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1
Carcinogenicity of methapyrilene hydrochloride, mepyramine hydrochloride, thenyldiamine hydrochloride, and pyribenzamine hydrochloride in Sprague-Dawley rats.盐酸美吡拉敏、盐酸甲氧苄二胺、盐酸噻吩二胺及盐酸去敏灵在斯普拉格-道利大鼠中的致癌性。
J Cancer Res Clin Oncol. 1986;111(1):71-4. doi: 10.1007/BF00402780.
2
Carcinogenicity studies of some analogs of the carcinogen methapyrilene in F344 rats.致癌物质甲吡咯烷一些类似物在F344大鼠中的致癌性研究。
J Cancer Res Clin Oncol. 1986;112(1):57-60. doi: 10.1007/BF00394940.
3
Early stages of chemically induced liver carcinogenesis by oral administration of the antihistaminic methapyrilene hydrochloride.通过口服抗组胺药盐酸美吡拉敏诱导化学性肝癌发生的早期阶段。
J Cancer Res Clin Oncol. 1983;106(1):53-7. doi: 10.1007/BF00399897.
4
Chronic toxicity tests of pyrilamine maleate and methapyrilene hydrochloride in F344 rats.
Food Chem Toxicol. 1984 Jan;22(1):27-30. doi: 10.1016/0278-6915(84)90048-6.
5
Characterization of the antihistamines tripelennamine, methapyrilene, and thenyldiamine and their N-oxides by thermospray mass spectrometry.通过热喷雾质谱法对组胺拮抗剂曲普利啶、美吡拉敏和乙二胺及其N-氧化物进行表征。
J Anal Toxicol. 1989 Mar-Apr;13(2):94-6. doi: 10.1093/jat/13.2.94.
6
NTP Hepatotoxicity Studies of the Liver Carcinogen Methapyrilene Hydrochloride (CAS No. 135-23-9) Administered in Feed to Male F344/N Rats.通过饲料给予雄性F344/N大鼠肝脏致癌物盐酸美吡拉敏（CAS编号：135 - 23 - 9）的NTP肝毒性研究。
Toxic Rep Ser. 2000 Feb;46:1-C7.
7
A study of the potential genotoxicity of methapyrilene and related antihistamines using the hepatocyte/DNA repair assay.使用肝细胞/DNA修复试验对甲吡咯啉及相关抗组胺药潜在遗传毒性的研究。
Mutat Res. 1984 Feb;135(2):131-7. doi: 10.1016/0165-1218(84)90166-6.
8
Fungal transformations of antihistamines: metabolism of methapyrilene, thenyldiamine and tripelennamine to N-oxide and N-demethylated derivatives.
Xenobiotica. 1988 Mar;18(3):301-12. doi: 10.3109/00498258809041666.
9
The carcinogenic effect of methapyrilene combined with nitrosodiethylamine given to rats in low doses.低剂量给予大鼠的甲吡咯烷与二乙基亚硝胺联合使用的致癌作用。
Carcinogenesis. 1992 Jul;13(7):1293-7. doi: 10.1093/carcin/13.7.1293.
10
Distribution of the liver carcinogen methapyrilene in Fischer rats and its interaction with macromolecules.肝脏致癌物甲吡咯烷在费希尔大鼠体内的分布及其与大分子的相互作用。
J Cancer Res Clin Oncol. 1982;103(1):69-73. doi: 10.1007/BF00410307.

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1
B-13 progenitor-derived hepatocytes (B-13/H cells) model lipid dysregulation in response to drugs and chemicals.B-13祖细胞来源的肝细胞（B-13/H细胞）可模拟脂质失调以响应药物和化学物质。
Toxicology. 2017 Jul 1;386:120-132. doi: 10.1016/j.tox.2017.05.014. Epub 2017 May 26.
2
Toxicogenomics in drug discovery and drug development: potential applications and future challenges.药物发现与药物开发中的毒理基因组学：潜在应用与未来挑战
Pharm Res. 2006 Aug;23(8):1659-64. doi: 10.1007/s11095-006-9003-8.

本文引用的文献

1
Liver tumors induced in rats by oral administration of the antihistaminic methapyrilene hydrochloride.通过口服抗组胺药盐酸美吡拉敏在大鼠中诱导产生的肝肿瘤。
Science. 1980 Aug 15;209(4458):817-9. doi: 10.1126/science.7403848.
2
The effects of methapyrilene hydrochloride on hepatocarcinogenicity and pentobarbital-induced sleeping time in rats and mice.
Toxicol Appl Pharmacol. 1982 Nov;66(2):252-8. doi: 10.1016/0041-008x(82)90290-3.
3
Inability of methapyrilene to induce sister chromatid exchanges in vitro and in vivo.美吡拉敏在体内外均无法诱导姐妹染色单体交换。
Cancer Res. 1982 Nov;42(11):4614-8.
4
Nitrosation and mutagenicity of some amine drugs.某些胺类药物的亚硝化作用和致突变性。
Toxicol Appl Pharmacol. 1980 Feb;52(2):237-44. doi: 10.1016/0041-008x(80)90110-6.
5
Guidelines for simple, sensitive significance tests for carcinogenic effects in long-term animal experiments.长期动物实验中致癌作用简单、灵敏显著性检验指南。
IARC Monogr Eval Carcinog Risk Chem Hum Suppl. 1980(2 Suppl):311-426.
6
Chronic toxicity tests of pyrilamine maleate and methapyrilene hydrochloride in F344 rats.
Food Chem Toxicol. 1984 Jan;22(1):27-30. doi: 10.1016/0278-6915(84)90048-6.
7
Distribution of the liver carcinogen methapyrilene in Fischer rats and its interaction with macromolecules.肝脏致癌物甲吡咯烷在费希尔大鼠体内的分布及其与大分子的相互作用。
J Cancer Res Clin Oncol. 1982;103(1):69-73. doi: 10.1007/BF00410307.
8
Early stages of chemically induced liver carcinogenesis by oral administration of the antihistaminic methapyrilene hydrochloride.通过口服抗组胺药盐酸美吡拉敏诱导化学性肝癌发生的早期阶段。
J Cancer Res Clin Oncol. 1983;106(1):53-7. doi: 10.1007/BF00399897.
9
DNA damage induced by the antihistaminic drug methapyrilene hydrochloride.抗组胺药盐酸美吡拉敏诱导的DNA损伤。
Mutat Res. 1982 Mar;103(3-6):213-8. doi: 10.1016/0165-7992(82)90045-8.

盐酸美吡拉敏、盐酸甲氧苄二胺、盐酸噻吩二胺及盐酸去敏灵在斯普拉格-道利大鼠中的致癌性。

Carcinogenicity of methapyrilene hydrochloride, mepyramine hydrochloride, thenyldiamine hydrochloride, and pyribenzamine hydrochloride in Sprague-Dawley rats.

作者信息

Habs M, Shubik P, Eisenbrand G

出版信息

J Cancer Res Clin Oncol. 1986;111(1):71-4. doi: 10.1007/BF00402780.

DOI:10.1007/BF00402780
PMID:3949852
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12253792/
Abstract

Four histamine antagonists, methapyrilene, thenyldiamine, mepyramine and pyribenzamine were tested for carcinogenicity in rats by continuous application in drinking water. Only methapyrilene displayed significant carcinogenic effects, inducing liver tumors in a dose-related pattern. Analogues not containing a thiophene ring (mepyramine, pyribenzamine) did not exhibit neoplastic effects under the experimental conditions.

摘要

通过在饮用水中持续给药，对四种组胺拮抗剂——新安替根、乙二胺、甲氧苄二胺和苯吡胺进行了大鼠致癌性测试。只有新安替根表现出显著的致癌作用，以剂量相关的方式诱发肝肿瘤。在实验条件下，不含噻吩环的类似物（甲氧苄二胺、苯吡胺）未表现出肿瘤形成作用。