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The Journal of Headache and Pain

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Open Access 01-12-2015 | Research article

Two TRPV1 receptor antagonists are effective in two different experimental models of migraine

Authors: Jannis E Meents, Jan Hoffmann, Sandra R Chaplan, Lars Neeb, Sigrid Schuh-Hofer, Alan Wickenden, Uwe Reuter

Published in: The Journal of Headache and Pain | Issue 1/2015

Abstract

Background

The capsaicin and heat responsive ion channel TRPV1 is expressed on trigeminal nociceptive neurons and has been implicated in the pathophysiology of migraine attacks. Here we investigate the efficacy of two TRPV1 channel antagonists in blocking trigeminal activation using two in vivo models of migraine.

Methods

Male Sprague–Dawley rats were used to study the effects of the TRPV1 antagonists JNJ-38893777 and JNJ-17203212 on trigeminal activation. Expression of the immediate early gene c-fos was measured following intracisternal application of inflammatory soup. In a second model, CGRP release into the external jugular vein was determined following injection of capsaicin into the carotid artery.

Results

Inflammatory up-regulation of c-fos in the trigeminal brain stem complex was dose-dependently and significantly reduced by both TRPV1 antagonists. Capsaicin-induced CGRP release was attenuated by JNJ-38893777 only in higher dosage. JNJ-17203212 was effective in all doses and fully abolished CGRP release in a time and dose-dependent manner.

Conclusion

Our results describe two TRPV1 antagonists that are effective in two in vivo models of migraine. These results suggest that TRPV1 may play a role in the pathophysiological mechanisms, which are relevant to migraine.

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Title: Two TRPV1 receptor antagonists are effective in two different experimental models of migraine
Authors: Jannis E Meents
Jan Hoffmann
Sandra R Chaplan
Lars Neeb
Sigrid Schuh-Hofer
Alan Wickenden
Uwe Reuter
Publication date: 01-12-2015
Publisher: Springer Milan
Published in: The Journal of Headache and Pain / Issue 1/2015
Print ISSN: 1129-2369
Electronic ISSN: 1129-2377
DOI: https://doi.org/10.1186/s10194-015-0539-z

Keynote webinar | Spotlight on sleep in brain health

Springer Medicine

Two TRPV1 receptor antagonists are effective in two different experimental models of migraine

Abstract

Background

Methods

Results

Conclusion

Keynote webinar | Spotlight on sleep in brain health

Springer Medicine

Abstract

Background

Methods

Results

Conclusion

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