G-protein-coupled receptors (GPCRs) are integral membrane proteins of
great pharmacological importance owing to their central role in the re
gulation of cellular responses to external stimuli. Heterologous expre
ssion systems have been used to explore ligand binding, G protein and
effector coupling, and structural aspects of the receptors, GPCRs can
be expressed in a functional form in all expression systems, but with
varying degrees of success because of differences in receptor and host
cell characteristics. This article will discuss aspects related to th
e choice and suitability of expression systems for the intended analys
is of GPCR properties.