(+)-Norfenfluramine
Based on 1 Customer Validation
(+)-Norfenfluramine a major hepatic metabolite of (+)-fenfluramine, is a selective 5-HT2B receptor agonist (Ki: 11.2 nM). (+)-Norfenfluramine potently stimulates the hydrolysis of inositol phosphates and increases intracellular Ca2+. (+)-Norfenfluramine can be used for the research of primary pulmonary hypertension and valvular heart disease.
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- Pureza: 98.79%
- No. CAS: 19036-73-8
- Fòrmula: C10H12F3N
- Peso molecular:203.20
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Ver todos los productos específicos de isoformas 5-HT Receptor
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Actividad biológica
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5-HT2B Receptor |
5-HT2B Receptor 11.2 nM (Ki) |
5-HT2A Receptor 1516 nM (Ki) |
5-HT2C Receptor 324 nM (Ki) |
(+)-Norfenfluramine (1 nM to 100 μM) contracts arteries with a dramatic decrease in threshold (aorta and mesenteric resistance artery) in rats[1].
(+)-Norfenfluramine (1 and 10 μM, 3 min) induces contraction in aorta from tissues of normotensive and hypertensive rats[1].
(+)-Norfenfluramine (0-10 μM, 3 min) induces 5-HT release from rat hippocampal synaptosomes by Ca2+-dependent way [2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
(+)-Norfenfluramine (2.5 and 5 mg/kg, i.p.) decreases of 5-HT and 5-HIAA levels in telencephalon and brainstem of rats[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Conscious SHAM and DOCA-salt rats[1].
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Dosage:1-300 μg/kg
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Administration:Intravenous injection (i.v.), given in a cumulative fashion at 6-min intervals.
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Result:Induced pressor response in conscious SHAM and DOCA-salt rats. (change in mean arterial blood pressure at 300 μg/kg, mm Hg, SHAM vehicle=36, SHAM ketanserin=7, DOCA=51, DOCA ketanserin=19).
Chemical Information
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No. CAS 19036-73-8
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Appearance Liquid (Density: 1.152±0.06 g/cm3)
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Peso molecular 203.20
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Fòrmula C10H12F3N
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Color Light yellow to green yellow
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SMILES
C=1(C=C(C=CC1)C(F)(F)F)C[C@H](C)N
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Synonyms
d-Norfenfluramine
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvente y solubilidad
DMSO : 100 mg/mL (492.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (12.30 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (12.30 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Wei Ni, et al. The 5-hydroxytryptamine2A receptor is involved in (+)-norfenfluramine-induced arterial contraction and blood pressure increase in deoxycorticosterone acetate-salt hypertension. J Pharmacol Exp Ther. 2007 May;321(2):485-91. [Content Brief]
[2]. M Gobbi, et al. In vitro studies on the mechanism by which (+)-norfenfluramine induces serotonin and dopamine release from the vesicular storage pool. Naunyn Schmiedebergs Arch Pharmacol. 1998 Sep;358(3):323-7. [Content Brief]
[3]. R Invernizzi, et al. Is receptor activation involved in the mechanism by which (+)-fenfluramine and (+)-norfenfluramine deplete 5-hydroxytryptamine in the rat brain? Br J Pharmacol. 1982 Mar;75(3):525-30. [Content Brief]
[4]. Erenburg N, Hamed R, Shaul C, Perucca E, Bialer M. Comparative activity of the enantiomers of fenfluramine and norfenfluramine in rodent seizure models, and relationship with their concentrations in plasma and brain. Epilepsia. 2023;64(6):1673-1683. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.9213 mL | 24.6063 mL | 49.2126 mL | 123.0315 mL |
| 5 mM | 0.9843 mL | 4.9213 mL | 9.8425 mL | 24.6063 mL | |
| 10 mM | 0.4921 mL | 2.4606 mL | 4.9213 mL | 12.3031 mL | |
| 15 mM | 0.3281 mL | 1.6404 mL | 3.2808 mL | 8.2021 mL | |
| 20 mM | 0.2461 mL | 1.2303 mL | 2.4606 mL | 6.1516 mL | |
| 25 mM | 0.1969 mL | 0.9843 mL | 1.9685 mL | 4.9213 mL | |
| 30 mM | 0.1640 mL | 0.8202 mL | 1.6404 mL | 4.1010 mL | |
| 40 mM | 0.1230 mL | 0.6152 mL | 1.2303 mL | 3.0758 mL | |
| 50 mM | 0.0984 mL | 0.4921 mL | 0.9843 mL | 2.4606 mL | |
| 60 mM | 0.0820 mL | 0.4101 mL | 0.8202 mL | 2.0505 mL | |
| 80 mM | 0.0615 mL | 0.3076 mL | 0.6152 mL | 1.5379 mL | |
| 100 mM | 0.0492 mL | 0.2461 mL | 0.4921 mL | 1.2303 mL |
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