Identification of the first surrogate agonists for the G protein-coupled receptor GPR132

Abstract

We report the first pharmacological tool agonist for in vitro characterization of the orphan receptor GPR132, preliminary structure–activity relationships based on 32 analogs and a suggested binding mode from docking.M.A.S. was supported by a research scholarship from the Drug Research Academy and Novo Nordisk A/S. D.E.G. and H.B.-O. gratefully acknowledge financial support by the Carlsberg Foundation. D.E.G. and D.S.P. gratefully acknowledges financial support by the Lundbeck Foundation. Nils Nyberg is acknowledged for help with NMR spectroscopy. NMR equipment used in this work was purchased via a grant from The Lundbeck Foundation (R77-A6742).This is the accepted manuscript. The final version is available at http://pubs.rsc.org/en/Content/ArticleLanding/2015/RA/c5ra04804d#!divAbstract