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血小板聚集抑制剂5-(2-氯苄基)-4,5,6,7-四氢噻吩并[3,2-c]吡啶盐酸盐(噻氯匹定)对血行转移的影响。

Effects of 5-(2-chlorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine hydrochloride (Ticlopidine), a platelet aggregation inhibitor, on blood-borne metastasis.

作者信息

Kohga S, Kinjo M, Tanaka K, Ogawa H, Ishihara M, Tanaka N

出版信息

Cancer Res. 1981 Nov;41(11 Pt 1):4710-4.

PMID:7306988
Abstract

A new platelet aggregation inhibitor compound, 5-(2-chlorobenzyl-4,5,6,7-tetrahydrothieno[3,2-C]pyridine hydrochloride (ticlopidine), was examined for its inhibitory effects on blood-borne metastasis using three different rodent tumors (B16 melanoma, Lewis lung carcinoma, and rat ascites hepatoma, AH130). Ticlopidine was administered p.o. to the rodents. It inhibited the aggregation of platelets induced by adenosine diphosphate, thrombin, crude extract of AH130, and viable AH130 and B16 melanoma cells and also resulted in a significant decrease of pulmonary metastasis induced by i.v. injection of B16 melanoma and AH130. Spontaneous pulmonary metastasis of Lewis lung carcinoma was also inhibited by p.o. administration of ticlopidine. This new compound may be a useful agent for inhibiting platelet aggregation caused by various agents and for suppressing hematogenous pulmonary metastasis.

摘要

一种新型血小板聚集抑制剂化合物,5 -(2 - 氯苄基)- 4,5,6,7 - 四氢噻吩并[3,2 - c]吡啶盐酸盐(噻氯匹定),使用三种不同的啮齿动物肿瘤(B16黑色素瘤、Lewis肺癌和大鼠腹水肝癌AH130)来检测其对血行转移的抑制作用。噻氯匹定经口服给予啮齿动物。它抑制由二磷酸腺苷、凝血酶、AH130粗提物以及活的AH130和B16黑色素瘤细胞诱导的血小板聚集,并且还导致静脉注射B16黑色素瘤和AH130所诱导的肺转移显著减少。口服噻氯匹定也抑制Lewis肺癌的自发性肺转移。这种新化合物可能是一种用于抑制由各种因素引起血小板聚集以及抑制血源性肺转移的有用药物。

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