pH-dependent inhibition of tetrodotoxin-resistant Na(+) channels by diclofenac in rat nociceptive neurons.
作者： Michiko Nakamura , Il-Sung Jang
DOI: 10.1016/J.PNPBP.2015.07.003
关键词:
摘要: Abstract Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used for the treatment of inflammatory pain. It is well established that NSAIDs exert their analgesic effects by inhibiting cyclooxygenase to prevent production prostaglandins; however, several including diclofenac also modulate other ion channels expressed in nociceptive neurons. In this study, we investigated pH-dependent on tetrodotoxin-resistant (TTX-R) Na + rat trigeminal sensory neurons using whole-cell patch clamp technique. Diclofenac decreased peak amplitude TTX-R currents (I ) a concentration dependent manner. While had little effect voltage-activation relationship, it significantly shifted steady-state fast inactivation relationship toward hyperpolarized potentials. increased extent use-dependent inhibition currents. accelerated development and retarded recovery from channels. The were stronger at pH 6.0 than pH 7.4 most parameters tested. Considering extracellular pH falls inflamed tissues, implicated prostaglandin-mediated maintenance hyperalgesia, our findings could provide an additional under acidic conditions.
sci-hub.se 参考文章(44)
Muthukrishnan Renganathan, Theodore R. Cummins, Stephen G. Waxman, Contribution of Nav1.8 Sodium Channels to Action Potential Electrogenesis in DRG Neurons Journal of Neurophysiology. ,vol. 86, pp. 629- 640 ,(2001) , 10.1152/JN.2001.86.2.629
Laurian Vlase, Dorin Farcau, Adrian Leucuţa, Mircea Nanulescu, No effect of short term ranitidine intake on diclofenac pharmacokinetics. Romanian journal of gastroenterology. ,vol. 13, pp. 306- 308 ,(2004)
Peter W. Reeh, Kay H. Steen, Chapter 8. Tissue acidosis in nociception and pain Progress in Brain Research. ,vol. 113, pp. 143- 151 ,(1996) , 10.1016/S0079-6123(08)61085-7
N Ogata, H Tatebayashi, Kinetic analysis of two types of Na+ channels in rat dorsal root ganglia. The Journal of Physiology. ,vol. 466, pp. 9- 37 ,(1993) , 10.1113/JPHYSIOL.1993.SP019706
Peter Holzer, Acid-Sensitive Ion Channels and Receptors Handbook of experimental pharmacology. ,vol. 194, pp. 283- 332 ,(2009) , 10.1007/978-3-540-79090-7_9
Nicolas Voilley, Jan de Weille, Julien Mamet, Michel Lazdunski, Nonsteroid anti-inflammatory drugs inhibit both the activity and the inflammation-induced expression of acid-sensing ion channels in nociceptors The Journal of Neuroscience. ,vol. 21, pp. 8026- 8033 ,(2001) , 10.1523/JNEUROSCI.21-20-08026.2001
Armen N Akopian, Veronika Souslova, Steven England, Kenji Okuse, Nobukuni Ogata, Jan Ure, Andrew Smith, Bradley J Kerr, Steven B McMahon, Sue Boyce, Ray Hill, Louise C Stanfa, Anthony H Dickenson, John N Wood, None, The tetrodotoxin-resistant sodium channel SNS has a specialized function in pain pathways Nature Neuroscience. ,vol. 2, pp. 541- 548 ,(1999) , 10.1038/9195
Mohamed Chahine, Michael E. O’Leary, Regulation/Modulation of Sensory Neuron Sodium Channels Voltage Gated Sodium Channels. ,vol. 221, pp. 111- 135 ,(2014) , 10.1007/978-3-642-41588-3_6
KH Steen, PW Reeh, F Anton, HO Handwerker, Protons selectively induce lasting excitation and sensitization to mechanical stimulation of nociceptors in rat skin, in vitro The Journal of Neuroscience. ,vol. 12, pp. 86- 95 ,(1992) , 10.1523/JNEUROSCI.12-01-00086.1992
M S Roberts, P Singh, Skin permeability and local tissue concentrations of nonsteroidal anti-inflammatory drugs after topical application. Journal of Pharmacology and Experimental Therapeutics. ,vol. 268, pp. 144- 151 ,(1994)