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Opioid Receptor Antibodies

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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Agonist-induced Threonine376 phosphorylation of the µ-Opioid Receptor.
pT376-MOP (phospho-µ-Opioid Receptor Antibody)
Threonine376 (T376) is a major phosphorylation site of the µ-opioid receptor (MOP). The pT376-MOP antibody detects phosphorylation in response to high-efficacy agonists but to low-efficacy agonists or after PKC activation. T376...
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Figure 1. Agonist-induced Threonine370 phosphorylation of the µ-opioid receptor.
pT370-MOP (phospho-µ-Opioid Receptor Antibody)
Threonine370 (T370) is a major phosphorylation site of the µ-opioid receptor (MOP). The pT370-MOP antibody detects phosphorylation in response to high-efficacy agonists but to low-efficacy agonists. The pT370-MOP antibody also detects...
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KO-Validated
MOP (non-phospho), µ-Opioid Receptor Antibody
MOP (non-phospho), µ-Opioid Receptor Antibody
The non-phospho-µ-opioid receptor antibody is directed against the distal end of the carboxyl-terminal tail of mouse, rat and human MOP. It detects selectively the canonical form of MOP and none of the putative splice variants. It can be...
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Agonist-induced Threonine363 phosphorylation of the κ-Opioid Receptor.
pT363-KOP (phospho-κ-Opioid Receptor Antibody)
Threonine363 is a major phosphorylation site of the kappa-opioid receptor (KOP). The pT363-KOP antibody detects phosphorylation in response to high-efficacy agonists. T363 phosphorylation is a key regulator of KOP desensitization,...
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Agonist-induced Serine356/Threonine357 phosphorylation of the κ-Opioid Receptor.
pS356/pT357-KOP (phospho-κ-Opioid Receptor...
Serine356/Threonine357 is a major phosphorylation site of the kappa-opioid receptor (KOP). The pS356/pT357-KOP antibody detects phosphorylation in response to agonists as well as after PKC activation. S356/T357 phosphorylation is a key...
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Agonist-induced Serine351 phosphorylation of the Nociceptin/Orphanin FQ Receptor.
pS351-NOP (phospho-Nociceptin/Orphanin FQ...
Serine351 (S351) is a major phosphorylation site of the nociceptin/orphanin FQ peptide receptor (NFQ receptor, NOP). The pS351-NOP antibody detects phosphorylation in response to agonists as well as after PKC activation. S351...
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Agonist-induced Serine346 phosphorylation of the Nociceptin/Orphanin FQ Receptor.
pS346-NOP (phospho-Nociceptin/Orphanin FQ...
Serine346 (S346) is a major phosphorylation site of the nociceptin/orphanin FQ peptide receptor (NFQ receptor, NOP). The pS346-NOP antibody detects phosphorylation in response to agonists as well as after PKC activation. S346...
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Figure 1. Agonist-induced Serine375 phosphorylation of the µ-opioid receptor.
pS375-MOP (phospho-µ-Opioid Receptor Antibody)
Serine375 (S375) is the primary phosphorylation site in a hierarchical phosphorylation cascade. The pS375-MOP antibody detects phosphorylation in response to high- and low-efficacy agonists but not after PKC activation. S375...
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KO-Validated
Validation of the Nociceptin/Orphanin FQ Receptor in transfected HEK293 cells.
NOP (non-phospho), Nociceptin/Orphanin FQ...
The non-phospho-NFQ receptor (NOP) antibody is directed against the distal end of the carboxyl-terminal tail of mouse, rat and human NOP. It can be used to detect total NOP receptors in Western blots independent of phosphorylation. The...
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Validation of the κ-Opioid Receptor in transfected HEK293 cells.
KOP (non-phospho) κ-Opioid Receptor Antibody
The non-phospho-kappa-opioid receptor antibody is directed against the distal end of the carboxyl-terminal tail of mouse, rat and human KOP. It can be used to detect total KOP receptors in Western blots independent of phosphorylation.
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Agonist-induced Threonine362/Serine363 phosphorylation of the Nociceptin/Orphanin FQ Receptor.
pT362/pS363-NOP (phospho-Nociceptin/Orphanin FQ...
Threonine362/Serine363 (T362/S363) is a major phosphorylation site of the nociceptin/orphanin FQ peptide receptor (NFQ receptor, NOP). The pT362/pS363-NOP antibody detects phosphorylation in response to agonists but not after PKC...
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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 Antibodies

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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