2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. Opioid Receptor
  5. Opioid Receptor Inhibitor

Opioid Receptor Inhibitor

Opioid Receptor Isoform Comparison

Opioid Receptor Inhibitors (19):

Cat. No. Product Name Effect Purity
  • HY-15997
    (-)-U-50488 hydrochloride
    		Inhibitor 99.71%
    (-)-U-50488 hydrochloride ((-)-Trans-(1S,2S)-U-50488 hydrochloride) is a selective kappa-opioid receptor (KOR) agonist (b>Kd=2.2 nM) over μ-opioid receptor (MOR) (b>Kd=430 nM). (-)-U-50488 hydrochloride is a more active enantiomer than (+)?trans-(1R,2R) U-50488 (HY-15997A)?or the (±)?trans-racemic mixture U-50488 (HY-15997B). (-)-U-50488 hydrochloride has a potent and sustained anti-HIV effect in fected blood monocyte-derived macrophages (MDM).
  • HY-B0557
    Bisacodyl
    		Inhibitor 99.59%
    Bisacodyl is a stimulant laxative agent that works directly on the colon to produce a bowel movement. Bisacodyl increases the secretion of PGE2 by direct activation of colon macrophages. PGE2 acts as a paracrine factor and decreases the expression of AQP3 in the colon, which inhibits water transfer from the luminal to the vascular side and leads to a laxative effect.
  • HY-124754
    Navacaprant
    		Inhibitor 99.97%
    Navacaprant (BTRX-335140) is a selective and orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively. Navacaprant endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. Navacaprant distributes well into the CNS and can be used for the research of neuropathy.
  • HY-18618A
    SB-612111 hydrochloride
    		Inhibitor 99.26%
    SB-612111 hydrochloride hydrochloride is a novel and potent opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). SB-612111 hydrochloride exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 hydrochloride effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model.
  • HY-101392
    Harmane
    		Inhibitor 99.91%
    Harmane is an inhibitor that binds to benzodiazepine receptors (with an IC50 value of 7 μM), has an IC50 of 24 μM for muscarinic acetylcholine receptors (QNB), an IC50 of 2.8 μM for opioid receptors, and IC50 values of 163 and 101 μM for spironolactone and serotonin, respectively. Harmane is a selective monoamine oxidase inhibitor (with IC50 values of 0.5 μM for MAO A and 5 μM for MAO B). Harman inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing levodopa (L-DOPA)-induced toxicity in PC12 cells. Harmane lowers blood pressure in rats through the I1 imidazoline receptor (I1 receptor) and has antidepressant, anxiolytic, anticonvulsant, and analgesic effects. Harmane enhances the mutagenicity induced by 2-acetylaminofluorene (AAF) .
  • HY-Y0790
    Cuminaldehyde
    		Inhibitor 99.03%
    Cuminaldehyde is the main component of Cuminum cyminum and has multiple biological activities, including anti-inflammatory, anti-cancer, anti-diabetic, anti-injury, anti-neuropathy and antibacterial effects. Cuminaldehyde is an inhibitor of aldose reductase (IC50= 0.00085 mg/mL), α-glucosidase (IC50=0.5 mg/mL) and lipoxygenase (IC50=1370 μM). Cuminaldehyde has potential application value in the research of neurodegenerative diseases, cancer, diabetes and neuropathic pain diseases.
  • HY-139690
    CCG258747
    		Inhibitor 99.17%
    CCG258747 is a selective GRK2 inhibitor (IC50=18 nM) with high selectivity over GRK1, GRK5, PKA, and ROCK1 (518, 83, >5500, and >550–fold, respectively).CCG258747 also blocks the internalization of the µ-opioid receptor. G protein-coupled receptor (GPCR) kinases (GRKs) are attractive targets for the research of heart failure.
  • HY-N0398
    Sec-O-Glucosylhamaudol
    		Inhibitor 99.81%
    Sec-O-Glucosylhamaudol is a natural compound extracted from Peucedanum japonicum Thunb, decreases levels of μ-opioid receptor, with analgesic effect.
  • HY-P1596
    Gluten Exorphin C
    		Inhibitor 98.97%
    Gluten exorphin C is an opioid peptide derived from wheat gluten. Its IC50 values are 40 μM and 13.5 μM for μ opioid and δ opioid activities in the GPI and MVD assays, respectively.
  • HY-18618
    SB-612111
    		Inhibitor
    SB-612111 is a novel and potent opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). SB-612111 exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model.
  • HY-P1246
    Neuropeptide AF (human)
    		Inhibitor
    Neuropeptide AF (human) is an endogenous antiopioid peptide.
  • HY-18617
    rel-SB-612111 hydrochloride
    		Inhibitor
    rel-SB-612111 hydrochloride is a novel and potent human opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). rel-SB-612111 hydrochloride exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. rel-SB-612111 hydrochloride effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model.
  • HY-N7437
    Akuammidine
    		Inhibitor
    Akuammidine, isolated from the seeds of Picralima nitida, shows a preference for μ-opioid binding sites with Ki values of 0.6, 2.4 and 8.6 μM at μ-, σ- and κ-opioid binding sites, respectively. Akuammidine possesses anti-inflammatory and anti-asthmatic properties.
  • HY-Y0790R
    Cuminaldehyde (Standard)
    		Inhibitor
    Cuminaldehyde (Standard) is the analytical standard of Cuminaldehyde. This product is intended for research and analytical applications. Cuminaldehyde is the main component of Cuminum cyminum and has multiple biological activities, including anti-inflammatory, anti-cancer, anti-diabetic, anti-injury, anti-neuropathy and antibacterial effects. Cuminaldehyde is an inhibitor of aldose reductase (IC50= 0.00085 mg/mL) and α-glucosidase (IC50=0.5 mg/mL). Cuminaldehyde can modulate α-synuclein fibrils. Cuminaldehyde can induce apoptosis in colon adenocarcinoma cells by targeting topoisomerase I and II. In addition, Cuminaldehyde also exerts anti-inflammatory activity by inhibiting lipoxygenase. Cuminaldehyde has a strong inhibitory effect on the growth of Aspergillus flavus and the biosynthesis of aflatoxin B1 (AFB1). Cuminaldehyde can exert anti-injury and anti-neuropathy effects by participating in opioid receptors, L-arginine/NO/cGMP pathways and anti-inflammatory effects. Cuminaldehyde has potential application value in the research of neurodegenerative diseases, cancer, diabetes and neuropathic pain diseases.
  • HY-N0398R
    Sec-O-Glucosylhamaudol (Standard)
    		Inhibitor
    Sec-O-Glucosylhamaudol (Standard) is the analytical standard of Sec-O-Glucosylhamaudol. This product is intended for research and analytical applications. Sec-O-Glucosylhamaudol is a natural compound extracted from Peucedanum japonicum Thunb, decreases levels of μ-opioid receptor, with analgesic effect.
  • HY-141468
    β-Chlornaltrexamine dihydrochloride
    		Inhibitor
    β-Chlornaltrexamine dihydrochloride (β-CNA dihydrochloride) is a potent long-term opioid receptor blocker. β-Chlornaltrexamine dihydrochloride can effectively block the inhibitory effect of κ opioid receptor agonists on dopamine release. β-Chlornaltrexamine dihydrochloride can be used to study the mechanism of pain perception.
  • HY-120846
    CHIR 4531
    		Inhibitor
    CHIR 4531, a trimer peptide, is a opiate ligand that binds to the mu-opiate receptor with a Ki of 6 nM.
  • HY-B0557R
    Bisacodyl (Standard)
    		Inhibitor
    Bisacodyl (Standard) is the analytical standard of Bisacodyl. This product is intended for research and analytical applications. Bisacodyl is a stimulant laxative agent that works directly on the colon to produce a bowel movement. Bisacodyl increases the secretion of PGE2 by direct activation of colon macrophages. PGE2 acts as a paracrine factor and decreases the expression of AQP3 in the colon, which inhibits water transfer from the luminal to the vascular side and leads to a laxative effect.
  • HY-W028263
    6-Hydroxyflavanone
    		Inhibitor
    6-Hydroxyflavanone is a compound that can be isolated from the Muntingia calabura leaves. 6-Hydroxyflavanone targets cyclooxygenase-2 (COX-2), 5-lipoxygenase (5-LOX), and opioid and GABA-A receptors that has anti-inflammatory and anti-neuropathic pain potential. 6-Hydroxyflavanone can be used for the research of diabetes.