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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,Ki 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]。
热销产品:Ribavirin | Belinostat | DBCO-amine | SAICAR | Ulixertinib | KU-55933 | Adenosine 5'-diphosphate | DBCO-(PEG)3-VC-PAB-MMAE | Carfilzomib | Alectinib
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.
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