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Molecular Pain

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Open Access 01-12-2013 | Research

Effect of amitriptyline on tetrodotoxin-resistant Na_v1.9 currents in nociceptive trigeminal neurons

Authors: Jingyao Liang, Xiaoyan Liu, Jianquan Zheng, Shengyuan Yu

Published in: Molecular Pain | Issue 1/2013

Abstract

Background

Amitriptyline (AMI) is tricyclic antidepressant that has been widely used to manage various chronic pains such as migraines. Its efficacy is attributed to its blockade of voltage-gated sodium channels (VGSCs). However, the effects of AMI on the tetrodotoxin-resistant (TTX-r) sodium channel Na_v1.9 currents have been unclear to present.

Results

Using a whole-cell patch clamp technique, this study showed that AMI efficiently inhibited Na_v1.9 currents in a concentration-dependent manner and had an IC₅₀ of 15.16 μM in acute isolated trigeminal ganglion (TG) neurons of the rats. 10 μM AMI significantly shifted the steady-state inactivation of Na_v1.9 channels in the hyperpolarizing direction without affecting voltage-dependent activation. Surprisingly, neither 10 nor 50 μM AMI caused a use-dependent blockade of Na_v1.9 currents elicited by 60 pulses at 1 Hz.

Conclusion

These data suggest that AMI is a state-selective blocker of Na_v1.9 channels in rat nociceptive trigeminal neurons, which likely contributes to the efficacy of AMI in treating various pains, including migraines.

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Title: Effect of amitriptyline on tetrodotoxin-resistant Nav1.9 currents in nociceptive trigeminal neurons
Authors: Jingyao Liang
Xiaoyan Liu
Jianquan Zheng
Shengyuan Yu
Publication date: 01-12-2013
Publisher: BioMed Central
Published in: Molecular Pain / Issue 1/2013
Electronic ISSN: 1744-8069
DOI: https://doi.org/10.1186/1744-8069-9-31

Keynote webinar | Spotlight on medication adherence

Springer Medicine

Effect of amitriptyline on tetrodotoxin-resistant Na_v1.9 currents in nociceptive trigeminal neurons

Abstract

Background

Results

Conclusion

Keynote webinar | Spotlight on medication adherence

Springer Medicine

Abstract

Background

Results

Conclusion

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