ArticleRegional anesthesia and pain medicine
The κ-opioid receptor agonist U-50488 blocks Ca2+ channels in a voltage- and G protein-independent manner in sensory neurons.
Article in Regional anesthesia and pain medicine. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed, 14 citations in OpenAlex.
- κ-Opioid Receptor Agonists as Robust Pain-Modulating Agents: Mechanisms and Therapeutic Potential in Pain Modulation.Journal of clinical medicine · 2025Review
- Opioid Receptors Modulate Inhibition within the Prefrontal Cortex through Dissociable Cellular and Molecular Mechanisms.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2025Article
- CoexpressedMolecular pharmacology · 2024Article
- Characterization of the Presence and Function of Platelet Opioid Receptors.ACS measurement science au · 2022Article
- Evaluation of Antinociceptive Effects of Chitosan-Coated Liposomes Entrapping the Selective Kappa Opioid Receptor Agonist U50,488 in Mice.Medicina (Kaunas, Lithuania) · 2021Article
- A 3.7 kb fragment of the mouse Scn10a gene promoter directs neural crest but not placodal lineage EGFP expression in a transgenic animal.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2015Article
- The differential effects of a selective kappa-opioid receptor agonist, U50488, in guinea pig heart tissues.BioMed research international · 2015Article
- Alteration of the mu opioid receptor: Ca2+ channel signaling pathway in a subset of rat sensory neurons following chronic femoral artery occlusion.Journal of neurophysiology · 2014Article
- Identification of CaV channel types expressed in muscle afferent neurons.Journal of neurophysiology · 2013Article
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2 authors at 1 institution in 1 country.
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Abstract
BACKGROUND AND
objectivesκ-Opioid receptor (κ-OR) activation is known to play a role in analgesia and central sedation. The purpose of the present study was to examine the effect of the κ-OR agonist, U-50488 (an arylacetamide), on Ca channel currents and the signaling proteins involved in acutely isolated rat dorsal root ganglion (DRG) neurons expressing the putative promoter region of the tetrodotoxin-resistant Na channel (NaV 1.8) that is known to be involved in pain transmission.
methodsAcutely isolated rat DRG neurons were transfected with cDNA coding for enhanced green fluorescent protein (EGFP), whose expression is driven by the NaV 1.8 promoter region. Thereafter, the whole-cell variant of the patch-clamp technique was used to record Ca channel currents in neurons expressing EGFP.
resultsExposure of EGFP-expressing DRG neurons to U-50488 (0.3-40 μM) led to voltage-independent inhibition of the Ca channel currents. The modulation of the Ca currents did not appear to be mediated by the Gα protein subfamilies: Gαi/o, Gαs, Gαq/11, Gα14, and Gαz. Furthermore, dialysis of the hydrolysis-resistant GDP analog, GDP-β-S (1 mM), did not affect the U-50488-mediated blocking effect, ruling out involvement of other G protein subunits. Finally, U-50488 (20 μM) blocked Ca channels heterologously expressed in HeLa cells that do not express κ-OR.
conclusionThese results suggest that the antinociceptive actions mediated by U-50488 are likely due to both a direct block of Ca channels in sensory neurons as well as G protein modulation of Ca currents via κ-OR-expressing neurons.
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