Eletriptan (Synonyms: UK 116044) |
| رقم الكتالوجGC43594 |
Eletriptan (UK-116044) هو ناهض لمستقبلات السيروتونين 5-HT1B و 5-HT1D انتقائي للغاية ونشط عن طريق الفم ، مع قيم pKi تبلغ 8.0 و 8.9 ، على التوالي
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Cas No.: 143322-58-1
Sample solution is provided at 25 µL, 10mM.
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Eletriptan is an agonist of the serotonin (5-HT) receptor types 5-HT1B and 5-HT1D. It inhibits forskolin-induced cAMP accumulation in and induces vasoconstriction of isolated rabbit common carotid artery rings (pD2s = 7.6 and 4.9, respectively), an effect that can be blocked by the 5-HT1B antagonist SB216641 but not the 5-HT1D antagonist BRL15572. Eletriptan preferentially induces constriction of isolated human cerebral over coronary arteries (EC50s = 15.8 and 1,995 nM, respectively). Formulations containing eletriptan have been used in the treatment of migraine headache.
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