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Biological evaluation of a novel angiotensin II AT_1 receptor antagonist with anti-hypertensive and anti-tumor effects

机译:新型血管紧张素II AT_1受体拮抗剂与抗高血压和抗肿瘤作用的生物学评价

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A novel nonpeptide angiotensin II receptor 1 antagonist, compound 1, N-butyryl-N-[(2'-(2, 5-dihydro-5-oxo-l, 2, 4-oxadiazol-3-yl) biphenyl-4-yl) methyl] -L-Valine was investigated by receptor-binding studies and vivo experiments in spontaneously hypertensive rats and renal hypertensive rats. Furthermore, treatment with compound 1 significantly inhibited the viability of human breast cancer cell line and promoted apoptosis of the cancer cells. The compound had the effects of anti-hypertension and anti-cancer, which suggested that this new compound could be considered as a candidate for both novel anti-hypertensive and anti-cancer agent.
机译:一种新型非肽血管紧张素II受体1拮抗剂,化合物1,N-丁酰基-N-[(2' - (2,5-二氢-5-氧代-1,2,4-恶二唑-3-基)联苯-4-通过受体结合研究和体内实验研究了甲基] -L-缬氨酸在自发性高血压大鼠和肾高血压大鼠中进行了体内实验。此外,用化合物1处理显着抑制人乳腺癌细胞系的生存力并促进癌细胞的凋亡。该化合物具有抗高血压和抗癌的影响,这表明这种新化合物可以被认为是新型抗高血压和抗癌剂的候选者。

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