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盐酸2-氨基乙基-4-(1,1-二甲基乙基)-6-碘苯酚(MK-447)的利尿和降压作用

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

作者信息

Scriabine A, Watson L S, Russo H F, Ludden C T, Sweet C S, Fanelli G M, Bohidar N R, Stone C A

出版信息

J Pharmacol Exp Ther. 1979 Jan;208(1):148-54.

PMID:759610
Abstract

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.

摘要

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。

相似文献

1
Diuretic and antihypertensive effects of 2-aminoethyl-4-(1,1-dimethylethyl)-6-iodophenol hydrochloride (MK-447).盐酸2-氨基乙基-4-(1,1-二甲基乙基)-6-碘苯酚(MK-447)的利尿和降压作用
J Pharmacol Exp Ther. 1979 Jan;208(1):148-54.
2
Renal and antihypertensive effects of a novel eukalemic diuretic, ICI 207,828.
J Pharmacol Exp Ther. 1992 Feb;260(2):450-7.
3
Effect of route of administration on the relative efficacy and potency of 2-aminoethyl-4-(1,1-dimethylethyl)-6-iodophenol HCl (MK447) and furosemide.给药途径对盐酸2-氨基乙基-4-(1,1-二甲基乙基)-6-碘苯酚(MK447)和呋塞米相对疗效及效价的影响。
Methods Find Exp Clin Pharmacol. 1990 Sep;12(7):481-6.
4
Physiological disposition and metabolism of 2-aminomethyl-4-(1,1-dimethylethyl)-6-iodophenol hydrochloride.盐酸2-氨甲基-4-(1,1-二甲基乙基)-6-碘苯酚的生理处置与代谢
Drug Metab Dispos. 1979 Sep-Oct;7(5):330-4.
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[Pharmacological and toxicological properties of the saluretic xipamide (4-chloro-5-sulfamoyl-2',6'-salicyloxylidide)].[利尿素氯磺水杨胺(4-氯-5-氨磺酰基-2',6'-水杨酰替苯胺)的药理和毒理学特性]
Arzneimittelforschung. 1975 Feb;25(2):245-51.
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Pharmacological properties of the novel highly potent diuretic 7-chloro-2,3-dihydro-1-(2-methylbenzoyl)-4(1H)-quinolinone 4-oxime-O-sulfonic acid potassium salt.新型高效利尿剂7-氯-2,3-二氢-1-(2-甲基苯甲酰基)-4(1H)-喹啉酮4-肟-O-磺酸酸钾盐的药理特性
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The diuretic response in normal volunteers to a new benzylamine, 2-aminomethyl-4-(1,1-dimethylethyl)-6-iodophenol HCl.正常志愿者对一种新的苄胺(2-氨甲基-4-(1,1-二甲基乙基)-6-碘苯酚盐酸盐)的利尿反应。
J Clin Pharmacol. 1978 Aug-Sep;18(8-9):414-24. doi: 10.1002/j.1552-4604.1978.tb02458.x.
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Micropuncture evaluation of the site of action of 2-aminomethyl-4-(1,1-dimethylethyl)-6-iodophenol hydrochloride (MK447) in the rat kidney.
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Comparative cardiovascular effects of loop-acting, thiazide-type and potassium-sparing diuretics in spontaneously hypertensive rats.
Methods Find Exp Clin Pharmacol. 1987 Feb;9(2):67-78.
10
Renal tubular secretion and effects of the alkaline diuretics amiloride, tizolemide (Hoe 740) and 2-aminomethyl-4(1,1-dimethylethyl)-6-iodophenol hydrochloride (MK-447).肾小管分泌以及碱性利尿剂阿米洛利、替唑利米(Hoe 740)和盐酸2-氨甲基-4-(1,1-二甲基乙基)-6-碘苯酚(MK-447)的作用
Naunyn Schmiedebergs Arch Pharmacol. 1981;317(4):357-63. doi: 10.1007/BF00501319.

引用本文的文献

1
Renal tubular secretion and effects of the alkaline diuretics amiloride, tizolemide (Hoe 740) and 2-aminomethyl-4(1,1-dimethylethyl)-6-iodophenol hydrochloride (MK-447).肾小管分泌以及碱性利尿剂阿米洛利、替唑利米(Hoe 740)和盐酸2-氨甲基-4-(1,1-二甲基乙基)-6-碘苯酚(MK-447)的作用
Naunyn Schmiedebergs Arch Pharmacol. 1981;317(4):357-63. doi: 10.1007/BF00501319.
2
Diuretics. Clinical pharmacology and therapeutic use (Part I).利尿剂。临床药理学与治疗应用(第一部分)
Drugs. 1985 Jan;29(1):57-87. doi: 10.2165/00003495-198529010-00003.