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| Other Sizes |
| Targets |
9-Fluorenol targets the dopamine transporter (DAT), acting as an inhibitor (antagonist). It has an IC50 of 9 μM for inhibiting DAT. By inhibiting DAT, it blocks the reuptake of dopamine, leading to increased extracellular dopamine levels, which is associated with its wake-promoting effects.
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| ln Vitro |
In cell-free systems, 9-Fluorenol inhibits dopamine uptake with an IC50 of 9 μM. This activity is measured using standard dopamine uptake inhibition assays with synaptosomal preparations or membrane preparations expressing the dopamine transporter. The compound's potency at DAT is confirmed in these assays. Cellular uptake assays demonstrate that 9-Fluorenol inhibits DAT-mediated dopamine transport in neuronal cells. By blocking dopamine reuptake, it increases extracellular dopamine levels. This mechanism is consistent with its wake-promoting activity, as enhanced dopaminergic signaling is associated with arousal.
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| ln Vivo |
1.19 Pharmacokinetic parameters: Plasma Brain Cmax, ng/g 263 4384 tmax, h 2 0.8 AUC0-t, ng h/g 1081 11639; 9-Fluorenol (100 mg/kg; ip) in rats[1]
In vivo, 9-Fluorenol displays wake-promoting activity. It is a major metabolite of a compound developed as a wake-promoting agent, and its activity contributes to the overall effect of the parent compound. Studies in animal models have confirmed its ability to promote wakefulness. |
| Enzyme Assay |
Dopamine uptake inhibition assays for 9-Fluorenol are performed using synaptosomal preparations or cells expressing the dopamine transporter. [³H]Dopamine is used as the substrate, and uptake is measured in the presence of varying concentrations of the compound. IC50 values are determined from inhibition curves.
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| Cell Assay |
Cellular assays for 9-Fluorenol are conducted using neuronal cell cultures or cells expressing the dopamine transporter. Cells are pre-incubated with the compound at various concentrations, then [³H]dopamine is added. Uptake is terminated after a defined period, and accumulated radioactivity is measured. IC50 values are calculated from concentration-response data.
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| Animal Protocol |
In vivo studies on 9-Fluorenol are conducted in animal models to assess its wake-promoting effects. The compound is administered systemically, and its effects on sleep-wake cycles are monitored using electroencephalography (EEG) or behavioral observation.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of 9-Fluorenol are related to its role as a metabolite. It is formed from a parent compound and may contribute to the overall pharmacokinetic and pharmacodynamic profile of the parent drug. Detailed PK parameters for 9-Fluorenol itself are not extensively reported.
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| Toxicity/Toxicokinetics |
Toxicity Summary
9-Hydroxyfluorene is a weak dopamine reuptake inhibitor. (Wikipedia) Preclinical toxicity data for 9-Fluorenol are limited. As a metabolite of a wake-promoting agent, its safety profile is likely related to that of the parent compound. Standard laboratory safety practices should be followed when handling the compound. |
| References |
[1]. Dunn D, et al. Wake promoting agents: search for next generation modafinil, lessons learned: part III. Bioorg Med Chem Lett. 2012 Jun 1;22(11):3751-3.
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| Additional Infomation |
Fluorene-9-ol is a hydroxyfluorene compound with the structure 9H-fluorene replaced by a hydroxyl group at the 9-position (a non-aromatic carbon atom). It is an animal metabolite. Fluorene-9-ol belongs to the hydroxyfluorene class and is also a secondary alcohol. It has been reported to be found in Pinellia ternata and Alepocephalus rostratus, with relevant data available. This compound belongs to the fluorene class. Fluorene compounds are fluorene structural units consisting of two benzene rings linked by cyclopentane, cyclopentene, or cyclopentadiene.
9-Fluorenol is a research compound and a metabolite of interest in the study of wake-promoting agents. It is used to study the role of dopamine in arousal and sleep-wake regulation. The compound is not approved for clinical use. |
| Molecular Formula |
C13H10O
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|---|---|
| Molecular Weight |
182.22
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| Exact Mass |
182.073
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| CAS # |
1689-64-1
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| PubChem CID |
74318
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
367.5±11.0 °C at 760 mmHg
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| Melting Point |
153-154 °C(lit.)
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| Flash Point |
131.3±11.5 °C
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| Vapour Pressure |
0.0±0.9 mmHg at 25°C
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| Index of Refraction |
1.687
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| LogP |
2.51
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
14
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| Complexity |
191
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O([H])C1([H])C2=C([H])C([H])=C([H])C([H])=C2C2=C([H])C([H])=C([H])C([H])=C12
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| InChi Key |
AFMVESZOYKHDBJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H10O/c14-13-11-7-3-1-5-9(11)10-6-2-4-8-12(10)13/h1-8,13-14H
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| Chemical Name |
9H-fluoren-9-ol
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 5.4879 mL | 27.4394 mL | 54.8787 mL | |
| 5 mM | 1.0976 mL | 5.4879 mL | 10.9757 mL | |
| 10 mM | 0.5488 mL | 2.7439 mL | 5.4879 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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