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Opioid Receptor

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Opioid Receptor 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. www.MedChemExpress.com 1 Opioid Receptor Agonists, Antagonists, Inhibitors, Activators & Modulators 6'-GNTI dihydrochloride 6-Alpha Naloxol Cat. No.: HY-110302 (Alpha-Naloxol) Cat. No.: HY-12799 6'-GNTI dihydrochloride, a κ-opioid receptor (KOR) 6-Alpha Naloxol(Alpha-Naloxol) is an opioid agonist, displays bias toward the activation of G antagonist closely related to naloxone; a human protein-mediated signaling over β-arrestin2 metabolite of naloxone. recruitment. 6'-GNTI 6'-GNTI dihydrochloride only activates the Akt pathway in striatal neurons. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg 6-beta-Naloxol D5 hydrochloride Ac-RYYRIK-NH2 (6β-Naloxol D5 hydrochloride) Cat. No.: HY-12780S Cat. No.: HY-P1318 6-beta-Naloxol D5 hydrochloride is the deuterium Ac-RYYRIK-NH2 is a potent and partial agonist on labeled 6-beta-Naloxol, which is an opioid ORL1 transfected in CHO cells (Kd=1.5 nM) and antagonist closely related to naloxone. behaves as a endogenous ligand of ORL1. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg Ac-RYYRIK-NH2 TFA Ac-RYYRWK-NH2 Cat. No.: HY-P1318A Cat. No.: HY-P1316 Ac-RYYRIK-NH2 TFA is a potent and partial agonist Ac-RYYRWK-NH2 is a potent and selective partial on ORL1 transfected in CHO cells (Kd=1.5 nM) agonist for the nociceptin receptor (NOP), and behaves as a endogenous ligand of ORL1. [3H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a Kd of 0.071 nM, but has no affinity for µ-, κ- or δ-opioid receptors. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg Ac-RYYRWK-NH2 TFA ADL-5859 Cat. No.: HY-P1316A Cat. No.: HY-13044 Ac-RYYRWK-NH2 is a potent and selective partial ADL5859 is a δ-opioid receptor agonist with Ki of agonist for the nociceptin receptor (NOP), 0.8 nM, selectivity against opioid receptor κ, μ, [3H]Ac-RYYRWK-NH2 binds to rat cortical and weak inhibitory activity at the hERG channel. membranes ORL1 with a Kd of 0.071 nM, but has no affinity for µ-, κ- or δ-opioid receptors. Purity: >98% Purity: 99.77% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Adrenorphin Akuammidine (Metorphamide) Cat. No.: HY-P1087 Cat. No.: HY-N7437 Adrenorphin is a opioid octapeptide, acting as a Akuammidine, isolated from the seeds of potent agonist of μ-opioid receptor, with Ki of 12 Picralima nitida, shows a preference for μ-opioid nM. 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. Purity: 95.49% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg 2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Alvimopan Alvimopan dihydrate (ADL 8-2698; LY 246736) Cat. No.: HY-13243 (ADL 8-2698 dihydrate; LY 246736 dihydrate) Cat. No.: HY-76657A Alvimopan (ADL 8-2698) is a potent, selective, Alvimopan dihydrate (ADL 8-2698 dihydrate) is a orally active and reversible μ-opioid receptor potent, selective, orally active and reversible antagonist, with an IC50 of 1.7 nM. Alvimopan has μ-opioid receptor antagonist, with an IC50 of 1.7 selectivity for μ-opioid receptor (Ki=0.47 nM) nM. over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Purity: >98% Purity: 98.70% Clinical Data: Launched Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg Alvimopan monohydrate AR-M 1000390 hydrochloride (ADL 8-2698 monohydrate; LY 246736 monohydrate) Cat. No.: HY-76657 Cat. No.: HY-101039A Alvimopan monohydrate (ADL 8-2698 monohydrate) is AR-M 1000390 hydrochloride is an exceptionally a potent, selective, orally active and reversible selective, potent δ opioid receptor agonist with μ-opioid receptor antagonist, with an IC50 of 1.7 an EC50 of 7.2±0.9 nM for δ agonist potency. nM. Purity: 99.18% Purity: 99.80% Clinical Data: Launched Clinical Data: No Development Reported Size: 2 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Asimadoline Asimadoline hydrochloride (EMD-61753) Cat. No.: HY-107384 (EMD-61753 hydrochloride) Cat. No.: HY-107384A Asimadoline (EMD-61753) is an orally active, Asimadoline (EMD-61753) hydrochloride is an orally selective and peripherally active κ-opioid agonist active, selective and peripherally active κ-opioid with IC50s of 5.6 nM (guinea pig) and 1.2 nM agonist with IC50s of 5.6 nM (guinea pig) and 1.2 (human recombinant). nM (human recombinant). Purity: 99.36% Purity: 99.80% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg AT-121 AT-121 hydrochloride Cat. No.: HY-112692 Cat. No.: HY-112692A AT-121 is a bifunctional nociception and mu AT-121 hydrochloride is a bifunctional nociception opioid receptor agonist, with Kis of 3.67 and and mu opioid receptor agonist, with Kis of 16.49 nM, respectively. AT-121 is a safe, 3.67 and 16.49 nM, respectively. AT-121 non-addictive analgesic, and shows antinociceptive hydrochloride is a safe, non-addictive analgesic, and antiallodynic effects. and shows antinociceptive and antiallodynic effects. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg Aticaprant BAM-22P (CERC-501; LY-2456302) Cat. No.: HY-101718 (Bovine adrenal medulla-22P) Cat. No.: HY-P1331 Aticaprant (CERC-501) is a potent and BAM-22P, a highly potent opioid peptide, is a centrally-penetrant kappa opioid receptor potent opioid agonist. antagonist with a Ki of 0.807 nM. Purity: 99.86% Purity: >98% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg, 20 mg, 50 mg Size: 500 μg, 1 mg, 5 mg www.MedChemExpress.com 3 BAN ORL 24 Bevenopran Cat. No.: HY-13222 (CB-5945; ADL-5945) Cat. No.: HY-100122 BAN ORL 24 is a potent and selective NOP receptor Bevenopran is a peripheral μ-opioid receptor antagonist. (IC50 values are 0.27, 2500, 6700 and antagonist. > 10000 nM for NOP, κ-, μ- and δ-receptors respectively). Purity: 98.09% Purity: >98% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg BPR1M97 BTRX-335140 Cat. No.: HY-128865 (CYM-53093) Cat. No.: HY-124754 BPR1M97 is a dual-acting mu opioid receptor BTRX-335140 (CYM-53093) is a potent and selective, (MOP) and nociceptin-orphanin FQ peptide (NOP) orally active κ opioid receptor (KOR) receptor agonist with Ki values of 1.8 and 4.2 antagonist, has antagonist activity for κOR, μOR nM, respectively. BPR1M97 shows high potency and and δOR with IC50 values of 0.8 nM, 110 nM, and blood-brain barrier penetration, and produces 6500 nM, respectively. potent antinociceptive effects. Purity: 98.99% Purity: 99.71% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg Cebranopadol Cebranopadol ((1α,4α)stereoisomer) (GRT6005) Cat. No.: HY-15536 (GRT6005 (1α,4α)stereoisomer) Cat. No.: HY-15536A Cebranopadol is an analgesic NOP and opioid Cebranopadol ((1α,4α)stereoisomer) is a receptor agonist with Kis/EC50s of 0.9 nM/13 stereoisomer of cebranopadol. Cebranopadol is a nM, 0.7 nM/1.2 nM, 2.6 nM/17 nM, 18 nM/110 nM for potent agonist activity on ORL-1. human NOP, MOP, KOP and delta-opioid peptide (DOP) receptor, respectively. Purity: 96.91% Purity: 95.60% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg Size: 10 mM × 1 mL, 2 mg, 5 mg Corydaline CTAP ((+)-Corydaline; Corydalin) Cat. No.: HY-N0923 Cat. No.: HY-P1335 Corydaline ((+)-Corydaline), an isoquinoline CTAP is a potent, highly selective, and brain alkaloid isolated from Corydalis yanhusuo, is an penetrant μ opioid receptor antagonist (IC50=3.5 AChE inhibitor with an IC50 of 226 µM. Corydaline nM) and displays over 1200-fold selectivity over δ is a μ-opioid receptor (Ki of 1.23 µM) agonist and opioid (IC50=4500 nM) and somatostatin receptors.
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