ArticleThe Journal of pharmacology and experimental therapeutics2011
Regulation of κ-opioid receptor signaling in peripheral sensory neurons in vitro and in vivo.
Article in The Journal of pharmacology and experimental therapeutics, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
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Who cites it
25 citing papers in PubMed, 33 citations in OpenAlex.
- Activation of G protein gated inwardly rectifying potassium (GIRK) channels in keratinocytes mediates peripheral kappa opioid receptor-mediated antinociception.Neuropharmacology · 2025Article
- The Utility of Peripherally Restricted Kappa-Opioid Receptor Agonists for Inhibiting Below-Level Pain After Spinal Cord Injury in Mice.Neuroscience · 2023Article
- 14-3-3γ mediates the long-term inhibition of peripheral kappa opioid receptor antinociceptive signaling by norbinaltorphimine.Neuropharmacology · 2022Article
- Age-related changes in peripheral nociceptor function.Neuropharmacology · 2022Article
- Long-term antagonism and allosteric regulation of mu opioid receptors by the novel ligand, methocinnamox.Pharmacology research & perspectives · 2021Article
- GRK2 Dictates a Functional Switch of the Peripheral Mu-Opioid Receptor.ACS chemical neuroscience · 2020Article
- Preclinical Testing of Nalfurafine as an Opioid-sparing Adjuvant that Potentiates Analgesia by the Mu Opioid Receptor-targeting Agonist Morphine.The Journal of pharmacology and experimental therapeutics · 2019Article
- Signaling characteristics and functional regulation of delta opioid-kappa opioid receptor (DOP-KOP) heteromers in peripheral sensory neurons.Neuropharmacology · 2019Article
- Dynamic Opioid Receptor Regulation in the Periphery.Molecular pharmacology · 2019Review
- Making Sense of Pharmacology: Inverse Agonism and Functional Selectivity.The international journal of neuropsychopharmacology · 2018Review
- Allosterism withinMolecular pharmacology · 2018Article
- Regulation of δ Opioid Receptor-Mediated Signaling and Antinociception in Peripheral Sensory Neurons by Arachidonic Acid-Dependent 12/15-Lipoxygenase Metabolites.The Journal of pharmacology and experimental therapeutics · 2017Article
- Novel Molecular Strategies and Targets for Opioid Drug Discovery for the Treatment of Chronic Pain.The Yale journal of biology and medicine · 2017Review
- Constitutive Desensitization of Opioid Receptors in Peripheral Sensory Neurons.The Journal of pharmacology and experimental therapeutics · 2016Article
- Biased agonists of the kappa opioid receptor suppress pain and itch without causing sedation or dysphoria.Science signaling · 2016Article
- Long-Term Reduction of Kappa Opioid Receptor Function by the Biased Ligand, Norbinaltorphimine, Requires c-Jun N-Terminal Kinase Activity and New Protein Synthesis in Peripheral Sensory Neurons.The Journal of pharmacology and experimental therapeutics · 2016Article
- Functional selectivity of kappa opioid receptor agonists in peripheral sensory neurons.The Journal of pharmacology and experimental therapeutics · 2015Article
- Dual regulation of δ-opioid receptor function by arachidonic acid metabolites in rat peripheral sensory neurons.The Journal of pharmacology and experimental therapeutics · 2015Article
- A cell-based, high-throughput homogeneous time-resolved fluorescence assay for the screening of potential κ-opioid receptor agonists.Acta pharmacologica Sinica · 2014Article
- Signalling profile differences: paliperidone versus risperidone.British journal of pharmacology · 2013Article
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
Abstract
There is considerable interest in understanding the regulation of peripheral opioid receptors to avoid central nervous system side effects associated with systemically administered opioid analgesics. Here, we investigated the regulation of the κ-opioid receptor (KOR) on rat primary sensory neurons in vitro and in a rat model of thermal allodynia. Under basal conditions, application of the KOR agonist trans-(1S,2S)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]benzeneacetamide hydrochloride hydrate (U50488) did not inhibit adenylyl cyclase (AC) activity nor release of calcitonin gene-related peptide (CGRP) in vitro and did not inhibit thermal allodynia in vivo. However, after 15-min pretreatment with bradykinin (BK), U50488 became capable of inhibiting AC activity, CGRP release, and thermal allodynia. Inhibition of AC by 5-hydroxytryptamine 1 or neuropeptide Y(1) receptor agonists and stimulation of extracellular signal-regulated kinase activity by U50488 did not require BK pretreatment. The effect of U50488 in BK-primed tissue was blocked by the KOR antagonist nor-binaltorphimine both in vitro and in vivo. The effect of BK in vitro was blocked by either indomethacin or bisindolylmaleimide, suggesting that an arachidonic acid (AA) metabolite and protein kinase C (PKC) activation mediate BK-induced regulation of the KOR system. Furthermore, the effect of U50488 in BK-treated tissue was blocked by a soluble integrin-blocking peptide (GRGDSP), but not the inactive reverse sequence peptide (GDGRSP), suggesting that, in addition to AA and PKC, RGD-binding integrins participate in the regulation of KOR signaling in response to U50488. Understanding the mechanisms by which peripheral KOR agonist efficacy is regulated may lead to improved pharmacotherapy for the treatment of pain with reduced adverse effects.
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Registered trials
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