The present invention relates to methods of identifying whether a
candidate compound is a modulator of a G protein-coupled receptor (GPCR).
In preferred embodiments, the GPCR is human. In other preferred
embodiments, the GPCR is coupled to Gi and lowers the level of
intracellular cAMP. In other preferred embodiments, the GPCR is expressed
endogenously by adipocytes. In further preferred embodiments, the GPCR
inhibits intracellular lipolysis. In other further preferred embodiments,
the GPCR is a nicotinic acid receptor. The present invention also relates
to methods of using a modulator of said GPCR. Preferred modulator is
agonist. Agonists of the invention are useful as therapeutic agents for
the prevention or treatment of metabolic-related disorders, including
dyslipidemia, atherosclerosis, coronary heart disease, stroke, insulin
resistance, and type 2 diabetes.