Referenced in: none

Automatically associated channels: TRP , TRPV , TRPV1

Title: TRPV1 modulators: Synthesis and in vitro evaluation of 1-heteroaryl piperidinecarboxamide and piperazinylurea derivatives.

Authors: Cenzo Congiu, Valentina Onnis, Gianfranco Balboni, Aniello Schiano-Moriello, Vincenzo Di Marzo, Luciano De Petrocellis

Journal, date & volume: Eur J Med Chem, 2015 Jul 15 , 100, 129-38

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/26079089

Abstract
A series of new 1-heteroaryl piperidinecarboxamide and piperazinylurea derivatives was synthesized and evaluated as TRPV1 modulators in a Ca(2+) channel assay in HEK-293 cells overexpressing the human recombinant TRPV1 channel. Structural variations in the putative key portions of the molecules afforded several compounds endowed with agonist and/or antagonist/desensitizing activity at low micromolar concentration. As promising examples from this series, the piperidine-3-carboxamide derivative 31 exerts agonist/desensitizing activity at low micromolar concentration, while piperazinylurea derivatives 39 and 41 act as antagonists with sub-micromolar potency.