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

Osutidine 是一种选择性组胺 H2 受体拮抗剂，能有效抑制组胺刺激的胃酸分泌。Osutidine 不影响卡巴胆碱或二丁酰环磷酸腺苷刺激的 [¹⁴C] 氨基比林的蓄积。Osutidine 具有不可逆抑制作用，包括非竞争性抑制。Osutidine 可用于胃粘膜损伤的研究。

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Osutidine

Osutidine Chemical Structure

CAS No. : 140695-21-2

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Osutidine 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

Osutidine 以浓度依赖的方式抑制 10-4 M 组胺刺激的 [14C]AP 在分离的犬胃黏膜细胞中的积累，IC50 为 1.85 × 10-6 M[1]。
Osutidine 对 10-4 M dbcAMP 刺激的 [14C]AP 在分离的犬胃黏膜细胞中的积累仅有轻微抑制作用 (最大抑制率为 20-32%)[1]。
Osutidine 使组胺浓度-反应曲线右移，并降低分离的犬胃黏膜细胞的最大反应，Schild 图斜率为 2.01，表明其对 H2 受体的拮抗作用不可克服且为非竞争性拮抗作用[1]。
Osutidine 与分离的犬胃黏膜细胞中的 H2 受体紧密结合，且难以通过洗涤逆转，表明其具有缓慢解离的特性[1]。
Osutidine 的主要活性对映体是 (-)-S-T-593，它负责 H2 受体拮抗作用，而 (+)-R-T-593 的活性较弱[1]。

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

Osutidine 相关抗体:
体内研究
(In Vivo)

Osutidine (6-60 mg/kg，腹腔注射，一次) 对 Sprague-Dawley 大鼠的胃黏膜具有显著的保护作用，能以剂量依赖的方式显著抑制乙醇引起的胃黏膜损伤[2]。

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.
分子量

456.58

Formula

C19H28N4O5S2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Osutidine 相关分类

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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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