Debrisoquin (hemisulfate)
(Synonyms: 硫酸异喹胍) 目录号 : GC46126
A post-ganglionic sympathetic blocker
Cas No.:581-88-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Debrisoquin is a post-ganglionic sympathetic blocker.1 It increases accumulation of the monoamine oxidase (MAO) substrate l-m-octopamine in isolated rabbit heart when used at a concentration of 1 mM.2 Debrisoquin reduces norepinephrine levels in the left and right atrium and ventricles, as well as the mesenteric and femoral arteries in anesthetized dogs when administered at a dose of 5 mg/kg per day for seven days.3 Debrisoquin decreases mean aortic pressure, heart rate, and total peripheral vascular resistance in the same model.
|1. Heffernan, A.G.A., and Carty, A.T. Clinical observations on the use of debrisoquine sulphate (declinax) in the treatment of hypertension. I. J. Med. Sc. 3(1), 37-43 (1970).|2. Giachetti, A., and Shore, P.A. Monoamine oxidase inhibition in the adrenergic neuron by bretylium, debrisoquin, and other adrenergic neuronal blocking agents. Biochem. Pharmacol. 16, 237-238 (1966).|3. Cavero, I., Gerold, M., Saner, A., et al. The cardiovascular effects of the antihypertensive drug debrisoquin: A contribution to the pharmacology of chronic treatment. I. one-week administration to dogs. J. Pharmacol. Exp. Ther. 206(1), 123-131 (1978).
| Cas No. | 581-88-4 | SDF | |
| 别名 | 硫酸异喹胍 | ||
| Canonical SMILES | NC(N1CCC2=CC=CC=C2C1)=N.O=S(O)(O)=O | ||
| 分子式 | C10H13N3 • 1/2H2SO4 | 分子量 | 224.3 |
| 溶解度 | PBS (pH 7.2): 1 mg/ml | 储存条件 | Store at -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 | 4.4583 mL | 22.2916 mL | 44.5831 mL |
| 5 mM | 0.8917 mL | 4.4583 mL | 8.9166 mL |
| 10 mM | 0.4458 mL | 2.2292 mL | 4.4583 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。
3,4-Dehydrodebrisoquine, a novel debrisoquine metabolite formed from 4-hydroxydebrisoquine that affects the CYP2D6 metabolic ratio
Drug Metab Dispos 2006 Sep;34(9):1563-74.PMID:16782768DOI:PMC1553181
Considerable unexplained intersubject variability in the debrisoquine metabolic ratio (urinary debrisoquine/4-hydroxydebrisoquine) exists within individual CYP2D6 genotypes. We speculated that debrisoquine was converted to as yet undisclosed metabolites. Thirteen healthy young volunteers, nine CYP2D6*1 homozygotes [extensive metabolizers (EMs)] and four CYP2D6*4 homozygotes [poor metabolizers (PMs)] took 12.8 mg of debrisoquine hemisulfate by mouth and collected 0- to 8- and 8- to 24-h urines, which were analyzed by gas chromatography-mass spectrometry (GCMS) before and after treatment with beta-glucuronidase. Authentic 3,4-dehydrodebrisoquine was synthesized and characterized by GCMS, liquid chromatography-tandem mass spectrometry, and (1)H NMR. 3,4-Dehydrodebrisoquine is a novel metabolite of debrisoquine excreted variably in 0- to 24-h urine, both in EMs (3.1-27.6% of dose) and PMs (0-2.1% of dose). This metabolite is produced from 4-hydroxydebrisoquine in vitro by human and rat liver microsomes. A previously unstudied CYP2D6*1 homozygote was administered 10.2 mg of 4-hydroxydebrisoquine orally and also excreted 3,4-dehydrodebrisoquine. EMs excreted 6-hydroxydebrisoquine (0-4.8%) and 8-hydroxydebrisoquine (0-1.3%), but these phenolic metabolites were not detected in PM urine. Debrisoquine and 4-hydroxydebrisoquine glucuronides were excreted in a highly genotype-dependent manner. A microsomal activity that probably does not involve cytochrome P450 participates in the further metabolism of 4-hydroxydebrisoquine, which we speculate may also lead to the formation of 1- and 3-hydroxydebrisoquine and their ring-opened products. In conclusion, this study suggests that the traditional metabolic ratio is not a true measure of the debrisoquine 4-hydroxylation capacity of an individual and thus may, in part, explain the wide intragenotype variation in metabolic ratio.