Donitriptan (
INN
Inns are generally establishments or buildings where travelers can seek lodging, and usually, food and drink. Inns are typically located in the country or along a highway; before the advent of motorized transportation they also provided accommo ...
) (code name F-11356) is a
triptan
Triptans are a family of tryptamine-based drugs used as abortive medication in the treatment of migraines and cluster headaches. This drug class was first commercially introduced in the 1990s. While effective at treating individual headaches, th ...
drug
A drug is any chemical substance that causes a change in an organism's physiology or psychology when consumed. Drugs are typically distinguished from food and substances that provide nutritional support. Consumption of drugs can be via inhal ...
which was investigated as an
antimigraine agent
Antimigraine drugs are medications intended to reduce the effects or intensity of migraine headache. They include drugs for the treatment of acute migraine symptoms as well as drugs for the prevention of migraine attacks.
Treatment of acute symp ...
but ultimately was never marketed.
It acts as a high-
affinity
Affinity may refer to:
Commerce, finance and law
* Affinity (law), kinship by marriage
* Affinity analysis, a market research and business management technique
* Affinity Credit Union, a Saskatchewan-based credit union
* Affinity Equity Part ...
, high-
efficacy/near-
full agonist
An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the ag ...
of the
5-HT1B (pK
i = 9.4–10.1;
IA = 94%) and
5-HT1D receptors (pK
i = 9.3–10.2;
IA = 97%), and is among the most
potent
Potent may refer to:
* for the heraldic fur
*Warren Potent for the Australian Olympic medalist in shooting
See also:
*Potency (disambiguation)
Potency may refer to:
* Potency (pharmacology), a measure of the activity of a drug in a biologica ...
of the triptan series of drugs.
[Perez M, Fourrier C, Sigogneau I, Pauwels PJ, Palmier C, Valentin JP, John GW, Halazy S (1995) Synthesis and serotonergic activity of arylpiperazide derivatives of serotonin: Potent agonists for 5-HT1D receptors. ''Journal of Medicinal Chemistry'' 38:3602–3607.] Donitriptan was being developed in
France
France (), officially the French Republic ( ), is a country primarily located in Western Europe. It also comprises of overseas regions and territories in the Americas and the Atlantic, Pacific and Indian Oceans. Its metropolitan ar ...
by
bioMérieux
bioMérieux SA is a French multinational biotechnology company founded and headquartered in Marcy-l'Étoile, France, close to Lyon. bioMérieux is present in 44 countries and serves more than 160 countries through a large network of distribu ...
-
Pierre Fabre and made it to
phase II clinical trial
Clinical trials are prospective biomedical or behavioral research studies on human subject research, human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel v ...
s in
Europe
Europe is a large peninsula conventionally considered a continent in its own right because of its great physical size and the weight of its history and traditions. Europe is also considered a subcontinent of Eurasia and it is located enti ...
before development was discontinued.
References
5-HT1B agonists
5-HT1D agonists
Antimigraine drugs
Indole ethers at the benzene ring
Aromatic nitriles
Phenylpiperazines
Triptans
Abandoned drugs
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