Eletriptan hydrobromide 是一种口服活性激动剂，对 5-HT1B/1D 受体具有特异性亲和力，Ki值分别为 0.92 和 3.14 nM。

Eletriptan hydrobromide is an orally active agonist with specific affinity for the 5-hydroxytriptamine1B/1D receptor.

[3H]Eletriptan has a total number of binding sites (Bmax) of 2478 fmol/mg and 1576 fmol/mg for 5-HT1B and 5-HT1D, respectively. [3H]Eletriptan has a significantly faster association rate (K(on) 0.249/min/nM) than [3H]sumatriptan (K(on) 0.024/min/nM) and a significantly slower off-rate (K(off) 0.027/min compared to 0.037/min for [3H]sumatriptan). [1] 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. [2]

177834-92-3

C22H27BrN2O2S

463.43

Eletriptan HBr;UK-116044;依来曲普坦氢溴酸盐;Eletriptan hydrobromide

DMSO:46.3 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years