Donitriptan hydrochloride |
Katalog-Nr.GC13265
One-Click Copy Product Info
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5-HT1B/1D receptors agonist, potent and selective
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 170911-68-9
Sample solution is provided at 25 µL, 10mM.
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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 | |
| Chemical Name | 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 | ||
| Formula | C23H25N5O2.HCl | M.Wt | 439.94 |
| Löslichkeit | Soluble in DMSO | Storage | Desiccate at RT |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.273 mL | 11.3652 mL | 22.7304 mL |
| 5 mM | 454.6 μL | 2.273 mL | 4.5461 mL |
| 10 mM | 227.3 μL | 1.1365 mL | 2.273 mL |
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)