Eletriptan Hydrobromide

Eletriptan Hydrobromide is a selective 5‑HT₁B/1D receptor agonist indicated for the acute treatment of migraine with or without aura. As a member of the triptan class, Eletriptan Hydrobromide produces a dose‑dependent reduction in carotid artery blood flow in vivo and displays potent antimigraine activity. Eletriptan Hydrobromide is supplied as an off‑white to light tan solid with a purity of ≥98% (HPLC). The indole core of Eletriptan Hydrobromide is critical for its high‑affinity binding to 5‑HT₁B and 5‑HT₁D receptors. Eletriptan Hydrobromide is also available as a reference standard for analytical method development, method validation, and quality control applications in ANDA filings.

 

Product Parameters

---

Parameter	Specification
Product Name	Eletriptan Hydrobromide
CAS Number	177834-92-3
Molecular Formula	C₂₂H₂₇BrN₂O₂S
Molecular Weight	463.43 g/mol
Physical Form	Solid
Appearance	Offwhite to light tan
Melting Point	169–171 °C
Storage Condition	Desiccate at room temperature

Bioactivity

---

Eletriptan (UK-116044) is a selective agonist of the 5-hydroxytryptamine 1B and 1D receptors, with Ki values of 0.92 nM and 3.14 nM, respectively.

 

In Vitro Study

---

Eletriptan induces concentration-dependent contraction of the middle meningeal artery, coronary arteries, and saphenous vein. Its potency in the middle meningeal artery is significantly higher than in the coronary arteries (86-fold) or the saphenous vein (66-fold). In clinical trials, it was observed that eletriptan (40 mg and 80 mg) and sumatriptan (100 mg) elicited similarly predictable contractions in the middle meningeal artery at their maximum free plasma concentrations (Cmax).

 

In Vivo Studies

---

In anesthetized dogs, Eletriptan (<1000 mg/kg, intravenous injection) induces dose-dependent reduction of carotid blood flow. Eletriptan decreases coronary artery diameter, with an ED50 value of 63 mg/kg in anesthetized dogs. In dural rats, administration of Eletriptan (<300 mg/kg, intravenous injection) prior to trigeminal ganglion electrical stimulation completely inhibits dose-dependent plasma protein leakage. In dural rats, Eletriptan (100 mg/kg, intravenous injection) fully suppresses plasma protein leakage. In migraine patients, the headache response rates were 24% in the placebo group, 54% with Eletriptan (20 mg), 65% with Eletriptan (40 mg), and 77% with Eletriptan (80 mg) at 2 hours post-administration. Eletriptan demonstrates excellent tolerability; the predominant adverse effects in migraine patients are mild to moderate in intensity and transient. In cats, the iontophoretic efflux of Eletriptan (50 nA) inhibited responses in 75% of cells and suppressed average cell discharge activity by 42%.

Contact Us

---

Ready to secure high‑quality Eletriptan Hydrobromide for your migraine drug manufacturing or analytical development program? Cosperpharm is your trusted partner. Contact our team today for pricing, documentation, or technical support — we are committed to delivering excellence in pharmaceutical intermediates and reference standards.