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Sumatriptan [4] binds to 5-HT 1D receptors, zolmitriptan, [5] rizatriptan, [6] naratriptan, [7] almotriptan, [8] and frovatriptan [9] binds to 5-HT 1B/1D and eletriptan [10] binds to 5-HT 1B/1D/1F receptors. Triptans are believed to exert their effects through vasoconstriction, leading to reduced carotid arterial circulation without affecting ...
Frovatriptan, sold under the brand name Frova, is a triptan drug developed by Vernalis for the treatment of migraine headaches [1] and for short term prevention of menstrual migraine. [2] The product is licensed to Endo Pharmaceuticals in North America and Menarini in Europe.
They continued developing and working on a desirable action on 5-HT by 5-HT 1 receptor activation for an anti-migraine drug. Continued work led to the development of sumatriptan, now known as the first 5-HT 1 agonist, selective for the 5-HT 1D/B receptors and also the 5-HT 1F receptor with less affinity. By 1991 sumatriptan became available in ...
In addition to being 5-HT 1B agonists, triptans (i.e. sumatriptan, almotriptan, zolmitriptan, naratriptan, eletriptan, frovatriptan and rizatriptan) are also agonists at the 5-HT 1D receptor, which contributes to their antimigraine effect caused by vasoconstriction of blood vessels in the brain. The same is true for ergotamine.
The triptan drug class includes 1st generation sumatriptan (which has poor bioavailability), and second generation zolmitriptan. [2] Due to their safety, efficacy and selectivity, triptans are considered first line agents for abortion of migraines. [2] These medications are selective 5-HT 1B/1D receptor agonists with some activity at 5-HT 1F.
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Zolmitriptan is a triptan and a substituted tryptamine. [3] [4] It is specifically the derivative of N,N-dimethyltryptamine (DMT) in which the hydrogen atom at position 5 of the indole ring has been substituted with a [(4S)-2-oxo-1,3-oxazolidin-4-yl]methyl group. [4] The experimental log P of zolmitriptan is 1.6 to 1.8. [4]
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