2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. Opioid Receptor
  5. κ Opioid Receptor/KOR Isoform
  6. κ Opioid Receptor/KOR Modulator

κ Opioid Receptor/KOR Modulator

κ Opioid Receptor/KOR Modulators (5):

Cat. No. Product Name Effect Purity
  • HY-125790
    Cyclazocine
    		Modulator
    Cyclazocine is a μ, δ, and κ opioid receptor modulator with Ki values of 0.32, 1.1, and 0.18 nM, respectively. Cyclazocine exhibits "mixed" pharmacological activities, acting as a μ-partial antagonist, κ-agonist, and low-affinity δ ligand. Cyclazocine shows antinociceptive activity in mice. Cyclazocine can be used in studies on psychoactive substance addiction.
  • HY-136832
    Noribogaine hydrochloride
    		Modulator 99.9%
    Noribogaine hydrochloride is an orally active, blood-brain barrier permeable SERT inhibitor (IC50=50-300 nM) and hERG channel blocker. Noribogaine hydrochloride enhances serotonergic transmission, activates the κ-opioid receptor (OPRK) G protein signaling pathway and inhibits β-arrestin recruitment. Meanwhile, Noribogaine hydrochloride blocks the μ-opioid receptor (OPRM) signaling pathway as well as ion channels associated with cardiac repolarization. Noribogaine hydrochloride induces neuritogenesis, upregulates GDNF mRNA expression, and modulates opioid tolerance. Noribogaine hydrochloride reduces alcohol-seeking behavior in experimental animals, and is widely used in studies related to depression, addiction, alcoholism, and cardiotoxicity.
  • HY-W158948
    6-Fluoro-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole
    		Modulator
    6-Fluoro-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole is a ORL-1 receptor modulator. 6-Fluoro-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole regulates downstream pathways associated with nociception, cognition and physiological processes. 6-Fluoro-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole is used in the research of central nervous system diseases and pain-related disorders including anxiety, depression, Alzheimer's disease and attention deficit disorder.
  • HY-170437
    MOR modulator-1
    		Modulator
    MOR modulator-1 (compound 6) is a potent and selective μ opioid receptor (MOR) modulator. MOR modulator-1 exhibits improved opioid receptor selectivity, enhanced in vivo antagonistic effect, and overall fewer withdrawal symptoms compared to NAT (6α-configuration). MOR modulator-1 links with carboxamido linker μ, δ, γ with Kis of 0.25, 41.1, 1.30 nM, respectively[1]
  • HY-182453
    RM1490
    		Modulator
    RM1490 (Compound 251) acts as an inhibitor of μ-opioid receptor (MOR) (IC50 ≤ 300 nM), an activator of δ-opioid receptor (DOR) (EC50 > 3000 nM), and an inhibitor of κ-opioid receptor (KOR) (IC50 ≤ 300 nM). RM1490 is applicable to the research of neuropsychiatric disorders.