kappa-opioid

Aticaprant (LY-2456302) (CERC-501) is a potent and centrally-penetrant antagonist of the kappa-opioid receptor (Ki: 0.807 nM).

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.

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.

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

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

Leumorphin, human, is a potent agonist of the kappa opioid receptor (κ opioid receptor) and inhibits the contraction of the guinea pig ileum's myenteric plexus-longitudinal muscle preparation [1].

PD 117302 is a nonpeptide opioid compound. It is a selective kappa-opioid agonist. PD 117302 causes naloxone-reversible locomotor impairment and diuresis. It is an Anti-Arrhythmia Agent, an Anticonvulsants, a Cardiovascular Agent, and a Central Nervous Sy

Akuammidine shows anti-inflammatory and anti-asthmatic properties, it has opioid analgesic activity, it shows a preference for mu-opioid binding sites with Ki values of 0.6, 2.4 and 8.6 microM at mu-, delta- and kappa-opioid binding sites, respectively.

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

Akuammigine has in vitro antimalarial activity. Akuammigine competitively antagonizes the effect of noradrenaline on postsynaptic alpha-adrenoceptors, yielding pA2 values of 4.68. Akuammidine also shows a preference for mu-opioid binding sites with Ki val

Tifluadom is a type of kappa-opioid benzodiazepine.

GNTI TFA is a selective kappa opioid receptor antagonist.

Riminkefon is a kappa opioid receptor agonist .

FE-200041 is a peripheral efficacious kappa opioid agonist.

CR-665, a kappa-opioid agonist, is used potentially for the treatment of postoperative pain.

E-2078, known chemically as (N-Me-Tyr1,N-Me-Arg7,D-Leu-NHEt8)-Dynorphin A (1-8), is a stable analog of Dynorphin A (1–8) and functions as a kappa opioid receptor (KOR) agonist [1].

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

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.

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

Trimebutine maleate (Polibutin) is a weak mu-opioid agonist and has antimuscarinic effects. Trimebutine is an agonist of peripheral mu, delta, and kappa opiate receptors served as a spasmolytic drug for therapy of both chronic and acute abdominal pain.

Eptazocine hydrobromide is an agonist of the Opioid receptor and is a kappa-Opioid receptor agonist. It is also an Opioid analgesic and an Opioid receptor antagonist.

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

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

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

Endomorphin-1 acetate is a highly selective and high-affinity μ-opioid receptor agonist (K i: 1.11 nM) that also demonstrates moderate affinity for kappa 3 binding sites (K i: 20-30 nM). This compound exhibits antinociceptive properties.

Dynorphin A TFA, an endogenous opioid peptide, plays a role in inhibitory neurotransmission within the central nervous system (CNS). It acts as a highly potent kappa opioid receptor (KOR) agonist and also stimulates other opioid receptors, including mu (MOR) and delta (DOR). Furthermore, Dynorphin A TFA has been observed to induce neuronal death, making it a significant subject in neurological disease research [1] [2].

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

Niravoline is a kappa-opioid agonist.

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.

CR 665 (JNJ 38488502) is a peripherally selective κ-opioid agonist, capable of activating the kappa opioid receptor with an EC50 value of 10.9 nM. It is utilized in the research of peripheral pain.

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

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

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

Icalcaprant is a kappa-opioid receptor antagonist [1].

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.

CSD-CH2(1,8)-NH2 is a selective and competitive kappa-opioid receptor (KOR) antagonist with a K i of 6.8 nM. It inhibits calcium mobilization in dorsal root ganglion (DRG) neurons and antagonizes the antinociceptive effect of U50,488, making it useful for research into neuropsychiatric disorders [1].

Difelikefalin (CR-845; FE-202845) is a peripherally restricted, selective agonist of the kappa opioid receptor (KOR). It exhibits anti-inflammatory properties and holds promise for modulating pruritus in conditions associated with chronic kidney disease.

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

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.

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

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.

Naloxone-d5 HCl is a deuterated compound of Naloxone HCl. Naloxone HCl has a CAS number of 357-08-4. Naloxone hydrochloride is a specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.

Naloxone-d5 is a deuterated compound of Naloxone.