Opioid Receptor
Opioid receptors are a group of G protein-coupled receptors with opioids as ligands. The endogenous opioids are dynorphins, enkephalins, endorphins, endomorphins and nociceptin. Opioid receptors are distributed widely in the brain, and are found in the spinal cord and digestive tract. Opioid receptors are molecules, or sites, within the body that are activated by opioid substances. Opioid receptors inhibit the transmission of impulse in excitatory pathways within the human body system. These pathways include the serotonin, catecholamine, and substance P pathways, which are all implicated in pain perception and feelings of well-being. Opioid receptors are further subclassified into mu, delta, and kappa receptors. All the classes, while exhibiting differing modes of action, share some basic similarities. They all are driven by the potassium pump mechanism, which is found on the plasma membrane of the majority of cells.
Opioid Receptor Isoform Specific Products
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Opioid Receptor Inhibitors
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Opioid Receptor Agonists
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Opioid Receptor Antagonists
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Opioid Receptor Activators
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Opioid Receptor Modulators
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Opioid Receptor Controls
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Opioid Receptor Ligands
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Opioid Receptor Related Products (616)
Related Products (616)
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Antibodies (3)
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Opioid Receptor Isoform Comparison
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Naloxegol
0 ImagesCat. No.: HY-A0118CAS No.: 854601-70-0Synonyms: NKTR-118; AZ-13337019Naloxegol (NKTR-118; AZ-13337019) is an orally active peripherally acting μ-opioid receptor antagonist with a target Ki of 7.42 nM. Naloxegol inhibits the binding of opioids to μ-opioid receptors in the gastrointestinal tract, and alleviates opioid-induced gastrointestinal hypomotility, delayed transit, hypertonicity, and increased fluid reabsorption. Naloxegol is applicable to research related to opioid-induced constipation.
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Cyprodime
0 ImagesCat. No.: HY-107750CAS No.: 118111-54-9Cyprodime is a selective μ opioid receptor (MOR) antagonist with Kis of 5.4, 244.6, and 2187 nM for μ, δ, and κ, respectively.
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LY2444296
0 ImagesSynonyms: FP3FBZLY2444296 is an orally bioavailable, high-affinity and selective short-acting kappa opioid receptor (KOPR) antagonist, with a Ki value of ～1 nM. LY2444296 exhibits anti-anxiety like effects.
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DIPPA hydrochloride
0 ImagesDIPPA hydrochloride is an irreversible, long-lasting, selective and high affinity κ-opioid receptor antagonist. DIPPA hydrochloride can be used for the research of anxiety and antidepressant.
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6β-Naltrexol
0 ImagesSynonyms: 6β-Hydroxynaltrexone6β-Naltrexol (6β-Hydroxynaltrexone), the primary metabolite of Naltrexone, is a peripherally selective opioid antagonist. 6β-Naltrexol selectively inhibits gastrointestinal opioid effects in human subjects and inhibits Morphine-induced slowing of gastrointestinal transit.
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BNTX maleate
0 ImagesSynonyms: 7-Benzylidenenaltrexone maleateBNTX (7-Benzylidenenaltrexone) maleate is a δ1-opioid receptor antagonist with the Kis of 0.1, 10.8, 13.3, and 58.6 nM for δ1, δ2-, μ-, and κ-opioid receptor, respectively. BNTX maleate shows antinociceptive activity.
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Methyl-6-alpha-Naltrexol
0 ImagesCat. No.: HY-N2304ACAS No.: 116388-85-3Methyl-6-alpha-Naltrexol is a metabolite of Methylnaltrexone (MNTX). Methylnaltrexone is a selective mu-opioid receptor antagonist and functions as a peripherally acting receptor antagonist in tissues of the gastrointestinal tract.
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Alvimopan monohydrate
0 ImagesCat. No.: HY-76657CAS No.: 1383577-62-5Synonyms: ADL 8-2698 monohydrate; LY 246736 monohydrateAlvimopan monohydrate (ADL 8-2698 monohydrate) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan monohydrate has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan monohydrate can be used for the research of postoperative ileus.
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JDTic
0 ImagesCat. No.: HY-10486CAS No.: 361444-66-8JDTic is a blood-brain barrier-permeable κ-opioid receptor antagonist (Ki=0.02 nM) with favorable in vitro ADME properties. JDTic blocks agonist-mediated Gi and β-arrestin signaling pathways as well as analgesic effects by stabilizing the inactive conformation of hKOR and activating JNK. JDTic may also induce transient asymptomatic ventricular tachycardia. JDTic is widely applicable to studies related to depression, anxiety, stress-induced addictive behaviors, and nicotine withdrawal.
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Naloxone hydrochloride dihydrate
0 ImagesCat. No.: HY-17417BCAS No.: 51481-60-8Naloxone hydrochloride is an orally active opioid receptor antagonist. Naloxone hydrochloride attenuates spinal cord stimulation‑associated anti‑hyperalgesic effects, antagonizes physiologic effects of endogenous opioid peptides linked to central nervous system injury sequelae, functions as a pressor agent to induce modest elevations in mean arterial blood pressure, exerts neuroprotective effects to improve post‑traumatic neurologic motor function, blocks opioid receptor‑mediated amnesic pathways, enhances memory consolidation, reverses Adrenocorticotropic hormone (ACTH) (HY-106373)‑ and epinephrine‑induced amnesia, and potentiates the memory‑facilitatory effects of ACTH and epinephrine.
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PF-4455242 hydrochloride
0 ImagesPF-4455242 hydrochloride is an orally bioavailable, blood-brain barrier-permeable κ-opioid receptor (KOR) inhibitor. PF-4455242 hydrochloride blocks in vivo effects induced by KOR and MOR agonists, and elicits KOR-independent outward currents in ventral tegmental area neurons. PF-4455242 hydrochloride promotes energy expenditure and activates the hypothalamic mTOR pathway. PF-4455242 hydrochloride attenuates stress-induced behavioral effects and produces antidepressant-like effects. PF-4455242 hydrochloride can be used in studies related to pain, depression, addictive disorders, and obesity induced by estrogen withdrawal.
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PF-04455242
0 ImagesCat. No.: HY-15691CAS No.: 1202647-54-8PF-04455242 is an orally bioavailable, blood-brain barrier-permeable κ-opioid receptor (KOR) inhibitor. PF-04455242 blocks in vivo effects induced by KOR and MOR agonists, and elicits KOR-independent outward currents in ventral tegmental area neurons. PF-04455242 promotes energy expenditure and activates the hypothalamic mTOR pathway. PF-04455242 attenuates stress-induced behavioral effects and produces antidepressant-like effects. PF-04455242 can be used in studies related to pain, depression, addictive disorders, and obesity induced by estrogen withdrawal.
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Naloxone hydrochloride solution
0 ImagesCat. No.: HY-FL17417BCAS No.: 51481-60-8Naloxone hydrochloride solution is mainly composed of Naloxone hydrochloride dihydrate (HY-17417B). Naloxone hydrochloride is an antagonist of Opioid receptor. Naloxone hydrochloride alleviates opioid-overdose-induced respiratory depression. Naloxone hydrochloride may cause pulmonary edema and cardiac arrhythmias.
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GSK1521498 free base hydrochloride
0 ImagesCat. No.: HY-115066ACAS No.: 1007578-24-6GSK1521498 free base (hydrochloride) is a potent and selective μ-opioid receptor (MOR) antagonist. GSK1521498 free base (hydrochloride) is being used for the treatment of disorders of compulsive consumption of food, alcohol, and agents.
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Icalcaprant
0 ImagesCat. No.: HY-156614CAS No.: 2227384-17-8Icalcaprant is a kappa-opioid receptor antagonist.
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AT-076
0 ImagesCat. No.: HY-106732CAS No.: 1657028-64-2AT-076 is an opioid pan antagonist at nociception, kappa, mu, and delta opioid receptors, with Ki values of 1.75 nM (NOP), 1.67 nM (MOP), 1.14 nM (KOP) and 19.6 nM (DOP), respectively.
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Loperamide phenyl
0 ImagesLoperamide phenyl is an impurity of Loperamide (HY-B0418A). Loperamide is an opioid receptor agonist.
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MK-5757
0 ImagesCat. No.: HY-14124CAS No.: 919482-44-3MK-5757 is a Nociceptin/Orphanin FQ Peptide Receptor antagonist. ORL1 antagonist 3 can improve cerebral blood flow disorders and ischemic damage, and alleviate abnormal neurological symptoms. ORL1 antagonist 3can be used for the research of neurological disease, such as traumatic brain injury.
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Naltrexone (Standard)
0 ImagesNaltrexone (Standard) is the analytical standard of Naltrexone (HY-76711). This product is intended for research and analytical applications. Naltrexone is an orally active, long-acting opioid receptor (opioid receptor) antagonist. Naltrexone blocks the euphoric effects of exogenous opioids and reduces alcohol craving by blocking opioid receptors (μ, κ, and δ) as well as opioid growth factor receptors. Low doses of Naltrexone are used to relieve chronic pain, treat inflammatory diseases and inhibit tumor growth, while high doses or continuous administration exert pro-inflammatory or pro-proliferative effects. Naltrexone relieves intractable pruritus caused by psoriasis, atopic dermatitis and other conditions, and its combination with Bupropion (HY-B0403) inhibits food craving, thereby reducing body weight.
