2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor
  4. 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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Osutidine

Osutidine Chemical Structure

CAS No. : 140695-21-2

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Osutidine Related Antibodies

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Description

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[1][2].

IC50 & Target

H2 Receptor

 

In Vitro

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.

Osutidine Related Antibodies
In Vivo

Osutidine (6-60 mg/kg, i.p., once) has a significant protective effect on the gastric mucosa in Sprague-Dawley rats, significantly inhibiting ethanol-induced gastric mucosal damage in a dose-dependent manner[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].
Dosage: 6 mg/kg, 60 mg/kg
Administration: I.p., once
Result: Significantly inhibited ethanol-induced gastric mucosal damage in a dose-dependent manner.
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].
Dosage: 60 mg/kg Racemic T-593, 60 mg/kg (+)-(R)-T-593, 60 mg/kg (-)-(S)-T-593
Administration: I.p., once
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.
Molecular Weight

456.58

Formula

C19H28N4O5S2
CAS No.
SMILES

OC(C1=CC=C(O)C=C1)CN/C(NS(C)(=O)=O)=N\CCSCC2=CC=C(CNC)O2
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References
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Osutidine Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Osutidine140695-21-2Histamine ReceptorAminopyrine accumulationHistamine H2-antagonistInsurmountable antagonismCanine gastric mucosal cellInhibitorinhibitorinhibit

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