2. Academic Validation
  3. Effect of acyclic monoterpene alcohols and their derivatives on TRP channels

Effect of acyclic monoterpene alcohols and their derivatives on TRP channels

  • Bioorg Med Chem Lett. 2014 Dec 1;24(23):5507-11. doi: 10.1016/j.bmcl.2014.10.012.
Giorgio Ortar 1,  Aniello Schiano Moriello 2,  Enrico Morera 3,  Marianna Nalli 3,  Vincenzo Di Marzo 2,  Luciano De Petrocellis 4
Affiliations

Affiliations

  • 1 Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, piazzale Aldo Moro 5, 00185 Roma, Italy. Electronic address: giorgio.ortar@uniroma1.it.
  • 2 Endocannabinoid Research Group, Istituto di Chimica Biomolecolare, Consiglio Nazionale delle Ricerche, via dei Campi Flegrei 34, 80078 Pozzuoli (Napoli), Italy.
  • 3 Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, piazzale Aldo Moro 5, 00185 Roma, Italy.
  • 4 Endocannabinoid Research Group, Istituto di Chimica Biomolecolare, Consiglio Nazionale delle Ricerche, via dei Campi Flegrei 34, 80078 Pozzuoli (Napoli), Italy. Electronic address: l.depetrocellis@icb.cnr.it.
PMID: 25455494 DOI: 10.1016/j.bmcl.2014.10.012
Abstract

A series of thirty-six geraniol, nerol, citronellol, geranylamine, and nerylamine derivatives was synthesized and tested on TRPA1, TRPM8, and TRPV1 channels. Most of them acted as strong modulators of TRPA1 channels with EC50 and/or IC50 values <1 μM. None was able to significantly activate TRPM8 channels, while thirteen of them behaved as 'true' TRPM8 antagonists. Little or no effect was generally observed on TRPV1 channels. Some of the compounds examined, that is, compounds 1d,g,n, 2c,d,h,i,o, 3b,e exhibited an appreciable selectivity for TRPA1 subtype.

Keywords

Acyclic monoterpene alcohols; TRPA1; TRPM8; TRPV1; Transient receptor potential channels.

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