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Opioid Receptor Phosphorylation Assays

Opioid receptors are activated by a variety of endogenous peptides including enkephalins, β-endorphin, dynorphins or nociceptin/orphanin FQ (N/OFQ) that mediate primarily inhibitory functions in the central and peripheral nervous system. The opioid receptor family consists of four members designated μ-opioid receptor (mu-opioid receptor, MOP), δ-opioid receptor (delta-opioid receptor, DOP), κ-opioid receptor (kappa-opioid receptor, KOP), N/OFQ receptor (NOP). All four opioid receptors can mediate analgesic effects, which are accompanied by receptor-specific side effects. MOP is the pharmacological target for many clinically-used analgesics including morphine, oxycodone, fentanyl and methadone. The utility of µ-analgesics is limited by sever side effects such as respiratory depression, constipation and addiction. Specific side-effects induced by DOP, KOP and NOP include seizures, dysphoria and sedation, respectively. One strategy for the development of safer analgesics with fewer side effects is the development of drugs that target multiple opioid receptors. An alternative approach is the development of biased opioid analgesics.

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OD signals in pT376-MOP Phosphorylation Assay
pT376-MOP Phosphorylation Assay Kit
The pT376-MOP Phosphorylation Assay Kit allows determination of MOP Phosphorylation in 96-well plates without the need for Western blot analysis.
600.00 € *
Details
NEW
OD signals in pT370-MOP Phosphorylation Assay
pT370-MOP Phosphorylation Assay Kit
The pT370-MOP Phosphorylation Assay Kit allows determination of MOP Phosphorylation in 96-well plates without the need for Western blot analysis.
600.00 € *
Details
NEW
OD signals in pS375-MOP Phosphorylation Assay
pS375-MOP Phosphorylation Assay Kit
The pS375-MOP Phosphorylation Assay Kit allows determination of MOP Phosphorylation in 96-well plates without the need for Western blot analysis.
600.00 € *
Details
NEW
OD signals in pT379-MOP Phosphorylation Assay
pT379-MOP Phosphorylation Assay Kit
The pT379-MOP Phosphorylation Assay Kit allows determination of MOP Phosphorylation in 96-well plates without the need for Western blot analysis.
600.00 € *
Details

For more information on opioid receptor pharmacology please refer to IUPHAR database. For further reading refer to:

Günther T, Dasgupta P, Mann A, Miess E, Kliewer A, Fritzwanker S, Steinborn R, Schulz S. Targeting multiple opioid receptors - improved analgesics with reduced side effects? Br J Pharmacol. 2018 Jul;175(14):2857-2868. doi: 10.1111/bph.13809. Epub 2017 May 26. Review. PubMed PMID: 28378462; PubMed Central PMCID: PMC6016677.

Williams JT, Ingram SL, Henderson G, Chavkin C, von Zastrow M, Schulz S, Koch T, Evans CJ, Christie MJ. Regulation of μ-opioid receptors: desensitization, phosphorylation, internalization, and tolerance. Pharmacol Rev. 2013 Jan 15;65(1):223-54. doi: 10.1124/pr.112.005942. Print 2013 Jan. Review. PubMed PMID: 23321159; PubMed Central PMCID: PMC3565916.

Gendron L, Cahill CM, von Zastrow M, Schiller PW, Pineyro G. Molecular Pharmacology of δ-Opioid Receptors. Pharmacol Rev. 2016 Jul;68(3):631-700. doi: 10.1124/pr.114.008979. Review. PubMed PMID: 27343248; PubMed Central PMCID: PMC4931872.

Toll L, Bruchas MR, Calo' G, Cox BM, Zaveri NT. Nociceptin/Orphanin FQ Receptor Structure, Signaling, Ligands, Functions, and Interactions with Opioid Systems. Pharmacol Rev. 2016 Apr;68(2):419-57. doi: 10.1124/pr.114.009209. Epub 2016 Mar 8. Review. PubMed PMID: 26956246; PubMed Central PMCID: PMC4813427.

For more information on opioid receptor pharmacology please refer to IUPHAR database. For further reading refer to: Günther T, Dasgupta P, Mann A, Miess E, Kliewer A, Fritzwanker S, Steinborn... read more »
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Opioid Receptor Phosphorylation Assays

For more information on opioid receptor pharmacology please refer to IUPHAR database. For further reading refer to:

Günther T, Dasgupta P, Mann A, Miess E, Kliewer A, Fritzwanker S, Steinborn R, Schulz S. Targeting multiple opioid receptors - improved analgesics with reduced side effects? Br J Pharmacol. 2018 Jul;175(14):2857-2868. doi: 10.1111/bph.13809. Epub 2017 May 26. Review. PubMed PMID: 28378462; PubMed Central PMCID: PMC6016677.

Williams JT, Ingram SL, Henderson G, Chavkin C, von Zastrow M, Schulz S, Koch T, Evans CJ, Christie MJ. Regulation of μ-opioid receptors: desensitization, phosphorylation, internalization, and tolerance. Pharmacol Rev. 2013 Jan 15;65(1):223-54. doi: 10.1124/pr.112.005942. Print 2013 Jan. Review. PubMed PMID: 23321159; PubMed Central PMCID: PMC3565916.

Gendron L, Cahill CM, von Zastrow M, Schiller PW, Pineyro G. Molecular Pharmacology of δ-Opioid Receptors. Pharmacol Rev. 2016 Jul;68(3):631-700. doi: 10.1124/pr.114.008979. Review. PubMed PMID: 27343248; PubMed Central PMCID: PMC4931872.

Toll L, Bruchas MR, Calo' G, Cox BM, Zaveri NT. Nociceptin/Orphanin FQ Receptor Structure, Signaling, Ligands, Functions, and Interactions with Opioid Systems. Pharmacol Rev. 2016 Apr;68(2):419-57. doi: 10.1124/pr.114.009209. Epub 2016 Mar 8. Review. PubMed PMID: 26956246; PubMed Central PMCID: PMC4813427.

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