Guanadrel
(Synonyms: 胍环啶) 目录号 : GC49117
An antihypertensive agent
Cas No.:40580-59-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Guanadrel is an antihypertensive agent.1 In vivo, guanadrel (5 mg/kg) inhibits reflex increases in mean arterial and femoral perfusion blood pressures induced by bilateral carotid occlusion in dogs. Formulations containing guanadrel have been used in the treatment of hypertension.
1.Finnerty, F.A., Jr., and Brogden, R.N.Guanadrel. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic use in hypertensionDrugs30(1)22-31(1985)
| Cas No. | 40580-59-4 | SDF | |
| 别名 | 胍环啶 | ||
| Canonical SMILES | N=C(NCC1COC2(CCCCC2)O1)N | ||
| 分子式 | C10H19N3O2 | 分子量 | 213.3 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml | 储存条件 | -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.6882 mL | 23.4412 mL | 46.8823 mL |
| 5 mM | 0.9376 mL | 4.6882 mL | 9.3765 mL |
| 10 mM | 0.4688 mL | 2.3441 mL | 4.6882 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Guanadrel. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic use in hypertension
Drugs 1985 Jul;30(1):22-31.PMID:3896742DOI:10.2165/00003495-198530010-00005.
Guanadrel sulphate is an orally active peripheral sympathetic inhibitor (adrenergic neuron-blocking drug). In comparative studies, Guanadrel was comparable in efficacy with guanethidine or methyldopa in mild to moderately severe hypertension, although generally it caused fewer central nervous system side effects than methyldopa and less orthostatic dizziness and diarrhoea than guanethidine. However, its efficacy in patients whose blood pressure remains inadequately controlled by other drugs (except diuretics alone) has yet to be adequately demonstrated. Guanadrel has a rapid onset of action and a half-life of about 10 hours, thus dose titration can be achieved more rapidly than with guanethidine, and twice daily administration is appropriate. Generally, Guanadrel has been well tolerated, withdrawal of treatment due to adverse effects seldom being necessary. Thus, Guanadrel appears to be a suitable alternative to methyldopa for the treatment of mild to moderately severe hypertension not controlled adequately by diuretics alone.
Guanadrel. A new antihypertensive drug
JAMA 1981 Apr 24;245(16):1639-42.PMID:7206175DOI:10.1001/jama.245.16.1639.
Guanadrel sulfate, a new adrenergic neuron inhibitor similar to guanethidine sulfate, was tested on 199 outpatients by 11 investigators. The patients had mild, moderate, or severe hypertension as determined by diastolic blood pressures of 95 to 105, 106 to 114, and 115 to 120 mm Hg, respectively. Guanadrel was found to be an effective antihypertensive agent for all levels of hypertension. Since Guanadrel has a short onset of action and a short offset of action, which prevents many of the side effects of guanathidine, the dosage could be adjusted rapidly and safely. At low doses side effects are infrequent. There was no organ toxicity and no CNS effect. Guanadrel should be an effective step II or step III drug for treatment of hypertension.
Guanadrel sulfate compared with methyldopa for mild and moderate hypertension
Pharmacotherapy 1982 Nov-Dec;2(6):378-83.PMID:6762533DOI:10.1002/j.1875-9114.1982.tb03215.x.
In a two-year study of 547 hypertensive patients receiving diuretics, the addition of Guanadrel sulfate or methyldopa reduced elevated blood pressure to a similar degree and provided good control in 70% of the patients. Guanadrel-treated patients experienced less frequent and less severe drowsiness than methyldopa-treated patients. The frequency of morning orthostatic faintness was low and similar in both treatment groups. Guanadrel produced no tissue toxicity. Guanadrel sulfate, a postganglionic sympathetic inhibitor, is nearly free of central nervous system side effects and is recommended over methyldopa for step 2 therapy when diuretics alone fail to control mild or moderate hypertension.
Disposition of Guanadrel in subjects with normal and impaired renal function
J Clin Pharmacol 1989 Feb;29(2):128-32.PMID:2715368DOI:10.1002/j.1552-4604.1989.tb03300.x.
The disposition of a single 25 mg oral dose of Guanadrel was evaluated in 22 subjects with various degrees of renal function. The terminal elimination half-life was significantly prolonged in subjects with a creatinine clearance (ClCr) less than 30 mL/min/1.73 m2 (19.2 +/- 16.8 h) compared to 3.7 +/- 1.9 h in subjects with a ClCr greater than 80 mL/min/1.73 m2. Apparent total body clearance (Clp/F) was also progressively lower in the patients with decreased renal function and the decline was significantly correlated with ClCr (Clp/F = 0.0294 + 0.0236 Clcr, r = 0.74, P = 0.002). Renal clearance and apparent nonrenal clearance also declined as creatinine clearance decreased, and both were significantly correlated with the observed ClCr. Apparent volume of distribution averaged 11.5 +/- 8.9 L/kg and did not differ in patients with decreased renal function compared to those with normal renal function. Thus, the disposition of Guanadrel is significantly altered in the presence of renal insufficiency and dosage adjustments may be necessary, especially in patients with ClCr less than 50 ml/min.
Homologous upregulation of human arterial alpha-adrenergic responses by Guanadrel
J Clin Invest 1993 Apr;91(4):1429-35.PMID:8473492DOI:10.1172/JCI116347.
The purpose of this study was to test the hypothesis that there is homologous upregulation of arterial alpha-adrenergic responsiveness during suppression of sympathetic nervous system (SNS) activity in humans. 10 subjects (19-28 yr) were studied during placebo and when SNS activity was suppressed by Guanadrel. Changes in forearm blood flow (FABF) mediated by the intraarterial infusion of norepinephrine (NE), angiotensin II (AII), and phentolamine were measured by plethysmography. During Guanadrel compared with placebo, plasma NE levels (1.28 +/- 0.09-0.85 +/- 0.06 nM; P = 0.0001) and the extra vascular NE release rate derived from [3H]NE kinetics were lower (7.1 +/- 0.7-4.0 +/- 0.2 nmol/min per m2; P = 0.0004), suggesting suppression of SNS activity. During Guanadrel, there was increased sensitivity in the FABF response to NE (analysis of variance P = 0.03). In contrast, there was no difference in the FABF response to AII (analysis of variance P = 0.81), suggesting that the upregulation observed to NE was homologous. The increase in FABF during phentolamine was similar during Guanadrel compared with placebo (Guanadrel: 141 +/- 37 vs. placebo; 187 +/- 27% increase; P = 0.33), suggesting that there was at least partial compensation to maintain constant endogenous arterial alpha-adrenergic tone. We conclude that there is homologous upregulation of arterial alpha-adrenergic responsiveness in humans when SNS activity is suppressed by Guanadrel.