Osutidine
Osutidine is a selective histamine H2 receptor antagonist, can effectively inhibit histamine-stimulated gastric acid secretion. Osutidine does not affect [14C]aminopyrine accumulation stimulated by carbachol or dibutyryl-cAMP. Osutidine is insurmountable and includes non-competitive inhibition. Osutidine can be used for the study of gastric mucosal injury.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 140695-21-2
- 分子式: C19H28N4O5S2
- 分子量:456.58
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
Histamine Receptor アイソフォーム固有の製品をすべて表示
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生物活性
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H2 Receptor |
Osutidine inhibits the accumulation of 10-4 M histamine-stimulated [14C]AP in isolated canine gastric mucosal cells in a concentration-dependent manner, with an IC50 of 1.85 × 10-6 M[1].
Osutidine only slightly inhibits the accumulation of [14C]AP stimulated by 10-4 M dbcAMP in isolated canine gastric mucosal cells (maximum inhibition of 20-32%)[1].
Osutidine shifts the histamine concentration-response curve to the right and reduces the maximum response in isolated canine gastric mucosal cells, with a Schild plot slope of 2.01, indicating that H2 receptor antagonism is insurmountable and non-competitive[1].
Osutidine binds tightly to H2 receptors in isolated canine gastric mucosal cells and is difficult to reverse by washing, indicating that it has slow dissociation properties[1].
Osutidine has (-)-S-T-593 as its main active enantiomer responsible for H2 receptor antagonism, while (+)-R-T-593 exhibits weak activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats, weighing 200-230 grams, were anesthetized with sodium pentobarbital (35 mg/kg) and 1 ml of 40% ethanol solution was administered via gastric tube to induce acute gastric mucosal injury[2].
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Dosage:6 mg/kg, 60 mg/kg
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Administration:I.p., once
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Result:Significantly inhibited ethanol-induced gastric mucosal damage in a dose-dependent manner.
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Animal Model:Male Sprague-Dawley rats, weighing 200-230 grams, were anesthetized with sodium pentobarbital (35 mg/kg) and 1 ml of 40% ethanol solution was administered via gastric tube to induce acute gastric mucosal injury[2].
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Dosage:60 mg/kg Racemic T-593, 60 mg/kg (+)-(R)-T-593, 60 mg/kg (-)-(S)-T-593
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Administration:I.p., once
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Result:Significantly inhibited ethanol-induced gastric damage, but the protective effect of the racemic mixture is significantly stronger than that of its individual enantiomer.
Directly improved gastric mucosal microcirculation and effectively inhibited gastric acid secretion, significantly reducing the oxygen consumption of parietal cells, thereby alleviating mucosal hypoxia.
化学情報
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CAS 番号 140695-21-2
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分子量 456.58
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分子式 C19H28N4O5S2
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SMILES
OC(C1=CC=C(O)C=C1)CN/C(NS(C)(=O)=O)=N\CCSCC2=CC=C(CNC)O2
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Inoie M, et al. Histamine H2-receptor antagonism of Osutidine, an anti-ulcer agent: studies on aminopyrine accumulation in isolated canine gastric mucosal cells. Jpn J Pharmacol. 1998 Nov;78(3):313-22. [Content Brief]
[2]. Tsuji S, et al. Effects of osutidine (T-593) and its enantiomers on gastric mucosal hemodynamics and mucosal integrity in anesthetized rats. Arzneimittelforschung. 2001 Jan;51(1):46-50. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Osutidine 関連分類
HY-105101 関連分類
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