5-HT1B,5-HT1D

463.43

DMSO : 46.3 mg/mL (100 mM)

类白色至黄褐色固体

Eletriptan has a total number of binding sites (Bmax) of 2478 fmol/mg and 1576 fmol/mg for 5-HT1B and 5-HT1D, respectively. Eletriptan has a significantly faster association rate (K(on) 0.249/min/nM) than sumatriptan (K(on) 0.024/min/nM) and a significantly slower off-rate (K(off) 0.027/min compared to 0.037/min for sumatriptan). Eletriptan induces concentration-dependent contractions of meningeal artery, coronary artery, and saphenous vein. The potency of Eletriptan is higher in meningeal artery than in coronary artery (86-fold) or saphenous vein (66-fold). The predicted contraction by Eletriptan (40 mg and 80 mg) and sumatriptan (100 mg) at free C(max) observed in clinical trials is similar in meningeal artery.

Eletriptan ( Headache response rates are 24% for placebo; 54% for Eletriptan (20 mg);65% for Eletriptan (40 mg);and 77% for Eletriptan (80 mg) at the primary endpoint (2 hours after dosing) in patients with migraine. Headache-free rates at 2 hours are 6% for placebo, 29% for Eletriptan (40 mg) and 37% for Eletriptan (80 mg) at the primary endpoint (2 hours after dosing) in patients with migraine. Eletriptan is well tolerated, and the majority of adverse events are mild or moderate in intensity and transient in patients with migraine. Iontophoretic ejection (50 nA) of Eletriptan suppresses the response in 75% of cells and causes an average suppression of cell firing of 42% in cats.

依来曲普坦氢溴酸盐；Eletriptan hydrobromide

C₂₂H₂₇BrN₂O₂S

177834-92-3