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 (614)
Related Products (614)
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Antibodies (3)
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Opioid Receptor Isoform Comparison
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BPRMU191
0 ImagesCat. No.: HY-159923CAS No.: 2131199-52-3BPRMU191 is a μ-opioid receptor (MOR) modulator that converts small-molecule morphinan antagonists into G protein-biased MOR agonists, thereby inducing MOR-dependent activation and analgesic effects. Co-administration of BPRMU191 with morphinan antagonists provides analgesia while reducing side effects such as gastrointestinal dysfunction, antinociceptive tolerance, and dependency-related adverse effects. BPRMU191, in combination with morphinan antagonists, offers a potential strategy for studying severe pain management and G protein-coupled receptor modulation.
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Ro-48-6791
0 ImagesCat. No.: HY-19267CAS No.: 172407-17-9Ro-48-6791 is a compound that may have the activity of activating opioid receptors. Computational studies have found that it may bind to and activate opioid receptors, and may mediate or increase their related physiological effects and side effects.
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Mu opioid receptor antagonist 2
0 ImagesCat. No.: HY-144607CAS No.: 2773925-64-5Mu opioid receptor antagonist 2 (compound 25) is a potent, selective and blood-brain barrier (BBB) penetrant μ opioid receptor (MOR) antagonist with a Ki of 0.37 nM and an EC50 of 0.44 nM. Mu opioid receptor antagonist 2 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 2 can be used for researching opioid use disorders (OUD).
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Dynorphin A TFA
0 ImagesCat. No.: HY-P1333ADynorphin A TFA is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A TFA is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A TFA can induce neuronal death, and can be used in the research of neurological disease.
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rel-SB-612111 hydrochloride
0 ImagesCat. No.: HY-18617CAS No.: 371980-94-8rel-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.
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PIPE-3297
0 ImagesCat. No.: HY-163277PIPE-3297 (compound 25) is a selective kappa opioid receptor (KOR) agonist, which activates the G-protein signaling with EC50 of 1.1 nM and exhibits low β-arrestin-2 recruitment activity (10%). PIPE-3297 induces myelination and reveals an anti-inflammatory activity.
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4-Isopropylbenzyl alcohol (Standard)
0 Images(±)-Leucine (Standard) is the analytical standard of (±)-Leucine. This product is intended for research and analytical applications. (±)-Leucine (DL-Leucine), an isomer of Leucine, chemosterilant and dietary additive. (±)-Leucine inhibits growth of Escherichia coli HfrH by 92.08%.
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[DPen2, Pen5] Enkephalin
![[DPen2, Pen5] Enkephalin](https://file.medchemexpress.com/product_pic/hy-p3546.gif "Click to View [DPen2, Pen5] Enkephalin Product Detail")
0 ImagesCat. No.: HY-P3546CAS No.: 88373-72-2[DPen2, Pen5] Enkephalin is a δ-opioid receptor selective analog of [Leu5]-Enkephalin (HY-P0288).
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Diallyl G
0 ImagesCat. No.: HY-129422CAS No.: 127808-81-5Diallyl G is a delta-opioid receptor antagonist. Diallyl G shows inhibitory effect on GTPase.
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ML138
0 ImagesCat. No.: HY-121800CAS No.: 1355243-24-1ML138 is a blood-brain barrier-permeable κ-opioid receptor (KOR) agonist, with an EC50 value of 0.87 μM and a human Ki value of 2.4 nM for human receptors; it exhibits high selectivity for KOR over μ, δ and other receptors. ML138 activates β-arrestin (beta-arrestin)-mediated signaling pathways, stimulates G protein coupling, and activates the downstream extracellular regulated protein kinase 1/2 (ERK1/2) mitogen-activated protein kinase (MAP kinase) signaling pathway. ML138 is applicable to research related to addictive behaviors.
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Phenethyl 4-ANPP
0 ImagesCat. No.: HY-172637CAS No.: 2712312-12-2Phenethyl 4-ANPP is a MOR (μ-opioid receptor) agonist. Phenethyl 4-ANPP is an analytical reference standard that is structurally similar to known opioids.
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Ac-RYYRIK-NH2
0 ImagesCat. No.: HY-P1318CAS No.: 200959-48-4Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain.
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N-Desmethylclozapine (Standard)
0 ImagesSynonyms: Norclozapine (Standard); Desmethylclozapine (Standard); Normethylclozapine (Standard)N-Desmethylclozapine (Standard) is the analytical standard of N-Desmethylclozapine. This product is intended for research and analytical applications. N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist.
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[(pF)Phe4]Nociceptin(1-13)NH2
![[(pF)Phe4]Nociceptin(1-13)NH2](https://file.medchemexpress.com/product_pic/hy-p1300.gif "Click to View [(pF)Phe4]Nociceptin(1-13)NH2 Product Detail")
0 ImagesCat. No.: HY-P1300CAS No.: 380620-88-2[(pF)Phe4]Nociceptin(1-13)NH2 is a highly potent and selective NOP receptor (OP4) agonist, with a pKi of 10.68 and a pEC50 of 9.31. [(pF)Phe4]Nociceptin(1-13)NH2 displays high selectivity over δ, κ, and μ opioid receptors (>3000 fold).
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[DAla2] Dynorphin A (1-9) (porcine)
![[DAla2] Dynorphin A (1-9) (porcine)](https://file.medchemexpress.com/product_pic/hy-p3646.gif "Click to View [DAla2] Dynorphin A (1-9) (porcine) Product Detail")
0 ImagesCat. No.: HY-P3646CAS No.: 95673-38-4[DAla2] Dynorphin A (1-9) (porcine) is a dynorphin, which can be used in studies of analgesic, addiction, and depression.
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GSK1521498
0 ImagesCat. No.: HY-19902CAS No.: 1426543-84-1GSK1521498 is a potent and selective μ-opioid receptor (MOR) antagonist. GSK1521498 has the potential for disorders of compulsive consumption of food, alcohol, and agents.
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Prodilidine hydrochloride
0 ImagesCat. No.: HY-105628ACAS No.: 3734-16-5Synonyms: CI-427 hydrochlorideProdilidine (CI-427) hydrochloride is a potent analgetic agent.
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Methocinnamox
0 ImagesCat. No.: HY-135698CAS No.: 117339-76-1Synonyms: M-CAMMethocinnamox (M-CAM) a selective and long-acting μ-opioid receptor (MOR) antagonist with a Ki of 0.6 nM. Methocinnamox binds to the orthosteric site of the MOR in a pseudo-irreversible, non-covalent manner, resulting in prolonged receptor blockade that persists until new receptors are synthesized. Methocinnamox acts as a reversible antagonist at both the kappa-opioid receptor (KOR) (Ki = 4.9 nM) and delta-opioid receptor (DOR) (Ki = 2.2 nM), and it exhibits no intrinsic agonist activity at these receptors. Methocinnamox can be used to reverse and prevent opioid overdose and addiction.
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Mu opioid receptor antagonist 9
0 ImagesCat. No.: HY-179282CAS No.: 3058600-77-1Mu opioid receptor antagonist 9 is potent, selective and CNS-pentrant mu-opioid receptor (MOR) antagonist with a Ki of 77.3 nM. Mu opioid receptor antagonist 9 exhibits selectivity over kappa-opioid receptor (KOR), and delta-opioid receptor (DOR). Mu opioid receptor antagonist 9 effectively blocks the antinociceptive effects of psychoactive substances. Mu opioid receptor antagonist 9 can reverse psychoactive substances-induced respiratory depression in mice. Mu opioid receptor antagonist 9 can be used for the research of Opioid Use Disorder (OUD).
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Trap-101 hydrochloride
0 ImagesCat. No.: HY-11052ACAS No.: 1216621-00-9Trap-101 hydrochloride is a potent, selective and competitive antagonist of NOP receptors over classical opioid receptors. Trap-101 stimulates GTPγ35S binding to CHOhNOP membranes with pKi values of 8.65, 6.60, 6.14 and <5 for NOP, μ-, κ-, and δ-opioid receptors, respectively. Trap-101 attenuates motor deficits in a rat model of parkinson's disease and can be used for the research of nervous system diseases.
