Referenced in: none

Automatically associated channels: TRP , TRPV , TRPV1

Title: TRPV1 modulators: structure-activity relationships using a rational combinatorial approach.

Authors: Laura Zaccaro, M Teresa García-López, Rosario González-Muñiz, Carolina García-Martínez, Antonio Ferrer-Montiel, Fernando Albericio, Miriam Royo

Journal, date & volume: Bioorg. Med. Chem. Lett., 2011 Jun 15 , 21, 3541-5

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/21612926

Abstract
A discrete library of linear and hydantoin-containing dipeptide derivatives, based on the Lys-Trp(Nps) scaffold, was prepared by solid-phase synthesis. SAR studies indicated that potency for TRPV1 blockade and selectivity towards NMDA is mainly dictated by the side-chain length and the basic nature of α, ω-groups in the N-terminal residue. The 2-Nps moiety at position 2 of Trp indole ring is preferred over the 2-pyridine one.