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== Implication of TRPV1 in the treatment of pain == | == Implication of TRPV1 in the treatment of pain == | ||
In 2011 Qutenza (NeurogesX) patch containing 8% of capsaicin has been | Capsaicin stimulates and desensitizes several receptors from the A(delta) and C fibers. This phenomenon will release inflammatory neuropeptides. | ||
Capsaicin assists the entry of Ca2+ in the neuron by a nonspecific membrane. | |||
TRPV1 can be activated by heat and voltage variation. | |||
This receptor exists under 3 different forms and ethanol is able to activate this receptor. | |||
In 2011 Qutenza (NeurogesX) patch containing 8% of capsaicin has been marketed in France and indicated in the [https://en.wikipedia.org/wiki/Neuropathic_pain neuropathic pain]. | |||
The absorption through the skin of these creams generated partial desensitization of the nerve endings. This is the cause of a decrease in painful sensations.<ref name="TRPV1 dans les neuropathies douloureuses - Des modèles animaux aux perspectives thérapeutiques">A. Danigo, L. Magy, et C. Demiot, « TRPV1 dans les neuropathies douloureuses - Des modèles animaux aux perspectives thérapeutiques », médecine/sciences, vol. 29, no 6‑7, Art. no 6‑7, juin 2013, doi: 10.1051/medsci/2013296012.</ref> | The absorption through the skin of these creams generated partial desensitization of the nerve endings. This is the cause of a decrease in painful sensations.<ref name="TRPV1 dans les neuropathies douloureuses - Des modèles animaux aux perspectives thérapeutiques">A. Danigo, L. Magy, et C. Demiot, « TRPV1 dans les neuropathies douloureuses - Des modèles animaux aux perspectives thérapeutiques », médecine/sciences, vol. 29, no 6‑7, Art. no 6‑7, juin 2013, doi: 10.1051/medsci/2013296012.</ref> | ||
[https://en.wikipedia.org/wiki/Capsazepine] is a synthetic competitive antagonist of this receptor which is currently used to study TRPV1 function. | |||
Many laboratories are conducting clinical studies on oral TRPV1 antagonists: GlaxoSmithKline, Amgen, | Many laboratories are conducting clinical studies on oral TRPV1 antagonists: [https://fr.wikipedia.org/wiki/GlaxoSmithKline], [https://en.wikipedia.org/wiki/Amgen], [https://en.wikipedia.org/wiki/Merck_%26_Co.]-Neurogen, [https://en.wikipedia.org/wiki/Abbott_Laboratories], [https://en.wikipedia.org/wiki/Eli_Lilly_and_Company], [https://en.wikipedia.org/wiki/AstraZeneca] and [https://en.wikipedia.org/wiki/Japan_Tobacco]. Nowadays at least seven orally active TRPV1 antagonist substances successfully went for clinical development and the laboratories cited before all completed phase I trials . However some of them have stopped their researches at phase II trials by unknown reason as GlaxoSmithKline <ref name="SB-705498">The National Center for Advancing Translational Sciences «SB-705498 » , https://drugs.ncats.io/drug/T74V9O0Y2W, (Consulté le: déc. 29, 2021)</ref> | ||
with the antagonist SB-705498 or Lilly with the antagonist GRC 6211 <ref name="Further Clinical Trials in Osteoarthritis Pain Suspended for GRC 6211">Calisha Myers, 24 oct. 2008, «Further Clinical Trials in Osteoarthritis Pain Suspended for GRC 6211 » , https://www.fiercebiotech.com/biotech/further-clinical-trials-osteoarthritis-pain-suspended-for-grc-6211, (Consulté le: déc. 29, 2021)</ref> | |||
The research on the antagonists of TRPV1 remains encouraging. <ref name="TRPV1 antagonists that cause hypothermia, instead of hyperthermia, in rodents: Compounds’ pharmacological profiles, in vivo targets, thermoeffectors recruited and implications for drug development">A. Garami,E. Pakai,H. A. McDonald,R. M. Reilly,A. Gomtsyan,J. J. Corrigan,E. Pinter,D. X. D. Zhu,S. G. Lehto,N. R. Gavva,P. R. Kym,A. A. Romanovsky, 20 jan. 2018, «TRPV1 antagonists that cause hypothermia, instead of hyperthermia, in rodents: Compounds’ pharmacological profiles, in vivo targets, thermoeffectors recruited and implications for drug development » ,https://onlinelibrary.wiley.com/doi/full/10.1111/apha.13038 | |||
, (Consulté le: déc. 29, 2021)</ref> | |||
