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.
