Cadralazine

产品说明书

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Chemical Structure| 64241-34-5 同义名 : -
CAS号 : 64241-34-5
货号 : A267563
分子式 : C12H21N5O3
纯度 : 95%
分子量 : 283.33
MDL号 : MFCD00865833
存储条件:

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Cadralazine is a new, orally effective antihypertensive vasodilator. The doses which reduce systolic blood pressure by 25% (ED25) are very similar after oral and intravenous administration (spontaneously hypertensive rats, 1.8 mg/kg, p.o.; 2.3 mg/kg, i.v.; renal hypertensive dogs, 0.26 mg/kg, p.o.; 0.24 mg/kg, i.v.; awake normotensive dogs, 0.98 mg/kg, p.o.; 1.01 mg/kg, i.v.). Cadralazine reverses hypertensive responses to epinephrine in awake normotensive dogs and anesthetized cats. The inhibition of the increase in blood pressure induced by sympathetic outflow activation in pithed rats parallels the antihypertensive activity in onset, intensity, and duration[3]. Cadralazine given i.v. (1 mg/kg) caused a sustained fall in total peripheral vascular resistances and mean blood pressure (from 103 to 90 mmHg) and an increase in heart rate (from 97 to 161 beats/min)[4]. Oral administration of 0.5 mg/kg or more of cadralazine depressed spontaneous motor activity and enhanced electroshock-induced convulsions in mice. The drug produced flush on the tail or ears at 0.5 mg/kg, p.o. or more and enhanced respiratory movement at 5.0 mg/kg, p.o. or more in rats. At 2.5 mg/kg, p.o., cadralazine prolonged the thiopental-sleeping time and inhibited methamphetamine-induced hypermotility as well as acetic acid-induced writhing in mice. Cadralazine at 5.0 mg/kg, p.o., lowered body temperature in rats[5]. Cadralazine at 2.5 mg/kg, p.o., or more reduced or tended to reduce urine volume and urinary excretion of electrolytes. Cadralazine at 5.0 mg/kg, p.o. or more antagonized carrageenin-induced hind paw edema in rats[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.53mL

0.71mL

0.35mL

17.65mL

3.53mL

1.76mL

35.29mL

7.06mL

3.53mL

参考文献

[1]McTavish D, Young RA, et al. Cadralazine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in the treatment of hypertension. Drugs. 1990 Oct;40(4):543-60.

[2]Takeyama K, Ikeno A, et al. Antihypertensive activity of cadralazine in experimental hypertensive rats. Arch Int Pharmacodyn Ther. 1988 Jan-Feb;291:163-74.

[3]Semeraro C, Dorigotti L, Banfi S, Carpi C. Pharmacological studies on cadralazine: a new antihypertensive vasodilator drug. J Cardiovasc Pharmacol. 1981 May-Jun;3(3):455-67

[4]Dorigotti L, Ferni G, Lombroso M, Semeraro C. Hemodynamic profile of the antihypertensive vasodilator cadralazine in conscious dogs. Arzneimittelforschung. 1984;34(9):984-7

[5]Nishimori T, Morino K, Tsuchiyama M, Ikeda H, Hasegawa K, Higashio T, Akita S, Yamauchi T, Nakao K, Inukai T. [Effects of cadralazine on the central nervous system]. Nihon Yakurigaku Zasshi. 1988 Apr;91(4):209-20. Japanese

[6]Nishimori T, Nishimura T, Kobayashi F, Nakano D, Fukuda Y, Sakonjyo H, Nakanishi J, Kimura A, Tsuji H, Higashio T, et al. [Effects of cadralazine on the respiration, circulation, kidney, autonomic nervous system, digestive system, blood and so on]. Nihon Yakurigaku Zasshi. 1988 Apr;91(4):221-36. Japanese