Patent ID: 8349571
Filing Date: 2013-01-08
Classification: G01N

Abstract:
1. A high content screening (HCS) assay for rapidly screening one or more compounds to determine functional response or pharmacological properties thereof, comprising: i) priming a cell or cell material expressing a GPCR with a sensor for a biological response; ii) contacting the compound(s)to be tested with the primed cell or cell material or contacting a cell or cell material which has been contacted with the compound(s) with the primed cell or cell material, whereby the compound(s) is to be pharmacologically analyzed as a ligand for GPCRs; iii) simultaneously or subsequently contacting with a fluorescent agonist or a fluorescent antagonist whose pharmacological properties are known, selected from a GPCR ligand moiety linked to a fluorescent moiety via a linker at a linking site which maintains ligand activity, the fluorescent moiety comprising a red absorbing BDI dye wherein the binding of the fluorescent agonist or antagonist and its associated biological response are detected or monitored in the same cell and are distinct allowing separate readout, wherein the fluorescent agonist or fluorescent antagonist is a novel fluorescent histamine receptor agonist or fluorescent histamine receptor antagonist selected from red absorbing BODIPY derivatives of GPCR ligands wherein the ligand is selected from the formula wherein R R R wherein H Or R L.h comprises linking functionality J