Scriabine A, Watson L S, Russo H F, Ludden C T, Sweet C S, Fanelli G M, Bohidar N R, Stone C A
J Pharmacol Exp Ther. 1979 Jan;208(1):148-54.
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.
2-氨甲基-4-(1,1-二甲基乙基)-6-碘苯酚盐酸盐,即MK-447,是一种化学结构新颖的利尿剂,在大鼠、犬和黑猩猩身上产生利尿和促尿盐排泄作用。口服剂量为0.1至10毫克/千克(0.32 - 32微摩尔/千克)时,在增加大鼠和犬的钠、钾和氯排泄方面,MK-447在相同或更高剂量下比呋塞米更有效。单次口服剂量时,MK-447在自发性高血压大鼠和肾性高血压犬中具有降压活性。已知在这些模型中,其他利尿剂只有通过反复给药才能降低动脉血压。吲哚美辛可降低MK-447在自发性高血压大鼠中的降压和利尿作用。