| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
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| Other Sizes |
| Targets |
Flesinoxan targets the 5-HT1A receptor, a G protein-coupled receptor that mediates serotonergic neurotransmission in the brain. As a selective agonist, flesinoxan activates 5-HT1A receptors, leading to the inhibition of adenylate cyclase and modulation of neuronal excitability. This receptor activation is responsible for the compound's anxiolytic and antidepressant effects, as well as its antihypertensive activity.
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| ln Vitro |
Flesinoxan is a potent 5-HT1A receptor agonist with an EC₅₀ of 24 nM. It shows high selectivity for 5-HT1A over other serotonin receptor subtypes and other neurotransmitter receptors. The compound's activity can be quantified in radioligand binding assays using [³H]-8-OH-DPAT and in functional assays measuring 5-HT1A-mediated inhibition of cAMP accumulation or activation of G protein-coupled inward rectifier potassium (GIRK) channels.
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| ln Vivo |
At postsynaptic 5-HT1A receptors, flesinoxan functions as a partial agonist; at presynaptic 5-HT1A receptors, it functions as a full agonist. The way that 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH-DPAT) counteracts the effects of 5-HT on CA3 pyramidal neurons is comparable to that of blesinoxan [1]. Flesinoxan administered intravenously suppresses the firing activity of dorsal raphe 5-HT neurons and CA3 pyramidal neurons. It was established how permeable the brain is to [3H]Flesinoxan and [3H]8-OH-DPAT. Brain concentrations of [3H]8-OH-DPAT were substantially greater than [3H]Flesinoxan nine minutes after intravenous injection[1]. The administration of Flesinoxan with 8-OH-DPAT subcutaneously induces hypothermia based on the dose. The hypothermia caused by Flesinoxan was considerably reduced by preadministration of the nonselective 5-HT1A antagonist pindolol and the 5-HT1/2 antagonist methysergide. 0.5 mg/kg of 8-OH-DPAT and 3 mg/kg of Flesinoxan produced hypothermia to comparable degrees. Compared to 8-OH-DPAT, the maximal effect of Flesinoxan happens 30 minutes later and dissipates more slowly [1].
Flesinoxan has been shown to have anxiolytic and antidepressant effects in animal models. It also exhibits antihypertensive activity. The compound's effects on serotonin neurotransmission have been studied in rodent models of anxiety and depression. Flesinoxan has been investigated in clinical trials for the treatment of anxiety and depression. |
| Enzyme Assay |
For non-cellular receptor binding assays, flesinoxan's affinity for the 5-HT1A receptor can be evaluated using radioligand binding displacement studies. Membrane preparations from cells expressing human 5-HT1A receptors (or from rat hippocampal tissue) are incubated with [³H]-8-OH-DPAT and varying concentrations of flesinoxan. Binding displacement curves are generated to determine the IC₅₀ and Ki values.
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| Cell Assay |
In vitro cellular assays for flesinoxan involve treating cells expressing the 5-HT1A receptor with the compound and measuring receptor-mediated signaling. Functional assays typically measure the inhibition of forskolin-stimulated cAMP accumulation, as 5-HT1A receptors are coupled to Gi proteins. Cells are treated with varying concentrations of flesinoxan, and cAMP levels are quantified by ELISA or AlphaScreen. The EC₅₀ for receptor activation is determined.
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| Animal Protocol |
In vivo animal experiments with flesinoxan involve administering the compound to rodents to assess its effects on behavior and autonomic function. The compound's anxiolytic effects are evaluated using the elevated plus maze, open field test, or social interaction test. Antidepressant effects are assessed using the forced swim test or tail suspension test. Antihypertensive effects are measured by monitoring blood pressure in spontaneously hypertensive rats.
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| ADME/Pharmacokinetics |
Flesinoxan has a molecular weight of 415.42 and a molecular formula of C₂₂H₂₆FN₃O₄. It is a solid at room temperature and is typically stored at -20°C. The compound is soluble in DMSO and other organic solvents. Purity is typically >98%. It is stable under recommended storage conditions and is protected from light and moisture.
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| Toxicity/Toxicokinetics |
Toxicological data for flesinoxan are limited as it is an investigational compound. In preclinical studies, it has been generally well-tolerated. As a 5-HT1A agonist, it may cause side effects related to serotonergic activation, including gastrointestinal disturbances, headache, and dizziness. The compound has been evaluated in clinical trials.
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| References |
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| Additional Infomation |
Flesinoxan is a potent and selective 5-HT1A receptor agonist with anxiolytic and antidepressant properties. It has been investigated for the treatment of anxiety, depression, and hypertension. The compound is available from various commercial suppliers for research applications.
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| Molecular Formula |
C22H26FN3O
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|---|---|
| Molecular Weight |
415.4654
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| Exact Mass |
415.191
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| CAS # |
98206-10-1
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| Related CAS # |
98205-89-1 (HCl);98206-10-1;
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| PubChem CID |
57347
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.271g/cm3
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| Boiling Point |
635.8ºC at 760mmHg
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| Flash Point |
338.3ºC
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| Index of Refraction |
1.585
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| LogP |
1.903
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
30
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| Complexity |
553
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1CN(CCN1CCNC(=O)C2=CC=C(C=C2)F)C3=C4C(=CC=C3)O[C@H](CO4)CO
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| InChi Key |
NYSDRDDQELAVKP-SFHVURJKSA-N
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| InChi Code |
InChI=1S/C22H26FN3O4/c23-17-6-4-16(5-7-17)22(28)24-8-9-25-10-12-26(13-11-25)19-2-1-3-20-21(19)29-15-18(14-27)30-20/h1-7,18,27H,8-15H2,(H,24,28)/t18-/m0/s1
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| Chemical Name |
4-fluoro-N-[2-[4-[(2S)-2-(hydroxymethyl)-2,3-dihydro-1,4-benzodioxin-5-yl]piperazin-1-yl]ethyl]benzamide
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| Synonyms |
DU29373; DU-29373; Flesinoxan
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~31.25 mg/mL (~75.22 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.01 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.01 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4069 mL | 12.0346 mL | 24.0691 mL | |
| 5 mM | 0.4814 mL | 2.4069 mL | 4.8138 mL | |
| 10 mM | 0.2407 mL | 1.2035 mL | 2.4069 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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