Block of sodium currents in rat dorsal root ganglion neurons by diphenhydramine
- Authors
- Kim, Yon Sang; Shin, Yong Kyoo; Lee, Chung-Soo; Song, Jin-Ho
- Issue Date
- Oct-2000
- Publisher
- ELSEVIER SCIENCE BV
- Keywords
- diphenhydramine; local anesthetic; sodium channel; dorsal root ganglion; patch clamp
- Citation
- BRAIN RESEARCH, v.881, no.2, pp 190 - 198
- Pages
- 9
- Journal Title
- BRAIN RESEARCH
- Volume
- 881
- Number
- 2
- Start Page
- 190
- End Page
- 198
- URI
- https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/25270
- DOI
- 10.1016/S0006-8993(00)02860-2
- ISSN
- 0006-8993
1872-6240
- Abstract
- To elucidate the local anesthetic mechanism of diphenhydramine, its effects on tetrodotoxin-sensitive (TTX-S) and tetrodotoxin-resistant (TTX-R) sodium currents in rat dorsal root ganglion (DRG) neurons were examined by the whole-cell voltage clamp method. Diphenhydramine blocked TTX-S and TTX-R sodium currents with K-d values of 48 and 86 muM, respectively, at a holding potential of -80 mV. It shifted the conductance-voltage curve for TTX-S sodium currents in the depolarizing direction but had little effect on that for TTX-R sodium currents. Diphenhydramine caused a shift of the steady-state inactivation curve for both types of sodium currents in the hyperpolarizing direction. The time-dependent inactivation became faster and the recovery from the inactivation was slowed by diphenhydramine in both types of sodium currents. Diphenhydramine produced a profound use-dependent block when the cells were repeatedly stimulated with high-frequency depolarizing pulses. The use-dependent block was more pronounced in TTX-R sodium currents. The results show that diphenhydramine blocks sodium channels of sensory neurons similarly to local anesthetics. (C) 2000 Elsevier Science B.V. All rights reserved.
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