(+)-Norfenfluramine hydrochloride
Based on 1 Customer Validation
(+)-Norfenfluramine hydrochloride, a major hepatic metabolite of (+)-fenfluramine, is a selective 5-HT2B receptor agonist (Ki: 11.2 nM). (+)-Norfenfluramine hydrochloride potently stimulates the hydrolysis of inositol phosphates and increases intracellular Ca2+. (+)-Norfenfluramine hydrochloride can be used for the research of primary pulmonary hypertension and valvular heart disease.
For research use only. We do not sell to patients.
- Purity: 99.77%
- CAS No.: 37936-89-3
- Formula: C10H13ClF3N
- Molecular Weight:239.67
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
All 5-HT Receptor Isoforms
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Biological Activity
|
5-HT2B Receptor |
5-HT2B Receptor 11.2 nM (Ki) |
5-HT2C Receptor 324 nM (Ki) |
5-HT2A Receptor 1516 nM (Ki) |
(+)-Norfenfluramine (1 nM to 100 μM) hydrochloride contracts arteries with a dramatic decrease in threshold (aorta and mesenteric resistance artery) in rats[1].
(+)-Norfenfluramine (1 and 10 μM, 3 min) hydrochloride induces contraction in aorta from tissues of normotensive and hypertensive rats[1].
(+)-Norfenfluramine (0-10 μM, 3 min) hydrochloride 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.) hydrochloride 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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CAS No. 37936-89-3
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Appearance Solid
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Molecular Weight 239.67
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Formula C10H13ClF3N
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Color White to off-white
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SMILES
N[C@@H](C)CC1=CC=CC(C(F)(F)F)=C1.[H]Cl
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Synonyms
d-Norfenfluramine hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H2O : 18.75 mg/mL (78.23 mM; ultrasonic and warming and heat to 60°C)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (275 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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Handling Instructions (2659 KB)
References
[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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| H2O | 1 mM | 4.1724 mL | 20.8620 mL | 41.7240 mL | 104.3101 mL |
| 5 mM | 0.8345 mL | 4.1724 mL | 8.3448 mL | 20.8620 mL | |
| 10 mM | 0.4172 mL | 2.0862 mL | 4.1724 mL | 10.4310 mL | |
| 15 mM | 0.2782 mL | 1.3908 mL | 2.7816 mL | 6.9540 mL | |
| 20 mM | 0.2086 mL | 1.0431 mL | 2.0862 mL | 5.2155 mL | |
| 25 mM | 0.1669 mL | 0.8345 mL | 1.6690 mL | 4.1724 mL | |
| 30 mM | 0.1391 mL | 0.6954 mL | 1.3908 mL | 3.4770 mL | |
| 40 mM | 0.1043 mL | 0.5216 mL | 1.0431 mL | 2.6078 mL | |
| 50 mM | 0.0834 mL | 0.4172 mL | 0.8345 mL | 2.0862 mL | |
| 60 mM | 0.0695 mL | 0.3477 mL | 0.6954 mL | 1.7385 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.