Ebrotidine

SKU: orb1308352

Description

Ebrotidine (FI3542) is a competitive histamine H2-receptor antagonist with a Ki of 127.5 nM. It exhibits potent gastric antisecretory and gastroprotective effects, making it a useful research tool for studying peptic ulcer disease and gastric acid secretion in both in vitro and in vivo experimental models.

Research Area

Immunology & Inflammation, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 100981-43-9
• MW: 477.42
• Purity: 97.50% (May vary between batches)
• Formula: C₁₄H₁₇BrN₆O₂S₃
• SMILES: NC(=N)Nc1nc(CSCCN\C=N\S(=O)(=O)c2ccc(Br)cc2)cs1
• Target: Histamine Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (8.38 mM);DMSO:100 mg/mL (209.46 mM)

Bioactivity

• Target IC50:
  H2 receptor:127.5 nM(Ki)
• In Vivo:
  Ebrotidine inhibited histamine- and pentagastrin-stimulated acid secretion in a dose-dependent manner (ED50: 0.21 and 0.44 mg/kg, respectively), following intravenous administration to rats . Results of the macroscopic assessment revealed that ebrotidine at doses of 50mg and higher/kg body weight effectively prevented mucosal injury and that the maximal protective effect was achieved by 1h. Physicochemical analysis established that ebrotidine evoked 30% increase in mucus gel dimension, and showed a 20% increase in phospholipids, and the content of sulfo- (18%) and sialomucins (21%) . The mean number of gastric erosions seen at endoscopy after treatment with ebrotidine plus ASA (2.0 +/- 0.3) was obviously lower than that after placebo plus ASA (3.7 +/- 0.2). This reduction in lesion core by ebrotidine was accompanied by a significant increase in gastric blood flow (by 15% in corpus and 26% in antrum), by a rise in transmucosal potential difference (by 12%), and by a decrease of mucosal micro bleeding .
  Read more...
• In Vitro:
  Ebrotidine displaced 3H-thiotidine specific binding to histamine H2-receptors (Ki: 127.5 nmol/l), showing a higher affinity (p < 0.05) than ranitidine (Ki: 190.0 nmol/l) and cimetidine (Ki: 246.1 nmol/l) .
  Read more...

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, FI 3542, FI3542, FI-3542, H2 receptor, Histamine Receptor, HistamineReceptor, Inhibitor, Ebrotidine

Compound Identifiers

PubChem CID

65869