ALMOTRIPTAN

Описание

Almotriptan is an agonist of the serotonin (5-HT) receptor subtypes 5-HT_1B and 5-HT_1D (IC₅₀s = 12 and 13 nM, respectively, in a radioligand binding assay). It is selective for human 5-HT_1B and 5-HT_1D receptors over rat 5-HT_1A and human 5-HT_2A and 5-HT₄ receptors (IC₅₀s = 0.85, 25.1, and 140 μM, respectively). Almotriptan induces contractions in isolated canine saphenous veins (EC₅₀ = 394 nM) but not isolated rabbit renal or mesenteric arteries. It increases carotid vascular resistance in anesthetized cats (ED₁₀₀ = 11 μg/kg, i.v.) without increasing blood pressure or heart rate. Formulations containing almotriptan have been used in the treatment of migraine headaches.

Химические свойства

Pale Yellow Solid

Использование

Almotriptan is a serotonin 5HT1B /1D-receptor agonist used for treatment of migraine.

Определение

ChEBI: The malate salt of almotriptan.

Общее описание

Almotriptan, marketed in 2000, has the highest oralbioavailability among all triptans. It is metabolizedby both MAO-A and CYP3A4, thus has a more favorableside effects profile when compared with sumatriptan.However, it is only available in a 12.5 mg tablet form.