Activation of the 5-HT4 receptor mediates widespread effects in centra
l and peripheral nervous systems. Recent developments, such as the ide
ntification of novel, selective agonists and antagonists, as well the
cloning of the receptor, have provided insights into the physiological
role of the receptor. In this article, Richard Eglen and colleagues a
ssess the emerging evidence relating to the function of the 5-HT4 rece
ptor in the brain. The cerebral distribution of the receptor, along wi
th neurochemical and electrophysiological data, suggests a role in cog
nition. The role of the receptor in modulation of dopamine transmissio
n and anxiolysis is also addressed.