Cannabinoid non-cannabidiol site modulation of TRPV2 structure and function

Autor: Liying Zhang, Charlotte Simonsen, Lucie Zimova, Kaituo Wang, Lavanya Moparthi, Rachelle Gaudet, Maria Ekoff, Gunnar Nilsson, Ute A. Hellmich, Viktorie Vlachova, Pontus Gourdon, Peter M. Zygmunt

Publikováno v: Nature Communications, Vol 13, Iss 1, Pp 1-18 (2022)

TRPV2 is activated by temperature and cannabinoids. Here, the authors have used cryo-EM and electrophysiology to identify a cannabinoid binding site distinct from that of cannabidiol as a possible drug target for treatment of inflammation and immune-

Externí odkaz: https://doaj.org/article/39ad6ca731ce46dbb34893218be33cf8

Fatty acid amide hydrolase-dependent generation of antinociceptive drug metabolites acting on TRPV1 in the brain.

Autor: David A Barrière, Christophe Mallet, Anders Blomgren, Charlotte Simonsen, Laurence Daulhac, Frédéric Libert, Eric Chapuy, Monique Etienne, Edward D Högestätt, Peter M Zygmunt, Alain Eschalier

Publikováno v: PLoS ONE, Vol 8, Iss 8, p e70690 (2013)

The discovery that paracetamol is metabolized to the potent TRPV1 activator N-(4-hydroxyphenyl)-5Z,8Z,11Z,14Z-eicosatetraenamide (AM404) and that this metabolite contributes to paracetamol's antinociceptive effect in rodents via activation of TRPV1 i

Externí odkaz: https://doaj.org/article/810f4c07d97e42ef97cc02ab50bec1e6

Anticonvulsive evaluation of THIP in the murine pentylenetetrazole kindling model: lack of anticonvulsive effect of THIP despite functionalδ-subunit-containing GABAAreceptors in dentate gyrus granule cells

Autor: Suzanne L. Hansen, Kasper Sønderskov, Uffe Kristiansen, Charlotte Simonsen, Nadia Lybøl von Schoubye, Alissa Kloppenburg, Kim Boddum

Publikováno v: Pharmacology Research & Perspectives
Simonsen, C, Boddum, K, von Schoubye, N L, Kloppenburg, A, Sønderskov, K, Hansen, S L & Kristiansen, U 2017, ' Anticonvulsive evaluation of THIP in the murine pentylenetetrazole kindling model : lack of anticonvulsive effect of THIP despite functional δ-subunit-containing GABAA receptors in dentate gyrus granule cells ', Pharmacology Research & Perspectives, vol. 5, no. 4, e00322 . https://doi.org/10.1002/prp2.322

THIP (4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol) is a GABAA receptor agonist with varying potencies and efficacies at γ-subunit-containing receptors. More importantly, THIP acts as a selective superagonist at δ-subunit-containing receptors (δ

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::595aea0e2d0a78bb7a244883ae996143
https://doi.org/10.1002/prp2.322

Fatty acid amide hydrolase-dependent generation of antinociceptive drug metabolites acting on TRPV1 in the brain

Autor: Christophe Mallet, Peter M. Zygmunt, Eric Chapuy, Charlotte Simonsen, Monique Etienne, Alain Eschalier, Anders Blomgren, David André Barrière, Frédéric Libert, Edward D. Högestätt, Laurence Daulhac

Publikováno v: PLoS ONE
PLoS ONE, Vol 8, Iss 8, p e70690 (2013)
PLoS ONE; 8(8), no e70690 (2013)

The discovery that paracetamol is metabolized to the potent TRPV1 activator N-(4-hydroxyphenyl)-5Z, 8Z, 11Z, 14Z-eicosatetraenamide (AM404) and that this metabolite contributes to paracetamol's antinociceptive effect in rodents via activation of TRPV

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7cb278bf0ec9e522652f8e2919459171
https://pubmed.ncbi.nlm.nih.gov/23940628

Excitability changes related to GABAA receptor plasticity during pregnancy

Autor: Istvan Mody, Isabella Ferando, Jamie Maguire, Charlotte Simonsen

Publikováno v: The Journal of neuroscience : the official journal of the Society for Neuroscience. 29(30)

Alterations in GABAAreceptor (GABAAR) expression and function, similar to those we described previously during pregnancy in the mouse dentate gyrus, may also occur in other brain regions. Here we show, using immunohistochemical techniques, a decrease

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6881f545c46df5c1a2a054706b5049df
https://pubmed.ncbi.nlm.nih.gov/19641122