Threo-methylphenidate hydrochloride
(Synonyms: 盐酸哌甲酯) 目录号 : GC17047
盐酸苏哌甲酯(Threo-methylphenidate hydrochloride)是一种儿茶酚胺再摄取抑制剂,抑制多巴胺转运蛋白(DAT)和去甲肾上腺素转运蛋白(NET)。
Cas No.:298-59-9
Sample solution is provided at 25 µL, 10mM.
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Threo-methylphenidate hydrochloride is a catecholamine reuptake inhibitor that inhibits dopamine transporter (DAT) and norepinephrine transporter (NET)[1]. Threo-methylphenidate hydrochloride is used to treat attention deficit hyperactivity disorder (ADHD)[2]. Threo-methylphenidate hydrochloride has central nervous system excitability and sympathomimetic effects, and can also affect the cardiovascular system[3].
In vitro, when glial cells were treated with Threo-methylphenidate hydrochloride (100µM, 30 min), a significant increase in [3H]-D-Asp was detected after 2 hours, and this effect persisted after 12hours[4]. The concentration range of Threo-methylphenidate hydrochloride that inhibits NET in HEK293 cells is 0.04-0.42µM, and the concentration range that inhibits DAT is 0.08-0.34µM[5].
In vivo, Threo-methylphenidate hydrochloride(30mg/kg) caused a shortening of the QT interval in the electrocardiogram of beagle dogs and an increase in blood pressure[3]. Threo-methylphenidate hydrochloride(10mg/kg, o.p.) may reduce urine flow and glomerular filtration rate in Wistar rats, but has no harmful effect on renal tubules[6].Threo-methylphenidate hydrochloride(4 mg/kg) increased the anticipatory response of zebrafish in a 5-choice series response task and also increased the overall activity level of the experimental group [7].
References:
Markowitz J S , Patrick K S. Differential Pharmacokinetics and Pharmacodynamics of Methylphenidate Enantiomers[J]. Journal of Clinical Psychopharmacology, 2008, 28: 54-61.
[2]Heal D J , Pierce D M .Methylphenidate and its Isomers: Their Role in the Treatment of Attention-Deficit Hyperactivity Disorder Using a Transdermal Delivery System[J].Cns Drugs, 2006, 20(9):713-738.
[3]Wakamatsu A , Nomura S , Tate Y ,et al. Effects of methylphenidate hydrochloride on the cardiovascular system in vivo and in vitro: A safety pharmacology study[J].Journal of Pharmacological & Toxicological Methods, 2009, 59(3):128-134.
[4]A M. Guillem, Z Martı´nez-Lozada, L C. Herna´ndez-Kell, et al. Methylphenidate Increases Glutamate Uptake in Bergmann Glial Cells[J]. Neurochem Res. 2015(40):2317-2324.
[5]Luethi, D.K., Philine J.Brandt, Simon D. K, et al. Pharmacological profile of methylphenidate-based designer drugs[J].Neuropharmacology, 2018, 134.
[6]Luiza Herbene Macedo Soares Salviano,et al. Study of the safety of methylphenidate: Focus on nephrotoxicity aspects[J].Life Sciences. 2015:137-142.
[7]Parker M O , Brock A J , Sudwarts A ,et al.Atomoxetine reduces anticipatory responding in a 5-choice serial reaction time task for adult zebrafish[J].Psychopharmacology, 2014, 231(13):2671.
盐酸苏哌甲酯(Threo-methylphenidate hydrochloride)是一种儿茶酚胺再摄取抑制剂,抑制多巴胺转运蛋白(DAT)和去甲肾上腺素转运蛋白(NET)[1]。盐酸苏哌甲酯用于治疗注意力缺陷多动障碍(ADHD)[2]。盐酸苏哌甲酯具有中枢神经系统兴奋和拟交感神经作用,还可影响心血管系统[3]。
在体外,盐酸苏哌甲酯(100 µM,30min)处理神经胶质细胞,2小时后检测到[3H]-D-Asp显著增加,并且该作用在12小时后仍然存在[4]。盐酸苏哌甲酯在HEK293细胞中抑制NET的浓度范围为0.04-0.42 µM,抑制DAT 的浓度范围为0.08-0.34 µM[5]。
在体内,盐酸苏哌甲酯(30mg/kg)导致比格犬心电图的QT间期缩短,出现血压升高[3]。盐酸苏哌甲酯(10mg/kg, o.p.)可能会降低Wistar大鼠尿流量和肾小球滤过率,对肾小管没有危害作用[6]。盐酸苏哌甲酯(4 mg/kg)增加了斑马鱼在5选择系列反应任务中的预期反应,还使实验组的总体活动水平增加[7]。
| Cell experiment [1]: | |
|
Cell lines |
Bergmann glial cells |
|
Preparation Method |
Cells were incubated for 30min with 100µM Threo-methylphenidate hydrochloride. |
|
Reaction Conditions |
100µM; 30min |
|
Applications |
when the cultured cells were treated with 100µM Threo-methylphenidate hydrochloride, a significant increase in [3H]-D-Asp was detected as early as 2h after Threo-methylphenidate hydrochloride and the effect was still present after 12 h. |
| Animal experiment [2]: | |
|
Animal models |
adult male Wistar rats |
|
Preparation Method |
determine the biochemical renal parameters at 24 h and 48 h after administration of Threo-methylphenidate. The animals were randomized into two groups: Threo-methylphenidate (10 mg/kg) and control group (aqueous solution). The drug was orally administered (gavage).The animals were kept in metabolic cages in the last 24 h of the experiment, after which their urine was collected. |
|
Dosage form |
10 mg/kg; 24 h and 48 h; p.o. |
|
Applications |
Threo-methylphenidate hydrochloride may have interfered with the vasodilator effect of prostaglandins, since it reduced the urinary flow and glomerular filtration rate. But Threo-methylphenidate hydrochloride did not have harmful effect on this organ, mainly, on the renal tubules. |
|
References: [1] A M. Guillem, Z Martı´nez-Lozada, L C. Herna´ndez-Kell, et al. Methylphenidate Increases Glutamate Uptake in Bergmann Glial Cells[J]. Neurochem Res. 2015(40):2317-2324. | |
| Cas No. | 298-59-9 | SDF | |
| 别名 | 盐酸哌甲酯 | ||
| 化学名 | (S)-methyl 2-phenyl-2-((S)-piperidin-2-yl)acetate hydrochloride | ||
| Canonical SMILES | O=C([C@@H](C1=CC=CC=C1)[C@H]2NCCCC2)OC.Cl | ||
| 分子式 | C14H19NO2.HCl | 分子量 | 269.77 |
| 溶解度 | <13.49mg/ml in Water; <26.98mg/ml in ethanol | 储存条件 | Store at RT |
| 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 | 3.7069 mL | 18.5343 mL | 37.0686 mL |
| 5 mM | 0.7414 mL | 3.7069 mL | 7.4137 mL |
| 10 mM | 0.3707 mL | 1.8534 mL | 3.7069 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet