Diphenidol inhibited sodium currents and produced spinal anesthesia

Yuk Man Leung, Bor Tsang Wu, Yu Chung Chen, Ching-Hsia Hung, Yu Wen Chen

Research output: Contribution to journalArticle

31 Citations (Scopus)

Abstract

The aim of this study was to evaluate the effect of diphenidol on blocking Na+ currents and spinal anesthesia. We used the patch-clamp method to examine if diphenidol blocked Na+ currents. Lidocaine, a common used local anesthesia, was used as control. We also evaluated the potencies and durations of diphenidol and lidocaine on spinal blockades of motor function, proprioception, and nociception in rats. Lidocaine exhibited a concentration- and state-dependent effect on tonic blockade of voltage-gated Na+ currents in mouse neuroblastoma N2A cells (IC50 of 8.1 and 138.9 μM at holding potentials of -70 and -100 mV, respectively). Diphenidol was more potent (IC50 of 0.77 and 62.6 μM at holding potentials of -70 and -100 mV, respectively). However, unlike lidocaine, block of Na+ currents by diphenidol lacked use-dependence. We also found that diphenidol acted like lidocaine and produced dose-related spinal blockades of motor function, proprioception and nociception. Although diphenidol had similar potencies of spinal anesthesia compared with lidocaine it produced a much longer duration of spinal blockades than lidocaine. Our results demonstrated that intrathecal diphenidol produced a long duration and similar potency on spinal anesthesia compared with lidocaine in rats. The anesthetic effect of diphenidol could be in part due to its blockade of Na+ currents.

Original languageEnglish
Pages (from-to)1147-1152
Number of pages6
JournalNeuropharmacology
Volume58
Issue number7
DOIs
Publication statusPublished - 2010 Jun 1

Fingerprint

Spinal Anesthesia
Lidocaine
Sodium
Proprioception
Nociception
Inhibitory Concentration 50
diphenidol
Local Anesthesia
Neuroblastoma
Anesthetics

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Cellular and Molecular Neuroscience

Cite this

Leung, Yuk Man ; Wu, Bor Tsang ; Chen, Yu Chung ; Hung, Ching-Hsia ; Chen, Yu Wen. / Diphenidol inhibited sodium currents and produced spinal anesthesia. In: Neuropharmacology. 2010 ; Vol. 58, No. 7. pp. 1147-1152.
@article{52fc6a27e9a84b9cb853a9ff1922cd53,
title = "Diphenidol inhibited sodium currents and produced spinal anesthesia",
abstract = "The aim of this study was to evaluate the effect of diphenidol on blocking Na+ currents and spinal anesthesia. We used the patch-clamp method to examine if diphenidol blocked Na+ currents. Lidocaine, a common used local anesthesia, was used as control. We also evaluated the potencies and durations of diphenidol and lidocaine on spinal blockades of motor function, proprioception, and nociception in rats. Lidocaine exhibited a concentration- and state-dependent effect on tonic blockade of voltage-gated Na+ currents in mouse neuroblastoma N2A cells (IC50 of 8.1 and 138.9 μM at holding potentials of -70 and -100 mV, respectively). Diphenidol was more potent (IC50 of 0.77 and 62.6 μM at holding potentials of -70 and -100 mV, respectively). However, unlike lidocaine, block of Na+ currents by diphenidol lacked use-dependence. We also found that diphenidol acted like lidocaine and produced dose-related spinal blockades of motor function, proprioception and nociception. Although diphenidol had similar potencies of spinal anesthesia compared with lidocaine it produced a much longer duration of spinal blockades than lidocaine. Our results demonstrated that intrathecal diphenidol produced a long duration and similar potency on spinal anesthesia compared with lidocaine in rats. The anesthetic effect of diphenidol could be in part due to its blockade of Na+ currents.",
author = "Leung, {Yuk Man} and Wu, {Bor Tsang} and Chen, {Yu Chung} and Ching-Hsia Hung and Chen, {Yu Wen}",
year = "2010",
month = "6",
day = "1",
doi = "10.1016/j.neuropharm.2010.02.007",
language = "English",
volume = "58",
pages = "1147--1152",
journal = "Neuropharmacology",
issn = "0028-3908",
publisher = "Elsevier Limited",
number = "7",

}

Diphenidol inhibited sodium currents and produced spinal anesthesia. / Leung, Yuk Man; Wu, Bor Tsang; Chen, Yu Chung; Hung, Ching-Hsia; Chen, Yu Wen.

In: Neuropharmacology, Vol. 58, No. 7, 01.06.2010, p. 1147-1152.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Diphenidol inhibited sodium currents and produced spinal anesthesia

AU - Leung, Yuk Man

AU - Wu, Bor Tsang

AU - Chen, Yu Chung

AU - Hung, Ching-Hsia

AU - Chen, Yu Wen

PY - 2010/6/1

Y1 - 2010/6/1

N2 - The aim of this study was to evaluate the effect of diphenidol on blocking Na+ currents and spinal anesthesia. We used the patch-clamp method to examine if diphenidol blocked Na+ currents. Lidocaine, a common used local anesthesia, was used as control. We also evaluated the potencies and durations of diphenidol and lidocaine on spinal blockades of motor function, proprioception, and nociception in rats. Lidocaine exhibited a concentration- and state-dependent effect on tonic blockade of voltage-gated Na+ currents in mouse neuroblastoma N2A cells (IC50 of 8.1 and 138.9 μM at holding potentials of -70 and -100 mV, respectively). Diphenidol was more potent (IC50 of 0.77 and 62.6 μM at holding potentials of -70 and -100 mV, respectively). However, unlike lidocaine, block of Na+ currents by diphenidol lacked use-dependence. We also found that diphenidol acted like lidocaine and produced dose-related spinal blockades of motor function, proprioception and nociception. Although diphenidol had similar potencies of spinal anesthesia compared with lidocaine it produced a much longer duration of spinal blockades than lidocaine. Our results demonstrated that intrathecal diphenidol produced a long duration and similar potency on spinal anesthesia compared with lidocaine in rats. The anesthetic effect of diphenidol could be in part due to its blockade of Na+ currents.

AB - The aim of this study was to evaluate the effect of diphenidol on blocking Na+ currents and spinal anesthesia. We used the patch-clamp method to examine if diphenidol blocked Na+ currents. Lidocaine, a common used local anesthesia, was used as control. We also evaluated the potencies and durations of diphenidol and lidocaine on spinal blockades of motor function, proprioception, and nociception in rats. Lidocaine exhibited a concentration- and state-dependent effect on tonic blockade of voltage-gated Na+ currents in mouse neuroblastoma N2A cells (IC50 of 8.1 and 138.9 μM at holding potentials of -70 and -100 mV, respectively). Diphenidol was more potent (IC50 of 0.77 and 62.6 μM at holding potentials of -70 and -100 mV, respectively). However, unlike lidocaine, block of Na+ currents by diphenidol lacked use-dependence. We also found that diphenidol acted like lidocaine and produced dose-related spinal blockades of motor function, proprioception and nociception. Although diphenidol had similar potencies of spinal anesthesia compared with lidocaine it produced a much longer duration of spinal blockades than lidocaine. Our results demonstrated that intrathecal diphenidol produced a long duration and similar potency on spinal anesthesia compared with lidocaine in rats. The anesthetic effect of diphenidol could be in part due to its blockade of Na+ currents.

UR - http://www.scopus.com/inward/record.url?scp=77950921891&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=77950921891&partnerID=8YFLogxK

U2 - 10.1016/j.neuropharm.2010.02.007

DO - 10.1016/j.neuropharm.2010.02.007

M3 - Article

C2 - 20176039

AN - SCOPUS:77950921891

VL - 58

SP - 1147

EP - 1152

JO - Neuropharmacology

JF - Neuropharmacology

SN - 0028-3908

IS - 7

ER -