Serotonin is a naturally occurring vasoactive substance that has diverse ca
rdiophysiological effects. These effects can be explained by the existence
of serotonin receptor subtypes which mediate different biological actions.
The vasoconstrictive actions of serotonin are mediated by 5-HT2 serotonergi
c receptors, and serotonin also amplifies the release and activities of oth
er vasoconstrictors, such as angiotensin and norepinephrine. Abnormalities
in the serotonergic system may play an important role in the pathophysiolog
y of multiple cardiovascular disease states such as systemic hypertension,
primary pulmonary hypertension and peripheral vascular disease. Selective 5
-HT2 serotonergic receptor blockers have been developed which appear to be
potent vasodilators with therapeutic potential in various cardiovascular di
sease states. The largest clinical experience has been collected with ketan
serin, and other agents in this class are being investigated. Prolongation
of the ECG QT interval with 5-HT2 serotonergic receptor blockers may pose a
potential risk with these treatments in some patients.