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Opioid Receptor Inhibitors (Inhibitors, Agonists and Modulators)

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Opioid Receptor Inhibitors (Inhibitors, Agonists and Modulators) Tel: 1-631-504-6093 Fax: 1-631-614-7828 E-mail: [email protected] 45-16 Ramsey Road Shirley, NY 11967, USA Opioid Receptor Inhibitors (inhibitors, agonists and modulators) Opioid receptors have been targeted for the treatment of pain and related disorders for thousands of years, and remain the most widely used analgesics in the clinic. Mu (μ), kappa (κ), and delta (δ) opioid receptors represent the originally classified receptor subtypes, with opioid receptor like-1 (ORL1) being the least characterized. All four receptors are G- protein coupled, and activate inhibitory G-proteins. These receptors form homo- and hetereodimeric complexes, signal to kinase cascades, and scaffold a variety of proteins. www.bocsci.com PZM21 - CAS 1997387-43-5 Catalog Number: B0084-007152 Price: $149/10 mg; $298/25 mg Molecular Weight: 361.5 Molecular Formula: C19H27N3O2S Description: PZM21 is a potent Gi activator with exceptional selectivity for μOR (EC50= 1.8 nM) and minimal β-arrestin-2 recruitment. [D-Ala2]-Leucine enkephalin - CAS 64963-01-5 Catalog Number: B0084-040423 Price: $388/1 g Molecular Weight: 569.659 Molecular Formula: C29H39N5O7 Description: [D-Ala2]-Leucine enkephalin is a delta opioid agonist used to study the signaling pathway of delta opioid receptors. (+)-Matrine - CAS 519-02-8 Catalog Number: B0084-070319 Price: $299/2 g Molecular Weight: 248.36 Molecular Formula: C15H24N2O Description: Matrine((+)-Matrine) is an alkaloid found in plants from the Sophora family, which has a variety of pharmacological effects, including anti-cancer effects, and action as a kappa opioid receptor agonist. Asimadoline - CAS 153205-46-0 Catalog Number: B0084-071264 Price: $399/50 mg Molecular Weight: 414.549 Molecular Formula: C27H30N2O2 Description: Asimadoline is a κ opioid receptor agonist with less brain-penetrant ability. Asimadoline is the potential treatment of irritable bowel syndrome. Mitragynine - CAS 4098-40-2 Catalog Number: B0084-071458 Price: $395/250 mg Molecular Weight: 398.503 Molecular Formula: C23H30N2O4 Description: Mitragynine is an indole alkaloid isolated from the plant Mitragyna speciosa, and acts as an opioid receptor agonist with preference for μ-opioid receptor. It is a neurochemical that exhibits stimulatory, antinociceptive, and opiate-like effects. 2 / 26 www.bocsci.com Naloxegol oxalate - CAS 1354744-91-4 Catalog Number: B0084-465947 Price: $229/100 mg Molecular Weight: 741.82 Molecular Formula: C36H55NO15 Description: Naloxegol oxalate is a CYP3A4 enzyme inhibitor, is a peripherally-selective opioid antagonist, for the treatment of opioid-induced constipation. LY2795050 - CAS 1346133-08-1 Catalog Number: B0084-474497 Price: $199/5 mg Molecular Weight: 407.89 Molecular Formula: C23H22ClN3O2 Description: LY2795050, a κ-opioid Receptor antagonist, has been found to be effective in imaging KOR behaving as a PET tracer. IC50: 0.72 nM and 25.8 nM for κ-opioid Receptor and κ-opioid. LY-2456302 - CAS 1174130-61-0 Catalog Number: Molecular Weight: 418.5 Molecular Formula: C26H27FN2O2 Description: LY-2456302, also called as CERC-501, is a potent, highly selective and centrally- penetrant kappa opioid receptor antagonist(Ki= 0.807 nM)with favorable pharmacokinetic and pharmacodynamic properties to evaluate the role of KOR in preclinical models of alcoholism. Hemorphin-7 - CAS 152685-85-3 Catalog Number: Molecular Weight: 997.11 Molecular Formula: C49H64N12O11 Description: Hemorphin-7, a hemorphin peptide with antinociceptive and antihypertensive effects, is an endogenous opioid peptide derived from the β-chain of hemoglobin. Hemorphin peptides activates opioid receptors and inhibiting angiotensin-converting enzyme (ACE). The much lower affinity of hemorphin- 7 for μ-receptors as compared to other opioid peptides may be compensated by its much higher plasma concentration, resulting in biological effects of comparable magnitude. 3 / 26 www.bocsci.com [(pF)Phe4]Nociceptin(1-13)NH2 - CAS 380620-88-2 Catalog Number: Molecular Weight: 1399.6 Molecular Formula: C61H99FN22O15 Description: [(pF)Phe4]Nociceptin(1-13)NH2 is a highly potent and selective nociceptin/orphanin FQ receptor (OP4) agonist peptide (pKi = 10.68; pEC50 = 9.80), with 8000-fold selectivity over δ, κ, and μ opioid receptors. BAM 22P - CAS 76622-26-9 Catalog Number: Molecular Weight: 2839.24 Molecular Formula: C130H184N38O31S2 Description: BAM 22P is a potent endogenous agonist peptide for sensory neuron specific receptor (SNSR) (EC50 = 13 and 16 nM for human SNSR3 and SNSR4, respectively). BAM 22P is also a potent opioid agonist (IC50 = 1.3 nM in guinea pig ileum preparation) displaying opioid- and non-opioid receptor mediated antinociceptive effects in vivo. DAMGO - CAS 78123-71-4 Catalog Number: Molecular Weight: 513.7 Molecular Formula: C26H35N5O6 Description: DAMGO is a highly selective peptide agonist of the μ opioid receptor. Dynorphin A - CAS 80448-90-4 Catalog Number: Molecular Weight: 2147.51 Molecular Formula: C99H155N31O23 Dynorphin A is a heptadecapeptide which is derived from the cleavage of Description: prodynorphin and found widely distributed in the central nervous system. It acts as an endogenous kappa receptor agonist with nanomolar binding affinity. It also activates human novel opioid receptor-like receptor of ORL1. It is resistant to enzymatic degradation and may has antinociceptive functions. 4 / 26 www.bocsci.com PL 017 - CAS 83397-56-2 Catalog Number: Molecular Weight: 535.64 Molecular Formula: C29H37N5O5 Description: PL 017, a morphiceptin analog, is a selective μ opioid receptor agonist (IC50= 5.5 and > 10000 nM for inhibition of 125I-FK 33,824 and 125I-DADLE binding to μ and δ sites respectively). Although the affinity of PL017 for µ-sites is lower than that of morphine, PL 017 is more potent than morphine in all in vitro studies, suggesting a difference in the way in which peptide and alkaloid activate µ-receptors. DPDPE - CAS 88373-73-3 Catalog Number: 645.79 C30H39N5O7S2 Molecular Weight: Molecular Formula: Description: DPDPE, a selective δ-opioid receptor agonist peptide, has been found to exhibit antinociceptive actions. DADLE - CAS 63631-40-3 Catalog Number: Molecular Weight: 569.66 Molecular Formula: C29H39N5O7 Description: DADLE is a prototypical δ-opioid receptor agonist with antinociceptive activity. It also exhibits activity at the μ-opioid receptor. ICI 174,864 - CAS 89352-67-0 Catalog Number: Molecular Weight: 691.87 Molecular Formula: C38H53N5O7 Description: ICI 174,864 is a potent and highly selective δ opioid antagonist. It shows partial agonist in vitro activity at δ receptors at high concentrations. CTAP - CAS 103429-32-9 Catalog Number: Molecular Weight: 1104.32 Molecular Formula: C51H69N13O11S2 Description: CTAP has been found to be a selective μ-opioid receptor antagonist. 5 / 26 www.bocsci.com Nor-Binaltorphimine dihydrochloride - CAS 113158-35-3 Catalog Number: Molecular Weight: 734.71 Molecular Formula: C40H43N3O6.2HCl Description: Nor-Binaltorphimine dihydrochloride is a potent and selective kappa opioid receptor antagonist. Nalbuphine hydrochloride - CAS 23277-43-2 Catalog Number: Molecular Weight: 393.9 Molecular Formula: C21H27NO4.HCl Description: Nalbuphine hydrochloride is the hydrochloride salt form of Nalbuphine, an agonist at κ-opioid receptors and an antagonist or partial agonist at μ-opioid receptors. Nalbuphine is used as a narcotic. Ac-RYYRWK-NH - CAS 200959-47-3 Catalog Number: Molecular Weight: 1012.17 Molecular Formula: C49H69N15O9 Description: Ac-RYYRWK-NH, a hexapeptide, is a partial agonist of the nociceptin/orphanin FQ (N/OFQ) peptide (NOP) receptorr (Ki = 0.71 nM), which exhibits selectivity over μ, δ and κ opioid receptors (IC50 > 4000 nM). Ac-RYYRIK-NH - CAS 200959-48-4 Catalog Number: Molecular Weight: 939.12 Molecular Formula: C44H70N14O9 Description: Ac-RYYRIK-NH may provide a promising starting point for in vivo tests for antagonism of the action of noc/OFQ and for the further development of highly active and specific antagonists. 6 / 26 www.bocsci.com Naltrexone - CAS 16590-41-3 Catalog Number: 16590-41-3 Molecular Weight: 341.40 Molecular Formula: C20H23NO4 Description: Naltrexone, also called as Celupan, competitively antagonise μ, κ, δ, and σ-opioid receptors with the effect to reduce the occurrence of addictive behaviours . Naltrexone HCl - CAS 16676-29-2 Catalog Number: 16676-29-2 Molecular Weight: 377.86 Molecular Formula: C20H23NO4.HCl Description: Naltrexone significantly suppresses ethanol self-administration and prevents ethanol-induced increases in dialysate dopamine levels. Trimebutine Maleate - CAS 34140-59-5 Catalog Number: 34140-59-5 Molecular Weight: 503.54 Molecular Formula: C22H29NO5.C4H4O4 Trimebutine is an opioid receptor agonist used as spasmolytic agent abdominal pain. Description: Loperamide HCl - CAS 34552-83-5 Catalog Number: 34552-83-5 Molecular Weight: 513.5 Molecular Formula: C29H33ClN2O2.HCl Description: Loperamide HCl is an opioid-receptor agonist with an ED50 of 0.15 mg/kg. ICI 199,441 hydrochloride - CAS 115199-84-3 Catalog Number: Molecular Weight: 427.80 Molecular Formula: C21H25Cl3N2O Description: ICI 199,441 hydrochloride is the hydrochloride salt of ICI 199,441, which is a selective and highly potent κ agonist. It is 146-fold more active than U-50488 in vitro. It has a broad range of effects on the immune system ranging from inflammatory response modulation to opioid and chemokine receptor expression. It has analgesic properties. 7 / 26 www.bocsci.com SNC 162 - CAS 178803-51-5 Catalog Number: Molecular Weight: 419.61 Molecular Formula: C27H37N3O
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