Diuretic and antihypertensive effects of 2-aminoethyl-4-(1,1- dimethylethyl)-6-iodophenol hydrochloride (MK-447)

A Scriabine, LS Watson, HF Russo, CT Ludden, CS Sweet, GM Fanelli , NR Bohidar and CA Stone

2-Aminomethyl-4-(1,1-dimethylethyl)-6-iodophenol hydrochloride or MK- 447, is a chemically novel diuretic agent which produced diuretic and saluretic effects in rats, dogs and chimpanzees. At doses ranging from 0.1 to 10 mg/kg p.o. (0.32-32 mumol/kg) MK-447 was more effective then furosemide at the same or higher doses in increasing the excretion of Na+, K+ and Cl- in rats and dogs. At single oral doses, MK-447 had antihypertensive activity in spontaneously hypertensive rats and renal hypertensive dogs. Other diuretics are known to lower arterial pressure in these models only by repeated administration. The antihypertensive and diuretic effects of MK-447 in spontaneously hypertensive rats were reduced by indomethacin.

Volume 208, Issue 1, pp. 148-154, 01/01/1979
Copyright © 1979 by American Society for Pharmacology and Experimental Therapeutics