更新于：2024-11-21

Guanoxan Sulfate

硫酸胍生

更新于：2024-11-21

概要

概要

基本信息

药物类型

小分子化药

别名

Guanoxan、Guanoxan sulfate (USAN)

+ [2]

靶点

adrenergic receptor

作用机制

adrenergic receptor激动剂(肾上腺素能受体家族激动剂)

治疗领域-

在研适应症-

非在研适应症-

原研机构-

在研机构-

非在研机构-

最高研发阶段批准上市

首次获批日期-

最高研发阶段(中国)-

特殊审评-

登录后查看时间轴

结构

分子式C20H28N6O8S

InChIKeyNSGHAKPGHCNTPS-UHFFFAOYSA-N

CAS号5714-04-5

关联

100 项与硫酸胍生相关的临床结果

登录后查看更多信息

100 项与硫酸胍生相关的转化医学

登录后查看更多信息

100 项与硫酸胍生相关的专利（医药）

登录后查看更多信息

项与硫酸胍生相关的文献（医药）

2001-09-01·Bioorganic & Medicinal Chemistry Letters4区 · 医学

N-Hydroxyl derivatives of guanidine based drugs as enzymatic NO donors

4区 · 医学

Article

作者: Xiaoping Tang ; James J Galligan ; Zhongling Zheng ; Xinchao Chen ; Ming Xian ; Xiaopeng Li ; Peng G Wang ; David L Kreulen

Recent research suggests that NO may play a role in the physiological effects of some guanidine-containing drugs. In this report, three guanidine-containing drugs (guanadrel, guanoxan, and guanethidine) together with their N-hydroxyl derivatives were synthesized and their NO-releasing abilities catalyzed by nitric oxide synthases (NOSs) and horseradish peroxidase were evaluated. The guanidine containing compounds could not release NO in the presence of NOS or peroxidase. The corresponding N-hydroxyl compounds exhibited weak NO-releasing ability under the catalyzed of NOS and good NO-releasing ability under the oxidation by horseradish peroxidase in the presence of H(2)O(2). These compounds also displayed vasodilatory activity.

1994-09-01·European Journal of Pharmacology3区 · 医学

Imidazolines stimulate release of insulin from RIN-5AH cells independently from imidazoline I1 and I2 receptors

3区 · 医学

Article

作者: Kulkarni, Rohit N. ; Olmos, Gabriel ; Haque, Munirul ; MacDermot, John

The effect on insulin release of efaroxan, an alpha 2-adrenoceptor antagonist and a highly potent drug at imidazoline I1 receptors, and the effects of seven other imidazoline compounds selective for the imidazoline I1 or I2 receptors, were studied in the rat insulinoma cell line RIN-5AH. The cells released insulin in response to glucose (0.3-10 mM), and efaroxan (100 microM) potentiated glucose-induced insulin release. (-)-Adrenaline completely displaced the binding of [125I]p-iodoclonidine to membranes of RIN-5AH cells, indicating that these cells do not express imidazoline I1 receptors. Cirazoline and idazoxan (100 microM), both highly potent drugs at imidazoline I2 receptors, and the guanidines guanoxan and amiloride (200 microM), also promoted insulin release from RIN-5AH cells. Irreversible blockade of imidazoline I2 receptors with 10 microM clorgyline did not prevent the stimulatory effects of cirazoline or idazoxan; however, these compounds completely reversed the inhibition by diazoxide (250 microM), an opener of ATP-dependent K+ channels (K+ATP channels), of glucose-induced insulin release. These data indicate that the imidazoline/guanidine compounds promote insulin release from RIN-5AH cells, by interacting with a novel binding site related to K+ATP channels that does not represent any of the known imidazoline I1 or I2 receptors.

1993-08-01·Archives of Biochemistry and Biophysics3区 · 生物学

Competitive Inhibition of Xanthine Oxidase by Guanidinium: Dependence upon Monovalent Anions and Effects on Production of Superoxide

3区 · 生物学

Article

作者: I. Fridovich ; A. Hausladen

Guanidinium chloride inhibits xanthine oxidase competitively with respect to xanthine. Although previously attributed solely to the guanidinium cation, it is now apparent that this inhibition owes much to the counter anion. Thus KCl or KBr, which were not themselves inhibitory, markedly increased the inhibitory potency of guanidinium sulfate. Weak binding of the guanidinium cation evidently creates a binding site for a monovalent anion, whose subsequent binding then stabilizes the binding of the guanidinium. In effect the ion pair is bound to the catalytic center. The proportion of univalent reduction of dioxygen by xanthine oxidase, at fixed concentrations of xanthine and dioxygen and at fixed pH, can be markedly increased by addition of a competitive inhibitor such as guanidinium bromide.

100 项与硫酸胍生相关的药物交易

登录后查看更多信息