FK453: A novel non-xanthine adenosine A(1) receptor antagonist as diuretic

被引：5

作者：

Terai, T ^{[1
]}

Kusunoki, T ^{[1
]}

Kita, Y ^{[1
]}

Akahane, A ^{[1
]}

Shiokawa, Y ^{[1
]}

Kohno, Y ^{[1
]}

Horiai, H ^{[1
]}

Uehara, Y ^{[1
]}

Yoshida, K ^{[1
]}

机构：

[1] UNIV TOKYO,DEPT MED 2,TOKYO,JAPAN

来源：

CARDIOVASCULAR DRUG REVIEWS | 1997年 / 15卷 / 01期

关键词：

acute renal failure; adenosine antagonist; diuretic; FK453; hypertension;

D O I：

10.1111/j.1527-3466.1997.tb00323.x

中图分类号：

R5 [内科学];

学科分类号：

1002 ; 100201 ;

摘要：

FK453 is a novel pyrazolopyridine derivative. The data presented in this review demonstrate that it is a potent, orally active, and highly selective antagonist for the adenosine A1 receptor subtype. FK453 has diuretic, uricosuric, and renal vasodilator activities in normal animals and antihypertensive activity in DOCA-saline hypertensive rats. FK453 reduces the severity of gentamicin-, cisplatin-, or glycerol-induced acute renal failure in rats. It has little effect on the central nervous, gastrointestinal, or hematological systems. There were no serious toxicological findings and no serious adverse events in healthy human volunteers. FK453 produced dose-dependent diuretic, natriuretic, and uricosuric effects in healthy human subjects and in patients with essential hypertension. In hypertensive patients, FK453 decreased blood pressure. FK453 is, therefore, a promising theraputic agent for the treatment of hypertension and renal failure.

引用

页码：44 / 58

页数：15

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