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Donitriptan
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Donitriptan (; developmental code name F-11356) is a which was investigated as an antimigraine agent but was never marketed. It acts as a selective 5-HT1B and 5-HT1D receptor . The drug reached phase 2 prior to the discontinuation of its development.

Pharmacology
+
12–25 (Ki)
182–1,150 ()
0.08–0.36 (Ki)
0.10–1.8 ()
94–100% ()
0.06–0.48 (Ki)
0.27–0.83 ()
97–99% ()
1,150–1,700 (Ki)
>10,000 ()
3,390–6,610 (Ki)
>10,000 ()
182–447 (Ki)
7.9 ()
813 (Ki)
25 ()
575 (Ki) (rat)
()
>10,000 (mouse)
2,000 (guinea pig)
813
2,340
372–617 (Ki)
5,890 ()
>10,000
>10,000
>10,000
>10,000
>10,000
>1,000
>1,000 ()
>1,000 ()
>1,000 ()
>10,000
>10,000
Notes: The smaller the value, the more avidly the drug binds to the site. All proteins are human unless otherwise specified. Refs:

Donitriptan acts as a high-affinity, high-efficacy near- of the 5-HT1B (Ki = 0.079–0.40nM; = 94%) and 5-HT1D receptors (Ki = 0.063–0.50nM; = 97%), and is among the most potent of the triptan series of drugs.

(2026). 9780781754002, Lippincott Williams & Wilkins.
It is also notable and unique among most of the triptans in being a potent serotonin 5-HT2A receptor agonist ( = 7.9nM), 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 and 5-methoxytryptamine, and an analogue of the dimethyltryptamine (DMT) and 5-MeO-DMT.

The predicted of donitriptan is 1.32 to 2.2.

History
Donitriptan was being developed in by bioMérieux-Pierre Fabre and made it to phase II in before development was discontinued.
(2013). 9780203911259, CRC Press.
(2003). 9783211839034, Springer Vienna. .
(2026). 9781604730487, Univ. Press of Mississippi.

See also

: , , , , , , , , ,
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