Tipepidine hydrochloride
目录号 : GC38391
Tipepidine hydrochloride 可逆地抑制多巴胺 D2 受体介导的 GIRK 电流 (IDA(GIRK))，从而激活 VTA 多巴胺神经元， 对 IDA(GIRK) 的 IC50 为 7.0 μM。Tipepidine hydrochloride 是一种非麻醉性镇咳药，具有抗抑郁样作用。
Cas No.:1449686-84-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Tipepidine hydrochloride reversibly inhibits dopamine (DA) D2 receptor-mediated GIRK currents (IDA(GIRK)) with an IC50 of 7.0 μM. Tipepidine hydrochloride subsequently activates VTA dopamine neuron[1]. Tipepidine hydrochloride, a non-narcotic antitussive, exerts an antidepressant-like effect[2].
Tipepidine (i.p.; 10-40 mg/kg; 0.5-23 hours) significantly decreases the immobility time in the forced swimming test in ACTH-treated rats. Tipepidine (i.p.; 40 mg/kg) increases the extracellular dopamine level of the nucleus accumbens (NAc) in ACTH-treated rats[2]. Animal Model: Male Wistar rats weighting 150-240 g (5-7 weeks old) [2]
[1]. Hamasaki R, et al. Tipepidine activates VTA dopamine neuron via inhibiting dopamine D? receptor-mediated inward rectifying K? current. Neuroscience. 2013 Nov 12;252:24-34. [2]. Kawaura K, et al. Tipepidine, a non-narcotic antitussive, exerts an antidepressant-like effect in the forced swimming test in adrenocorticotropic hormone-treated rats. Behav Brain Res. 2016 Apr 1;302:269-78.
| Cas No. | 1449686-84-3 | SDF | |
| Canonical SMILES | CN1C/C(CCC1)=C(C2=CC=CS2)\C3=CC=CS3.[H]Cl | ||
| 分子式 | C15H18ClNS2 | 分子量 | 311.89 |
| 溶解度 | DMSO: 41.67 mg/mL (133.60 mM) | 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 | 3.2063 mL | 16.0313 mL | 32.0626 mL |
| 5 mM | 0.6413 mL | 3.2063 mL | 6.4125 mL |
| 10 mM | 0.3206 mL | 1.6031 mL | 3.2063 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。
Beyond stimulants: a systematic review of randomised controlled trials assessing novel compounds for ADHD
Expert Rev Neurother 2019 Jul;19(7):707-717.PMID:31167583DOI:10.1080/14737175.2019.1628640.
Introduction: Despite stimulants being highly efficacious in short-term randomized controlled trials (RCTs), not all patients respond or can successfully tolerate them. A number of novel non-stimulant options are currently in the pipeline for the treatment of attention-deficit/hyperactivity disorder (ADHD). Areas covered: The authors conducted a systematic review of RCTs registered in ClinicalTrials.gov in the past 5 years (January 2014 and February 2019), supplemented by searches in PubMed, Web of Science, and drug manufacturer websites to find recent RCTs on novel non-stimulant ADHD medications. Expert opinion: The authors found 28 pertinent RCTs of compounds acting on a variety of biological targets, including Dasotraline, Viloxazine (SPN-812), Centanafadine SR (CTN SR), OPC-64005, Fasoracetam (NFC-1, AEVI-001), Metadoxine (MDX), Vortioxetine, Tipepidine Hibenzate, Oxytocin, Sativex (delta-9-tetrahydrocannabinol (THC) plus cannabidiol), Mazindol, and Molindone hydrochloride (SPN-810). Given the high effect size found in RCTs of stimulants in terms of efficacy on ADHD core symptoms, it is unlikely that these novel agents will show better efficacy than stimulants, at the group level. However, they may offer comparable or better tolerability. Additionally, agents acting on etiopathophysiological targets disrupted in specific subgroups of patients with ADHD will move forward the pharmacotherapy of ADHD from a 'one size fits all' to a 'precision medicine' approach.