Cholecystokinin (CCK) and gastrin belong to one family of gastrointestinal
peptides that regulate a variety of functions in the gastrointestinal tract
and in the central nervous system. On the basis of pharmacological, physio
logical and molecular studies, receptors for these peptides can be divided
into at least two different types: CCKA- and CCKB-receptors. CCKA- and CCKB
-receptors are both G-protein coupled receptors and are highly conserved be
tween species. Molecular techniques have revealed a distinct species- and t
issue-specific variation in receptor expression and pharmacology. In additi
on, previously unknown targets for CCK and gastrin such as the kidney were
identified. This review discusses the physiological functions of the hormon
es CCK and gastrin and their receptors. The molecular structure of these re
ceptors and the results of recent structure-function analysis are reviewed.