Valsartan CAS No.137862-53-4

Valsarta (CGP-48933) is an angiotensin II receptor antagonist used to treat hypertension and heart failure.

Related Categories
Signal Pathways >> G Protein-Coupled Receptors/G Proteins >> Angiotensin Receptors
Research Areas >> Cardiovascular Diseases

In vitro studies Valsartan is a synthetic non-peptide angiotensin II type 1 receptor antagonist that dilates blood vessels and lowers blood pressure by blocking the action of angiotensin. Valsartan significantly reduces the expression of AT1R in aged aortic endothelial cells [1]. Valsartan pretreatment leads to inhibition of TLR2 signaling and pro-inflammatory cytokines. AGTR1 expression is upregulated after alcohol exposure and is blocked by valsartan pretreatment [2].

In vivo studies Valsartan significantly attenuates the expression of TGF-β/Smad, Hif-1α, and fibrosis-related proteins in rats after MI. Compared with saline and hydralazine, valsartan also significantly improves cardiac function, infarct area, wall thickness, and myocardial vascularization in ischemic hearts [3]. Valsartan partially reverses the effects of a high-salt diet on cardiac damage such as hypertension, fibrosis, and inflammatory cell infiltration, as well as the inhibition of aquaporin 1 and angiogenic factors; valsartan alone does not produce such effects [4]. Valsartan is an effective antidepressant/anxiety agent that promotes hippocampal neurogenesis and BDNF expression. Chronic administration of valsartan (5–40 mg/kg/day, po) increases the time spent in the OFT center and the latency to feed in the NSF, reduces the immobility time in the TST and FST, and increases the preference in the sucrose SPT [5]. Animal Experiments Rats: Rats were randomly divided into two groups: (i) valsartan treatment group, which received 3 mg/kg/day of valsartan intravenously in 0.5 mL of normal saline for 1 week; (ii) hydralazine treatment group, which received 0.2 mg/kg/day of hydralazine in saline; and (iii) control group, which received saline in the same manner (n = 15 in each group) [4]. Mice: Valsartan was dissolved in water containing 0.5% methylcellulose solution. Valsartan (5–40 mg/kg/day) was administered orally (po) at a volume of 10 mL/kg body weight using tube feeding. Potential changes in blood pressure in response to long-term treatment with valsartan were assessed using a commercially designed blood pressure analysis system. Mice were trained to the device for at least two consecutive days prior to the start of the study. To record blood pressure, mice were placed on a heated pad (35°C) and measured in steady state using a programmable tail-cuff sphygmomanometer. The average of 10 readings for each mouse was recorded [5].