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).

Riminkefon is a kappa opioid receptor agonist.

GNTI TFA is a selective kappa opioid receptor antagonist.

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].

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

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.

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

SalA-VS-07 is a partial agonist of the kappa-opioid receptor (KOR), with a bias towards G proteins. It is useful for research in pain management and other medical conditions.

MOR agonist-4 (2d), having an EC50 of 11 nM, is a G protein-biased agonist of the Kappa opioid receptor (KOR). This compound features a triazole-based, electron-withdrawing CF3 group and a bias factor of 38. MOR agonist-4 is utilized for antipruritic and analgesic applications.

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

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].

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

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

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

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].

CR 665 (JNJ 38488502) is a peripherally selective κ-opioid agonist with an EC50 of 10.9 nM for kappa opioid receptor activation, used in peripheral pain research.

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

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

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