinonaltrindole (GNTI) is a selective antagonist of the kappa opioid receptor.

KOR agonist 4 (compound 39) is an agonist targeting the κ opioid receptor (Kappa Opioid Receptor) and activates G protein signaling. It has an EC50 of 14 nM and an Emax of 83% for binding to GTPγS. This compound demonstrates moderate to high intrinsic clearance in human liver cells and shows selectivity for the κ opioid receptor over the μ (MOR) and δ (DOR) opioid receptors by factors of 60 and 810, respectively. KOR agonist 4 is useful for research into central nervous system (CNS) disorders.

CJ-15208 is a potent and selective κ-opioid receptor antagonist from a fungus, Ctenomyces serratus ATCC15502 (IC50 are 47 nM for kappa, 260 nM for mu, and 2,600 nM for delta respectly). In the electrically-stimulated twitch response assay of rabbit vas de

LY255582 is a selective centrally active opioid receptor antagonist with high affinity for mu, delta and kappa receptors with Ki of 0.4 nM, 5.2, 2.0 nM, respectively. LY255582 inhibits diet-associated increases in mesolimbic dopamine levels and reduces consumption of food intake. LY255582 is commonly used in obesity research. LY255582 is a potential compound for the study of opioid receptor-mediated cell signaling.

MR2034 is an agonist of kappa-Opioid receptor. MR2034 stimulates hypothalamic-pituitary-adrenal axis.

R-84760 is a κ-opioid receptor agonist. R-84760 produces an extremely potent antinociceptive effect against tonic pain through the kappa-opioid receptors; the sites of action of subcutaneously administered R-84760 are the supraspinal and spinal loci in th

U-54494A hydrochloride is a benzamide derivative related to kappa opioid receptor agonists. U-54494A hydrochloride has anticonvulsant activity.

Selective sigma (σ) receptor ligand. Displays high affinity for σ1; also binds at σ2 sites (Ki = 1.5 nM and 50.8 nM respectively). Selective over a range of receptor types including dopaminergic and muscarinic receptors, DAT and SERT. Prezzavento et al (2007) Novel sigma receptor ligands: synthesis and biological profile. J.Med.Chem. 50 951 PMID:17328523 |Prezzavento et al (2008) A new sigma ligand, (±)-PPCC, antagonizes kappa opioid receptor-mediated antinociceptive effect. Life Sci. 82 549 PMID:18261749 |Antonini et al (2009) Anti-amnesic properties of (±)-PPCC, a novel sigma receptor ligand, on cognitive dysfunction induced by selective cholinergic lesion in rats. J.Neurochem. 109 744 PMID:19245662

Difelikefalin (CR-845; FE-202845) is a peripherally restricted, selective kappa opioid receptor (KOR) agonist with anti-inflammatory properties, demonstrating potential for modulating pruritus in chronic kidney disease.

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.

4-Me-PDTic is a potent and selective Kappa Opioid Receptor Antagonist. 4-Me-PDTic had a Ke = 0.37 nM in a [35S]GTPγS binding assay and was 645- and >8100-fold selective for the κ relative to the μ and δ opioid receptors, respectively. Calculated logBB and CNS (central nervous system) multiparameter optimization (MPO) and low molecular weight values all predict that 4-Me-PDTic will penetrate the brain and pharmacokinetic studies in rats shows that 4-Me-PDTic does indeed penetrate the brain.

4-Me-PDTic is a potent and selective kappa opioid receptor antagonist.

GNTI TFA is a selective kappa opioid receptor antagonist.

Riminkefon is a kappa opioid receptor agonist.

ICI-204879 HCl is a potent and selective agonists at the opioid kappa-receptor.

Enadoline (Free Base) is a kappa-opioid receptor agonist; PD 129290 (CAM 570; CI 977) is the S,S(-)-enantiomer; PD 129289 (CAM 569) is the corresponding R,R(+)-enantiomer. In human studies, it produced visual distortions and feelings of dissociation, reminiscent of the effects of salvinorin A. It was studied as a potential analgesic, but abandoned because of the dose-limiting effects of dysphoria, which could be expected from a κ-opioid agonist. There was mention of its potential in treating comatose head injury or stroke victims, where that type of side effect would be immaterial.

nor-Binaltorphimine dihydrochloride is a long-acting potent and highly selective kappa opioid receptor antagonist.

Anrikefon (HSK21542) is a kappa opioid receptor agonist with analgesic effects.