A developing trend in exploring the sites at which drugs act is to use mole
cular rather than chemical agents to alter receptors, intracellular signall
ing mechanisms or gene expression. The 5-HT neurotransmission system is tar
geted by drugs useful in many behavioural disorders, including anxiety, dep
ression, psychosis and eating disorders. It also regulates many physiologic
al functions and provides some examples of the potential use of these new m
olecular approaches. This article reviews the progress made in the molecula
r manipulation of 5-HT receptors and discusses the potential of such tools
for the treatment of diseases associated with the 5-HT transmission system.