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This image shows the crystal
structure of serotonin receptor (5HT2B) in complex with ergotamine. The
background shows chemical structures of fenfluramine and phentermine
(fen-phen), a popular anti-obesity treatment later withdrawn due to valvular
heart disease and pulmonary hypertension. Fenfluramine activation of 5HT2B
receptors was shown to be the culprit of these serious cardiovascular problems.
A heart structure crossed by "Rx" highlights the troubled history of
fen-phen. Since then, many drugs have been shown to have the same side-effect
in humans including drugs used in treating migraine headaches (ergotamine,
dihydroergotamine), Parkinson's Disease (cabergoline, pergolide) and other
disorders (Benfluorex). (Image courtesy of the Stevens lab.)