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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- CAS. Nr.: 140695-21-2
- Formel: C19H28N4O5S2
- Molecular Weight:456.58
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Speicherung:
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Biologische Aktivität
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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.
Chemical Information
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CAS. Nr. 140695-21-2
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Molecular Weight 456.58
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[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
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Osutidine Related Classifications
HY-105101 Related Classifications
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