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Synthesis of Carbamide Derivatives Bearing Tetrahydroisoquinoline Moieties and Biological Evaluation as Analgesia Drugs in Mice
Author(s) -
Qiu Qianqian,
Wang Jingjie,
Deng Xin,
Qian Hai,
Lin Haiyan,
Huang Wenlong
Publication year - 2015
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201400455
Subject(s) - trpv1 , tetrahydroisoquinoline , antagonism , chemistry , antagonist , pharmacology , analgesic , transient receptor potential channel , nociception , receptor , stereochemistry , medicine , biochemistry
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.