Angiotensin II Type 1 Receptor Antagonist, TCV-116, Prevents Neointima Formation in Injured Arteries in the Dog

The Japanese Journal of Pharmacology

Naotaka Shiota1¹  Shinji Takai¹  Mizuo Miyazaki¹  Hiroshi Sakonjo¹ 

[1] Department of Pharmacology, Osaka Medical College

关键词: Angiotensin II;    Angiotensin converting enzyme;    Chymase;    AT1-receptor antagonist;   

DOI  :  10.1254/jjp.79.455

学科分类：药理学

来源: Nihon Yakuri Gakkai Henshuubu / Japanese Pharmacological Society

【 摘 要 】

References(25)Cited-By(11)We investigated the effect of an angiotensin (Ang) II antagonist, (+/-)-1-(cyclohexyloxy- carbonyloxy)-ethyl 2-ethoxy-1-[[2′-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-1H-benzimidazole-7-carboxylate (TCV-116), on neointima formation in dog artery injured by a balloon catheter. Dogs were orally treated with 10 mg/kg TCV-116 or placebo twice a day for 5 weeks. After treatment with these drugs for 1 week, the right carotid artery was injured by a balloon catheter. The left carotid artery was regarded as the control. In the group treated with placebo, neointima formation in the injured arteries was observed. The activities of angiotensin converting enzyme (ACE) and chymase in the injured carotid arteries were increased 2.56- and 3.26-fold compared with those in the non-injured arteries, respectively. The neointimal area in dogs treated with placebo and TCV-116 were 0.51±0.07 and 0.21±0.07 mm2, respectively, and this difference was significant. In conclusion, an Ang II antagonist, TCV-116, prevented neointima formation by blocking the action of Ang II generated by both ACE and chymase in the injured arteries.

【 授权许可】

Unknown