Donitriptan hydrochloride
目录号 : GC13265
5-HT1B/1D receptors agonist, potent and selective
Cas No.:170911-68-9
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
Donitriptan hydrochloride is a potent, selective, high-efficacy agonist at 5-HT1B/1D receptors both in vivo and in vitro in neuronal and vascular models relevant to migraine.
Donitriptan hydrochloride has subnanomolar affinity for cloned human and nonhuman 5-HT1B and 5-HT1D receptors with Ki values ranging from 0.1-4.3 nM. It potently inhibits forskolin-induced cAMP accumulation mediated by recombinant human and nonhuman, stably transfected 5-HT1B and 5-HT1D receptors with mean EC50 values ranging from 0.2-1.9 nM [1].
In mammals, 5-hydroxytryptamine (5-HT) is important in regulating emotions and related behaviors as a neurotransmitter [2]. In C6 glioma cells transfected with human 5-HT1B or 5-HT1D receptors, donitriptan hydrochloride enhanced specific GTPγ35S binding at both 5-HT1B and 5-HT1D receptors to a greater extent, compared with rizatriptan, naratriptan, sumatriptan, dihydroergotamine and zolmitriptan, but to a level equivalent to which evoked by 5-HT. In guinea pig-isolated trigeminal ganglion neurons, treatment with donitriptan hydrochloride resulted in increase in Ca2+-dependent K+ current (pD2 = 7.3) [1].
Oral administration with donitriptan hydrochloride in guinea pigs resulted in hypothermic responses with an ED50 of 1.6 mg/kg. Compared with zolmitriptan, naratriptan and rizatriptan with an ED50 of 8.3, 9.9 and 12.3 mg/kg, respectively, donitriptan hydrochloride showed superior potency. There is likelihood that donitriptan hydrochloride gains access to the brain [1].Donitriptan hydrochloride is orally active and well tolerated by animals, displays unique craniovascular selectivity and a long duration of action, and gains access to the brain.
References:
[1]. Gareth W. John, Michel Perez, Petrus J. Pauwels, et al. Donitriptan, a Unique High-Efficacy 5-HT1B/1D Agonist: Key Features and Acute Antimigraine Potential. CNS Drug Reviews, 2000, 6(4): 278-289.
[2]. Liang Hua, QinWang, ZhenQin, et al. Detection of 5-hydroxytryptamine (5-HT) in vitro using a hippocampal neuronal network-based biosensor with extracellular potential analysis of neurons. Biosensors and Bioelectronics, 2015, 66:572-578.
| Cas No. | 170911-68-9 | SDF | |
| 化学名 | 4-(4-(2-((3-(2-aminoethyl)-1H-indol-5-yl)oxy)acetyl)piperazin-1-yl)benzonitrile hydrochloride | ||
| Canonical SMILES | O=C(COC1=CC=C2NC=C(CCN)C2=C1)N3CCN(C4=CC=C(C#N)C=C4)CC3.Cl | ||
| 分子式 | C23H25N5O2.HCl | 分子量 | 439.94 |
| 溶解度 | Soluble in DMSO | 储存条件 | Desiccate 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.273 mL | 11.3652 mL | 22.7304 mL |
| 5 mM | 0.4546 mL | 2.273 mL | 4.5461 mL |
| 10 mM | 0.2273 mL | 1.1365 mL | 2.273 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。