A comprehensive study on the putative Î´-opioid receptor (sub)types using the highly selective Î´-antagonist, Tyr-Tic-(2S,3R)-Î²-MePhe-Phe-OH

Article ID	Journal	Published Year	Pages	File Type
10958303	Neurochemistry International	2011	10 Pages	PDF

Abstract

âº Selective ligands are needed for identifying receptors and their functions. âº Tyr-Tic-(2S,3R)-Î²-MePhe-Phe-OH is a highly potent and selective Î´-opioid antagonist in murine brain and DOR-CHO cells. âº It behaved as a Î´1-opioid receptor antagonist in the antinociception assay in mouse after i.t. administration. âº Subtypes of Î´-opioid receptors were not detected in vitro in ligand binding, receptor autoradiography and functional assays.

Keywords

IC50 7-benzylidenenaltrexone DOR-1 BNTX DSLET Deltorphin II DPDPE TRIS Emax TIC Bmax ED50 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid [35S]GTPγS δ-Opioid receptor subtypes δ-Opioid receptor i.t.intrathecal Receptor density equilibrium dissociation constant GDP Inhibitory constant DADLE Mouse brain TIPP