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The Effect of &kgr;-Opioid Receptor Agonists on Tetrodotoxin-Resistant Sodium Channels in Primary Sensory Neurons

The Effect of &kgr;-Opioid Receptor Agonists on Tetrodotoxin-Resistant Sodium Channels in Primary... The Effect of -Opioid Receptor Agonists on Tetrodotoxin-Resistant Sodium Channels in Primary Sensory Neurons BACKGROUND: A non-opioid receptor-mediated inhibition of sodium channels in Xin Su, MD dorsal root ganglia (DRGs) by -opioid receptor agonists (-ORAs) has been reported to contribute to the antinociceptive actions in animals and humans. In this Neil A. Castle, PhD study, we examined structurally diverse -ORAs for their abilities to inhibit tetrodotoxin-resistant (TTX-r) sodium channels in adult rat DRGs. Brett Antonio, BS METHODS: Whole-cell recordings of TTX-r sodium currents were performed on cultured adult rat DRGs. Structurally diverse -ORAs were studied for their Rosemarie Roeloffs, PhD abilities to inhibit TTX-r sodium channels. RESULTS: The racemic -ORA, ()U50,488, inhibited TTX-r sodium currents in a James B. Thomas, PhD voltage-dependent manner, yielding IC values of 49 and 8 M, at prepulse potentials of 100 and 40 mV, respectively. Furthermore, we found that both the -ORA U50,488 active enantiomer 1S,2S U50,488 and the inactive enantiomer 1R,2R Douglas S. Krafte, PhD U50,488 were equally potent inhibitors of TTX-r sodium currents. Structurally related -ORAs, such as BRL 52537 and ICI 199,441 also inhibited TTX-r sodium Mark L. Chapman, PhD currents. However, sodium channel inhibition and -opioid receptor agonism have a http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Anesthesia & Analgesia Wolters Kluwer Health

The Effect of &kgr;-Opioid Receptor Agonists on Tetrodotoxin-Resistant Sodium Channels in Primary Sensory Neurons

Anesthesia & Analgesia , Volume 109 (2) – Aug 1, 2009

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References (48)

ISSN
0003-2999
eISSN
1526-7598
DOI
10.1213/ane.0b013e3181a909a4
pmid
19608841
Publisher site
See Article on Publisher Site

Abstract

The Effect of -Opioid Receptor Agonists on Tetrodotoxin-Resistant Sodium Channels in Primary Sensory Neurons BACKGROUND: A non-opioid receptor-mediated inhibition of sodium channels in Xin Su, MD dorsal root ganglia (DRGs) by -opioid receptor agonists (-ORAs) has been reported to contribute to the antinociceptive actions in animals and humans. In this Neil A. Castle, PhD study, we examined structurally diverse -ORAs for their abilities to inhibit tetrodotoxin-resistant (TTX-r) sodium channels in adult rat DRGs. Brett Antonio, BS METHODS: Whole-cell recordings of TTX-r sodium currents were performed on cultured adult rat DRGs. Structurally diverse -ORAs were studied for their Rosemarie Roeloffs, PhD abilities to inhibit TTX-r sodium channels. RESULTS: The racemic -ORA, ()U50,488, inhibited TTX-r sodium currents in a James B. Thomas, PhD voltage-dependent manner, yielding IC values of 49 and 8 M, at prepulse potentials of 100 and 40 mV, respectively. Furthermore, we found that both the -ORA U50,488 active enantiomer 1S,2S U50,488 and the inactive enantiomer 1R,2R Douglas S. Krafte, PhD U50,488 were equally potent inhibitors of TTX-r sodium currents. Structurally related -ORAs, such as BRL 52537 and ICI 199,441 also inhibited TTX-r sodium Mark L. Chapman, PhD currents. However, sodium channel inhibition and -opioid receptor agonism have a

Journal

Anesthesia & AnalgesiaWolters Kluwer Health

Published: Aug 1, 2009

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