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Ebrotidine CAS: 100981-43-9

Category: Inhibitors
Product Name: Ebrotidine
Cat No: I000109
CAS No: 100981-43-9
Synonyms: N-(4-bromophenyl)sulfonyl-N'-[2-[[2-(diaminomethylideneamino)-1,3-thiazol-4-yl]methylsulfanyl]ethyl]methanimidamide
Molecular Formula: C14H17BrN6O2S3
Molecular Weight: 477.42
SMILES: O=S(C1=CC=C(Br)C=C1)(/N=C/NCCSCC2=CSC(NC(N)=N)=N2)=O
InChI: None
InChIKey: None
Solubility: 10 mM in DMSO
Target: Histamine
IC50: 127.5 nM (Ki)[1]; 0.21mg/kg (ED50, histamine- stimulated acid secretion) [2]
Storage: Store at -20°C
CAS 100981-43-9,Ebrotidine
  • Description

Ebrotidine(FI 3542) is a competitive H2-receptor antagonist (Ki= 127.5 nM) with a potent antisecretory activity and evidenced gastroprotection.
IC50 Value: 127.5 nM (Ki)[1]; 0.21mg/kg (ED50, histamine- stimulated acid secretion) [2]
Target: H2 receptor
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) [1].
in vivo: Following intravenous administration to rats, ebrotidine inhibited histamine- and pentagastrin-stimulated acid secretion in a dose-dependent manner, ED50 being 0.21 and 0.44 mg/kg, respectively [2]. The mean number of gastric erosions seen at endoscopy after treatment with ebrotidine plus ASA (2.0 +/- 0.3) was significantly 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 microbleeding [3]. Results of 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 20% increase in phospholipids, and the content of sulfo- (18%) and sialomucins (21%) [4].

  • Spec

Appearance:Solid powder
Purity: > 98%

  • References


1:Determination of ebrotidine and its metabolites by micellar electrokinetic capillary chromatography. Sentellas S, Puignou L, Galceran MT.J Chromatogr A. 2002 Nov 8;976(1-2):221-7. PMID: 12462613
2:Determination of ebrotidine metabolites in overlapping peaks from capillary zone electrophoresis using chemometric methods. Sentellas S, Saurina J, Hernández-Cassou S, Galceran MT, Puignou L.Electrophoresis. 2001 Jan;22(1):71-6. PMID: 11197182
3:Determination of ebrotidine and its metabolites by capillary electrophoresis with UV and mass spectrometry detection. Sentellas S, Puignou L, Moyano E, Galceran MT.J Chromatogr A. 2000 Aug 4;888(1-2):281-92. PMID: 10949494
4:Liver injury caused by ebrotidine: a new example of the utility of the postmarketing surveillance. Castillo JR, Torelló J, Hernandez A.Eur J Clin Pharmacol. 2000 May;56(2):187-9. No abstract available. PMID: 10877015
5:Prevention and healing of experimental indomethacin-induced gastric lesions: effects of ebrotidine, omeprazole and ranitidine. Arroyo MT, Lanas A, Sáinz R.Eur J Gastroenterol Hepatol. 2000 Mar;12(3):313-8. PMID: 10750652
6:[Hepatoxicity due to ebrotidine: report of two cases]. Quílez C, Palazón JM, Jover R, Martínez R, Chuliá T, Griñó P, Belda G.Gastroenterol Hepatol. 1999 Oct;22(8):434-5. Spanish. No abstract available. PMID: 10592681
7:Effect of ebrotidine on gastric mucosal inflammatory responses to Helicobacter pylori lipopolysaccharide. Slomiany BL, Piotrowski J, Slomiany A.J Physiol Pharmacol. 1999 Sep;50(3):391-404. PMID: 10574469
8:Rapid progression to liver cirrhosis of toxic hepatitis due to ebrotidine. Pineda JA, Larrauri J, Macías J, Hernández A, Guijarro J, Sayago M, Gavilán F, Aguilar J, Lissen E.J Hepatol. 1999 Oct;31(4):777-8. No abstract available. PMID: 10551406
9:Acute liver injury associated with the use of ebrotidine, a new H2-receptor antagonist. Andrade RJ, Lucena MI, Martin-Vivaldi R, Fernandez MC, Nogueras F, Pelaez G, Gomez-Outes A, Garcia-Escaño MD, Bellot V, Hervás A, Cárdenas F, Bermudez F, Romero M, Salmerón J.J Hepatol. 1999 Oct;31(4):641-6. PMID: 10551387
10:Allergic dermatitis due to oral ebrotidine. Carretero Aníbarro P, Blanco Carmona J, García González F, Garcés Sotillos M, Herrero Gil D, Pérez Giménez R, Juste Picón S.J Investig Allergol Clin Immunol. 1999 May-Jun;9(3):193-4. PMID: 10412683


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