Ebrotidine

Research use only, not for human use.

Ebrotidine is a competitive H2-receptor antagonist with Ki of 127.5 nM. Ebrotidine has a potent antisecretory activity and evidenced gastroprotection.

Ebrotidine is a competitive H2-receptor antagonist with Ki of 127.5 nM. Ebrotidine has a potent antisecretory activity and evidenced gastroprotection.(In Vitro):Ebrotidine displaced 3H-thiotidine specific binding to histamine H2-receptors, showing a higher affinity than ranitidine (Ki = 190.0 nM) and cimetidine (Ki = 246.1 nM) .(In Vivo):Ebrotidine inhibited histamine- (ED50: 0.21 mg/kg) and pentagastrin- (ED50: 0.44 mg/kg) stimulated acid secretion in a dose-dependent manner in rats . Ebrotidine at doses of 50mg and higher/kg body weight effectively prevented mucosal injury, and that the maximal protective effect was achieved by 1h. Ebrotidine evoked 30% increase in mucus gel dimension, and showed 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 microbleeding.

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FI3542

GPCR/G Protein

Histamine Receptor

Human Endogenous Metabolite| Nucleoside Antimetabolite/Analog

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100981-43-9

477.41

C14H17BrN6O2S3

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (209.46 mM)

NC(=N)Nc1nc(CSCCN\C=N\S(=O)(=O)c2ccc(Br)cc2)cs1

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(-20℃)

With Ice Pack

≥ 2 years