Cimetidine | 西咪替丁

MCE 国际站：Cimetidine

中文名：西咪替丁

CAS：51481-61-9

品牌：MedChemExpress (MCE)

存储条件：Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.

生物活性：Cimetidine (SKF-92334) 是一种具有口服活性的 组胺 H2 受体 拮抗剂，K_i 为 0.6 μM。西咪替丁是一种胃酸减少剂，可用于十二指肠和胃溃疡的研究。西咪替丁具有抗癌和抗炎活性^[1][2][5]。  

体外：西咪替丁 (SKF-92334) 是 H2R 的部分激动剂，其药理学特征不同于雷尼替丁和法莫替丁，这可能有助于其对胃肠道癌症的抗肿瘤活性 [1]。西咪替丁对高 OCT2 mRNA 水平的卵巢癌细胞（IGROV-1 细胞）中顺铂的摄取和细胞毒性没有影响^[3]。西咪替丁对3LL细胞的增殖、存活、迁移和侵袭无影响。西咪替丁逆转了 MDSC 介导的 T 细胞抑制，并改善了 IFN-γ 的产生^[4]。西咪替丁介导的 NCAM 下调涉及抑制 NF-kappaB 的核转位，NF-kappaB 是 NCAM 基因表达的转录激活因子^[5]。

体内：西咪替丁 (SKF-92334) 减少荷瘤小鼠脾脏、血液和肿瘤组织中的 S CD11b(+)Gr-1(+) 髓源性抑制细胞 (MDSC) 积累^[4]。西咪替丁对大鼠牙周病具有有益作用，可降低牙龈结缔组织中的RANKL/OPG比值，减少牙槽骨吸收^[6]。

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研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Immunology/Inflammation  |  Anti-infection

作用靶点：Histamine Receptor  |  Bacterial

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides

参考文献：[1]. Takahashi, H.K., et al., Cimetidine induces interleukin-18 production through H2-agonist activity in monocytes. Mol Pharmacol, 2006. 70(2): p. 450-3.

[2]. Sprowl, J.A., et al., Conjunctive therapy of cisplatin with the OCT2 inhibitor cimetidine: influence on antitumor efficacy and systemic clearance. Clin Pharmacol Ther, 2013. 94(5): p. 585-92.

[3]. Zheng, Y., et al., Cimetidine suppresses lung tumor growth in mice through proapoptosis of myeloid-derived suppressor cells. Mol Immunol, 2013. 54(1): p. 74-83.

[4]. Fukuda, M., K. Kusama, and H. Sakashita, Cimetidine inhibits salivary gland tumor cell adhesion to neural cells and induces apoptosis by blocking NCAM expression. BMC Cancer, 2008. 8: p. 376.

[5]. Longhini, R., et al., Cimetidine Reduces the Alveolar Bone Loss in Induced Periodontitis in Rat Molars. J Periodontol, 2013.

[6]. M J Smit, et al. Inverse agonism of histamine H2 antagonist accounts for upregulation of spontaneously active histamine H2 receptors. Proc Natl Acad Sci U S A. 1996 Jun 25;93(13):6802-7.