Referenced in: none

Automatically associated channels: TRP , TRPV , TRPV1

Title: Synthesis of carbamide derivatives bearing tetrahydroisoquinoline moieties and biological evaluation as analgesia drugs in mice.

Authors: Qianqian Qiu, Jingjie Wang, Xin Deng, Hai Qian, Haiyan Lin, Wenlong Huang

Journal, date & volume: Arch. Pharm. (Weinheim), 2015 May , 348, 347-52

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/25824579

Abstract
Transient receptor potential vanilloid 1 (TRPV1) is a ligand-gated non-selective cation channel that is considered to be an important pain integrator. Tetrahydroisoquinoline, the prototypical antagonist of TRPV1, has a clear therapeutic potential. Here, a series of carbamide derivatives of tetrahydroisoquinoline were designed and synthesized. Preliminary biological tests suggested that the compounds I 1, I 2, and I 9 had favorable TRPV1 antagonism activity. In further studies, I 1 exhibited better antinociceptive activity than the positive control BCTC in diverse pain models. All of these results suggested that I 1 can be considered as the lead candidate for the further development of antinociceptive drugs.