盐酸西咪替丁

盐酸西咪替丁用途

盐酸西咪替丁(SKF-92334)是一种口服活性逆组胺H2受体拮抗剂,Ki为0.6μM。盐酸西咪替丁是一种胃酸还原剂,可用于十二指肠和胃溃疡的研究。盐酸西咪替丁具有抗癌和抗炎活性[1][2][5]。

点击显示

盐酸西咪替丁名称

[ CAS 号 ]:
70059-30-2

[ 中文名 ]:
盐酸西咪替丁

[ 英文名 ]:
Cimetidine hydrochloride

[中文别名 ]:

[英文别名 ]:

EINECS 274-297-2
MFCD01724314
Cimetidin-HCl
Cimetidine Hydrochloride USP24
Cimetidinhydrochlorid
cimetex
Cimetidine hydrochloride

盐酸西咪替丁生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 免疫及炎症 >> 组胺受体

研究领域 >> 内分泌

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体

[ 靶点 ]

H2 Receptor:0.6 μM (Kd)

[体外研究]

盐酸西咪替丁(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,可能有助于其对胃肠道癌症的抗肿瘤活性[1]。盐酸西咪替丁对高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]。盐酸西咪替丁对3LL细胞的增殖、存活、迁移和侵袭没有影响。盐酸西咪替丁逆转MDSC介导的T细胞抑制,并提高IFN-γ的产生[4]。西咪替丁介导的NCAM下调涉及抑制NF-κB(NCAM基因表达的转录激活剂)的核易位[5]。

[体内研究]

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

[参考文献]

[1]. 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.

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

[3]. 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.

[4]. 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.

[5]. 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.

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

盐酸西咪替丁物理化学性质

[ 沸点 ]:
488ºC at 760 mmHg

[ 分子式 ]:
C₁₀H₁₇ClN₆S

[ 分子量 ]:
288.80000

[ 闪点 ]:
248.9ºC

[ 精确质量 ]:
288.09200

[ PSA ]:
114.19000

[ LogP ]:
2.18118

[ 外观性状 ]:
白色结晶粉末

[ 储存条件 ]:
室温，密封，干燥

盐酸西咪替丁MSDS

详细MSDS(安全技术说明书)

盐酸西咪替丁毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: MF0035100

CHEMICAL NAME :: Guanidine, N-cyano-N'-methyl-N''-(2-(((5-methyl-1H-imidazol-4-yl )methyl)thio)ethyl)-, monohydrochloride

CAS REGISTRY NUMBER :: 70059-30-2

LAST UPDATED :: 199504

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C10-H16-N6-S.Cl-H

MOLECULAR WEIGHT :: 288.84

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 12 mg/kg/6H-I

TOXIC EFFECTS :: Blood - leukopenia Blood - thrombocytopenia

MUTATION DATA

TYPE OF TEST :: Unscheduled DNA synthesis

TEST SYSTEM :: Rodent - rat Liver

DOSE/DURATION :: 500 umol/L

REFERENCE :: ENMUDM Environmental Mutagenesis. (New York, NY) V.1-9, 1979-87. For publisher information, see EMMUEG. Volume(issue)/page/year: 7,833,1985 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X3086 No. of Facilities: 485 (estimated) No. of Industries: 1 No. of Occupations: 6 No. of Employees: 17435 (estimated) No. of Female Employees: 14362 (estimated)

点击显示

盐酸西咪替丁安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

[ RTECS号 ]:
MF0035100

[ 海关编码 ]:
2933290090

盐酸西咪替丁海关

[ 海关编码 ]: 2933290090

[ 中文概述 ]:
2933290090. 其他结构含非稠合咪唑环的化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933290090. other compounds containing an unfused imidazole ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

盐酸西咪替丁文献

Pharmacokinetic study of hydroxypropylmethylcellulose microparticles loaded with cimetidine.

Adv. Clin. Exp. Med. 22(1) , 41-5, (2013)

The objective of this study was to assess the pharmacokinetic behavior of floating hydroxypropylmethylcellulose microparticles loaded with cimetidine (FMC) prepared using the non-solvent addition coac...

Multiple mechanisms of ligand interaction with the human organic cation transporter, OCT2.

Am. J. Physiol. Renal Physiol. 304(1) , F56-67, (2013)

OCT2 is the entry step for organic cation (OC) secretion by renal proximal tubules. Although many drugs inhibit OCT2 activity, neither the mechanistic basis of their inhibition nor their transport sta...

Inhibition of human alcohol and aldehyde dehydrogenases by cimetidine and assessment of its effects on ethanol metabolism.

Chem. Biol. Interact. 202(1-3) , 275-82, (2013)

Previous studies have reported that cimetidine, an H2-receptor antagonist used to treat gastric and duodenal ulcers, can inhibit alcohol dehydrogenases (ADHs) and ethanol metabolism. Human alcohol deh...

更多文献