Polymorphisms in G-protein-coupled receptors can alter drug affinity and/or
a activity. In addition, genetic differences in amino acid sequences can i
nduce ligand-independent signaling, which in turn can lead to disease. With
growing efforts in the field of pharmacogenomics, it is anticipated that p
olymorphism-inducer alterations in drug and/or receptor function will be a
focus of increasing concern during the course of future drug-development ef
forts. In this review, the spectrum of pharmacological consequences that re
sult from polymorphisms in the cholecystokinin CCK2 receptor will be discus
sed, thereby illustrating emerging themes in pharmacogenomics.