| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| Targets |
5-HT2B Receptor 11.2 nM (Ki) 5-HT2C Receptor 324 nM (Ki) 5-HT2A Receptor 1516 nM (Ki)
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| ln Vitro |
Rats' aorta and mesenteric resistance arteries, which have a sharply decreased threshold, are contracted by (+)-norfenfluramine hydrochloride (1 nM to 100 μM)[1]. Rat tissues with normotensive and hypertension conditions exhibit aortic contraction in response to (+)-norfenfluramine hydrochloride (1 and 10 μM, 3 min)[1]. 5-HT release from rat hippocampus synaptosomes is induced by (+)-Norfenfluramine (0-10 μM, 3 min) hydrochloride in a Ca2+-dependent manner [2].
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| ln Vivo |
In conscious SHAM and DOCA-salt rats, (+)-Norfenfluramine (1-300 μg/kg, iv) hydrochloride causes a pressor response[1]. Rat telencephalon and brainstem 5-HT and 5-HIAA levels are decreased by (+)-Norfenfluramine hydrochloride (2.5 and 5 mg/kg, ip)[3].
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| Animal Protocol |
Animal/Disease Models: Conscious SHAM and DOCA-salt rats[1].
Doses: 1-300 μg/kg Route of Administration: intravenous (iv) injection (iv), given in a cumulative fashion at 6-min intervals. Experimental Results: 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). |
| 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.
[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. [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. |
| Molecular Formula |
C10H13CLF3N
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|---|---|
| Molecular Weight |
239.67
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| CAS # |
37936-89-3
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| Related CAS # |
(+)-Norfenfluramine;19036-73-8
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| SMILES |
Cl[H].FC(C1=C([H])C([H])=C([H])C(=C1[H])C([H])([H])[C@]([H])(C([H])([H])[H])N([H])[H])(F)F
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| Solubility (In Vitro) |
H2O: 18.75 mg/mL (78.23 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.1724 mL | 20.8620 mL | 41.7240 mL | |
| 5 mM | 0.8345 mL | 4.1724 mL | 8.3448 mL | |
| 10 mM | 0.4172 mL | 2.0862 mL | 4.1724 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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