Histamine H2 receptor antagonist-1
Antiulcer Agent 3 is a orally active histamine H2-receptor competitive antagonist (pA2 = 6.7). Antiulcer Agent 3 reduces gastric acid secretion. Antiulcer Agent 3 reduces gastric lesions in water-immersion stress-induced ulcer rat models. Antiulcer Agent 3 protects against HCl-ethanol-induced gastric lesions in rats. Antiulcer Agent 3 can be used for the research of peptic ulcer disease.
For research use only. We do not sell to patients.
- CAS No.: 127966-78-3
- Formula: C19H30N2O3S
- Molecular Weight:366.52
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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H2 Receptor 6.7 (pA2) |
Antiulcer Agent 3 (compound 8) acts as a competitive histamine H2 receptor antagonist in isolated guinea pig right atria, with a pA2 value of 6.7[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Antiulcer Agent 3 (administered orally; single dose; 5 minutes before stress) inhibits water-immersion stress-induced gastric ulcers in rats, with an oral ED50 of 13.3 mg/kg[1].
Antiulcer Agent 3 (oral administration; single dose) exhibits cytoprotective activity against hydrochloric acid-ethanol-induced gastric ulcers in rats, with an oral ED50 of 43.7 mg/kg[1].
Antiulcer Agent 3 (0.25-1.0 mg/kg; intravenous injection; single administration) inhibits Histamine (HY-B1204)-induced gastric acid secretion in conscious dogs with Heidenhain pouches, and exhibits significant long-acting activity at the dose of 1.0 mg/kg, with an ED50 of 0.38 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 180-200 g, gastric fistula model)[1]
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Dosage:30 mg/kg
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Administration:i.d.; single dose
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Result:Inhibited basal gastric acid secretion by 79.5%.
Achieved an ED50 of 12.9 mg/kg for gastric acid antisecretory activity.
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Animal Model:LR beagle (male, 9-10 kg, Heidenhain pouch model)[1]
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Dosage:0.25 mg/kg; 0.5 mg/kg; 1.0 mg/kg
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Administration:i.v.; single dose
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Result:Inhibited histamine-stimulated gastric acid secretion.
Produced a significant, long-lasting reduction in acid output at 1.0 mg/kg, with values significantly different from controls at p < 0.05 or p < 0.01 for multiple time points up to 180 minutes.
Chemical Information
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CAS No. 127966-78-3
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Molecular Weight 366.52
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Formula C19H30N2O3S
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SMILES
O=C(NCCCOC1=CC=CC(CN2CCCCC2)=C1)CSCCO
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Histamine H2 receptor antagonist-1 Related Classifications
HY-116596 Related Classifications
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- Histamine H2 receptor antagonist-1
- 127966-78-3
- Histamine Receptor
- gastric lesions
- rats
- water-immersion stress-induced ulcer rat models
- gastric acid secretion
- guinea pig right atria
- histamine H2-receptor
- peptic ulcer disease
- Heidenhain pouch
- HCl-ethanol-induced gastric lesions
- gastric fistula
- Inhibitor
- inhibitor
- inhibit