Donitriptan


Donitriptan is a triptan drug which was investigated as an antimigraine agent but was never marketed. It acts as a selective serotonin 5-HT1B and 5-HT1D receptor agonist. The drug reached phase 2 clinical trials prior to the discontinuation of its development.

Pharmacology

Donitriptan acts as a high-affinity, high-efficacy near-full agonist of the serotonin 5-HT1B and 5-HT1D receptors, and is among the most potent of the triptan series of drugs. It is also notable and unique among most of the triptans in being a potent serotonin 5-HT2A receptor agonist, albeit with about one or two orders of magnitude lower activational potency than at the serotonin 5-HT1B and 5-HT1D receptors.

Chemistry

Donitriptan is a tryptamine derivative, a 5-substituted derivative of tryptamine and 5-methoxytryptamine, and an analogue of the psychedelic drugs dimethyltryptamine and 5-MeO-DMT.
The predicted log P of donitriptan is 1.32 to 2.2.

History

Donitriptan was being developed in France by bioMérieux-Pierre Fabre and made it to phase II clinical trials in Europe before development was discontinued.