Synthesis of Novel Analogs
of Cabergoline: Improving
Cardiovascular Safety by Removing 5‑HT<sub>2B</sub> Receptor
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Abstract
The dopamine agonist cabergoline has been used to treat
prolactinomas,
Parkinson’s disease, Cushing’s disease, and sexual dysfunction.
However, its clinical use was severely curtailed when it was found
that patients taking cabergoline had an increased risk of developing
cardiac-valve regurgitation. This potentially life-threatening condition
has been associated with drugs, such as cabergoline, that are 5-HT<sub>2B</sub> receptor agonists. We prepared analogs of cabergoline and
have identified several that have limited or no agonism at the 5-HT<sub>2B</sub> receptor