Eletriptan hydrobromide

SKU: orb1310824

Description

Eletriptan hydrobromide is a selective 5-HT1B/1D receptor agonist suitable for oral administration. It is widely used in pharmacological research to study migraine pathophysiology and receptor mechanisms in both in vitro binding assays and in vivo animal models.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 177834-92-3
• MW: 463.43
• Purity: >99.99% (May vary between batches)
• Formula: C₂₂H₂₇BrN₂O₂S
• SMILES: Br.CN1CCC[C@@H]1Cc1c[nH]c2ccc(CCS(=O)(=O)c3ccccc3)cc12
• Target: 5-HT Receptor
• Solubility: DMSO:60 mg/mL (129.47 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.32 mM)

Bioactivity

• Target IC50:
  5-HT1D:3.14 nM(Ki)|5-HT1B:0.92 nM(Ki)
• In Vivo:
  The total number of binding sites (Bmax) of [3H]Eletriptan to 5-HT1B and 5-HT1D was 2478 fmol/mg and 1576 fmol/mg, respectively.The binding rate of [3H]Eletriptan (K(on) 0.249/min/nM) was significantly faster than that of [3H]sumatriptan (K(on) 0.024/ min/nM), while the shedding rate (K(off) 0.027/min compared to 0.037/min for [3H]sumatriptan) was significantly slower than [3H]Eletriptan . Eletriptan induces concentration-dependent constriction in meningeal arteries, coronary arteries, and saphenous veins.Eletriptan is more potent in meningeal arteries than in coronary arteries (86-fold) or saphenous veins (66-fold). The predicted contractility of Eletriptan (40 mg and 80 mg) and sumatriptan (100 mg) at free C (max) in meningeal arteries observed in clinical trials is similar.
• In Vitro:
  [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). 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Eletriptan, Eletriptan HBr, Eletriptan Hydrobromide, Eletriptan hydrobromide, Inhibitor, inhibit, 5-hydroxytryptamine Receptor, 5HTReceptor, 5HT Receptor, 5-HT Receptor, 5-HT1D, 5-HT1B, Serotonin Receptor, UK116044, UK-116044, UK 116044

Compound Identifiers

PubChem CID

656631