Amiloride hydrochloride dihydrate

Amiloride hydrochloride dihydrate (MK-870 hydrochloride dihydrate) is an inhibitor of both epithelial sodium channel (ENaC^[1]) and urokinase-type plasminogen activator receptor (uTPA^[2]). Amiloride hydrochloride dihydrate is a blocker of polycystin-2 (PC2; TRPP2^[3]) channel. IC50 & Target: ENaC^[1]; uTPA^[2]; polycystin-2(TRPP2)^[3] In Vivo: Amiloride hydrochloride dihydrate is a potent epithelial sodium channels (ENaCs) blocker. Amiloride is highly concentrated in the plasma 15 to 30 minutes following the injections. 2 mg/kg dose of Amiloride hydrochloride dihydrate has no effect on blood pressure, heart rate, mesenteric vascular resistance, or hindquarters vascular resistance as compare to the baseline measurements (n=7). Over a 2 hour period, Amiloride hydrochloride dihydrate elicits negligible responses in arterial pressure (-1±1 mmHg) and heart rate (-10±6 bpm/min) as compare to baseline levels. Results show an Amiloride hydrochloride dihydrate dose-related response pattern for the c-Fos activation in the area postrema (AP). Even at the lowest dose of Amiloride hydrochloride dihydrate (0.1 mg/kg), the number of c-Fos labeled neurons in the AP is statistically different from the control rats at a p<0.01 level^[1].