Fenoldopam, first approved in the Netherlands in 1992, ended by
reaching its first market, the US, for the short-term management of severe
hypertension, including malignant hypertension, in the hospital setting.
Fenoldopam can be prepared in 3 steps from the corresponding phenethylamine
and aryloxiran, the pivotal step being the cyclisation in benzazepine in acidic
medium. Fenoldopam is a potent dopamine D1 receptor agonist acting
peripherally to produce systemic vasodilation.As it does not cross the bloodbrain
barrier, it does not exert significant central dopaminergic activity.
Fenoldopam also interacts significantly with 5HT1c and 5HT2 receptors. In
comparative trials with the most common drug used for this condition in Europe,
Fenoldopam was found to be appreciably more potent than nifedipine.
Furthermore, Fenoldopam is fast acting and maintains a long-lasting
antihypertensive effect.
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Fenoldopam mesylate may be used to study dopamine D1-mediated cell signaling.
