Disease relevance of D00400

• Valsartan (Diovan, Novartis) is one of the seven currently approved ARBs in the USA for the treatment of hypertension, and it has been shown to be very effective in controlling blood pressure given once-daily in doses of 80-160 or 320 mg [1].
• Eighty patients with cirrhosis and portal hypertension were divided in two groups as follows: group I - 40 patients who received valsartan (Diovan) 80 mg /day for 7 days and group II - 40 patients who received placebo [2].
• The hemodynamic effects of valsartan ((S)-N-valeryl-N-¿[2'-(1H-tetrazol-5-yl)bipheneoyl-4-yl]meth yl¿valine, CAS 137862-53-4, CGP 48933), a new angiotensin II type 1 receptor antagonist, on rats with myocardial infarction induced by coronary artery ligation was examined [3].
• Parts 1 and 2 comprised a double-masked intraindividual trial between CGP 48933 and its vehicle (saline) in five healthy volunteers (Part 1) and five patients with early stages of primary open-angle glaucoma (Part 2), to assess local tolerance and the effect on IOP [4].

High impact information on D00400

• Low concentrations of the subtype AT1-receptor antagonist CGP 48933, but not the subtype AT2-receptor antagonist CGP 42112, blocked AII-induced SMC migration [5].
• Benazepril, an ACEi, facilitated matrix degradation via the bradykinin (BK) B2 receptor on tubular epithelial cells in the kidney, whereas CGP-48933, an ARB, did not [6].
• AIM: Two formulations of valsartan (Diovan), 320 mg tablets and marketed 160 mg capsules, were evaluated for bioequivalence after single dosing [7].
• SARILE blocked completely the pressor response to [Asp1, Val5]-ANG II but the AT1 antagonists losartan and CGP 48933 and the AT2 antagonist PD 123319 all failed to block the pressor response to [Asp1, Val5]-ANG II [8].
• This study was conducted to determine the tolerability and efficacy of valsartan (DIOVAN) compared to perindopril (COVERSYL) in Malaysian patients with mild to moderate hypertension [9].

Biological context of D00400

• A new angiotensin-II- receptor blocker, CGP 48933: local tolerance and effect on intraocular pressure. A pilot study [4].

Associations of D00400 with other chemical compounds

• METHODS AND RESULTS: Accordingly, atrial and ventricular myocardial electrophysiological properties were examined in adult rat (n = 13) and guinea pig (n = 9) myocardial preparations in the presence of the specific AT1 Ang II receptor antagonist, valsartan (CGP 48933; 0.5, 5, or 500 mumol/L) [10].

Gene context of D00400

• PD completely blocked the chronic hypotensive response to the combination of Ang II and VAL to control levels before VAL administration [11].

References