Quinidine
(Synonyms: 奎尼丁) 目录号 : GC14264An antiarrhythmic agent
Cas No.:56-54-2
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
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- SDS (Safety Data Sheet)
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Animal experiment: |
Rats: Three rats are placed in individual metabolic cages with free access to food and water. After 24 h, urine is collected (0 h) and the rats receive the following treatment: (1) no treatment; (2) 80 mg quinidine/kg (po) at 1.0 mL/kg, and (III) 50% ethanol (1.0 mL/kg). Two hours later, all three rats receive a single dose of 15 mg amphetamine/kg (po) at 1.0 mL/kg. Urine is then collected at 24 and 48 h after the administration of quinidine. This procedure is repeated three times. After collection of urine, volume and pH are measured and the urine is stored until analysis[3]. |
References: [1]. Kehl SJ, et al. Quinidine-induced inhibition of the fast transient outward K+ current in rat melanotrophs. Br J Pharmacol. 1991 Jul;103(3):1807-13. |
Quinidine is an antiarrhythmic agent for the treatment of abnormal heart rhythms and also malaria.
Quinidine is a clinical anti-arrythmic drug which affects ionic currents in heart muscle and which has also been shown to be a potent blocker of several classes of K+ channel in a variety of cell types. Bath application of quinidine causes a dose-dependent reduction of the peak amplitude of Ik. The Kd for blockade of Ik at 0 mV is estimated to be 41 μM. Quinidine elicits a dose-dependent increase of the rate of the decay of Ik and this effect is enhanced by membrane depolarization. Quinidine also causes a 5 mV hyperpolarizing shift of the steady-state inactivation curve and increases the half-time for recovery from inactivation. Quinidine does not affect the onset of inactivation measured at -30 mV[1].
Quinidine sulfate is rapidly absorbed, with peak plasma concentrations 60-90 min after an oral dose. Other salts (gluconate, polygalacturonate) are more slowly absorbed, with lower peak concentrations. Quinidine is approximately 70-90 % bound to plasma proteins. It undergoes hepatic oxidative metabolism to form an N-oxide, a 3-hydroxy form, an O-demethyl form and 2'-quinidinone. Over one-half of patients starting quinidine stop within the first year of therapy because of side effects. These include, commonly, diarrhea, nausea, and vomiting which are not necessarily related to high plasma concentrations[2]. Quinidine inhibits metabolism of amphetamine in rats. Quinidine pretreatment results in a significant decrease in the excretion of p-hydroxyamphetamine at 24 and 48 h to 7.2 and 24.1% of the vehicle-control levels, respectively, accompanied by a significant increase in amphetamine excretion between 24 and 48 h to 542% of the control[3].
References:
[1]. Kehl SJ, et al. Quinidine-induced inhibition of the fast transient outward K+ current in rat melanotrophs. Br J Pharmacol. 1991 Jul;103(3):1807-13.
[2]. Roden DM, et al. Class I antiarrhythmic agents: quinidine, procainamide and N-acetylprocainamide, disopyramide.
[3]. Moody DE, et al. Quinidine inhibits in vivo metabolism of amphetamine in rats: impact upon correlation between GC/MS and immunoassay findings in rat urine. J Anal Toxicol. 1990 Sep-Oct;14(5):311-7.
Cas No. | 56-54-2 | SDF | |
别名 | 奎尼丁 | ||
化学名 | (R)-(6-methoxyquinolin-4-yl)((1S,2R,4S,5S)-5-vinylquinuclidin-2-yl)methanol | ||
Canonical SMILES | O[C@H](C(C1=C2)=CC=NC1=CC=C2OC)[C@@H]3[N@@]4C[C@@H](C=C)[C@@H](CC4)C3 | ||
分子式 | C20H24N2O2 | 分子量 | 324.42 |
溶解度 | ≥ 11.95mg/mL in DMSO | 储存条件 | 4°C, protect from light, stored under nitrogen |
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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.0824 mL | 15.4121 mL | 30.8242 mL |
5 mM | 0.6165 mL | 3.0824 mL | 6.1648 mL |
10 mM | 0.3082 mL | 1.5412 mL | 3.0824 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 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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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。
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