Key result
Compound 1, a novel AT1 receptor antagonist, demonstrated high affinity (IC50 1.65 nM) and reduced blood pressure for over 12 hours at 10 mg/kg in spontaneously hypertensive rats.
Why the study?
Does novel compound 1 reduce blood pressure and exhibit anti-tumor effects in preclinical models?
Does novel compound 1 reduce blood pressure and exhibit anti-tumor effects in preclinical models?
A novel AT1 receptor antagonist demonstrates promising anti-hypertensive and anti-tumor effects in preclinical models.
May support further preclinical development of novel AT1 antagonists; leaves open human translation and clinical efficacy.
A new compound 2-(4-((2-butyl-5-nitro-1H-benzo[d]imidazol-1-yl)methyl)-1H-indol-1-yl) benzamide (1) was designed, synthesized and evaluated as a novel AT1 receptor antagonist. Compound 1 displayed high affinity to AT1 receptor with an IC50 value of 1.65 ± 0.2 nM in radio-ligand binding assays. It had an efficient and long-lasting effect in reducing blood pressure which could last for more than 12 h at the dose of 10 mg/kg in spontaneously hypertensive rats. Acute toxicity tests suggested that compound 1 was safe with the LD50 value of 2519.81 mg/kg. Besides, in vitro and in vivo tests suggested its anti-proliferative and anti-tumor activities, respectively. So compound 1 could be considered as a novel anti-hypertension, anti-tumor candidate and deserved further investigation.
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Bao et al. (2015) studied Hypertension and tumor. Compound 1 (2-(4-((2-butyl-5-nitro-1H-benzo[d]imidazol-1-yl)methyl)-1H-indol-1-yl) benzamide) was evaluated on Blood pressure reduction and AT1 receptor affinity. Compound 1, a novel AT1 receptor antagonist, demonstrated high affinity (IC50 1.65 nM) and reduced blood pressure for over 12 hours at 10 mg/kg in spontaneously hypertensive rats.
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