Literature DB >> 22503249

Modulation of thermo-transient receptor potential (thermo-TRP) channels by thymol-based compounds.

Giorgio Ortar1, Ludovica Morera, Aniello Schiano Moriello, Enrico Morera, Marianna Nalli, Vincenzo Di Marzo, Luciano De Petrocellis.   

Abstract

A series of thirty-three thymol, p-cymene-3-carboxylic acid, and 3-amino-p-cymene derivatives was synthesized and tested on TRPA1, TRPM8, and TRPV3 channels. Most of them acted as strong modulators of TRPA1, TRPM8, and TRPV3 channels with EC(50) and/or IC(50) values distinctly lower than those of thymol and related monoterpenoids. Some of the compounds examined, that is, 3c, 4e, f, 6b, and 8b exhibited an appreciable subtype-selectivity.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID: 22503249     DOI: 10.1016/j.bmcl.2012.03.055

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  7 in total

1.  Thymol inhibits oral squamous cell carcinoma growth via mitochondria-mediated apoptosis.

Authors:  Jorge J De La Chapa; Prajjal Kanti Singha; Debbie R Lee; Cara B Gonzales
Journal:  J Oral Pathol Med       Date:  2018-06-09       Impact factor: 4.253

2.  Pharmacological profiling of the TRPV3 channel in recombinant and native assays.

Authors:  Olivera Grubisha; Adrian J Mogg; Jessica L Sorge; Laura-Jayne Ball; Helen Sanger; Cara L A Ruble; Elizabeth A Folly; Daniel Ursu; Lisa M Broad
Journal:  Br J Pharmacol       Date:  2014-05       Impact factor: 8.739

Review 3.  Differential Activation of TRP Channels in the Adult Rat Spinal Substantia Gelatinosa by Stereoisomers of Plant-Derived Chemicals.

Authors:  Eiichi Kumamoto; Tsugumi Fujita
Journal:  Pharmaceuticals (Basel)       Date:  2016-07-28

4.  Effects of Lippia sidoides essential oil, thymol, p-cymene, myrcene and caryophyllene on rat sciatic nerve excitability.

Authors:  R Barbosa; Y Cruz-Mendes; K S Silva-Alves; F W Ferreira-da-Silva; N M Ribeiro; L P Morais; J H Leal-Cardoso
Journal:  Braz J Med Biol Res       Date:  2017-10-19       Impact factor: 2.590

Review 5.  TRP channels and monoterpenes: Past and current leads on analgesic properties.

Authors:  Hugues Petitjean; Eléa Héberlé; Louis Hilfiger; Olga Łapieś; Guillaume Rodrigue; Alexandre Charlet
Journal:  Front Mol Neurosci       Date:  2022-07-29       Impact factor: 6.261

6.  The TRPA1 Agonist Cinnamaldehyde Induces the Secretion of HCO3- by the Porcine Colon.

Authors:  David Manneck; Gisela Manz; Hannah-Sophie Braun; Julia Rosendahl; Friederike Stumpff
Journal:  Int J Mol Sci       Date:  2021-05-14       Impact factor: 5.923

Review 7.  TRP Channels as Drug Targets to Relieve Itch.

Authors:  Zili Xie; Hongzhen Hu
Journal:  Pharmaceuticals (Basel)       Date:  2018-10-06
  7 in total

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