| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Animal Protocol |
Animal/Disease Models: Male Long-Evans rat (250-300 g)[3]
Doses: 30-60 mg/kg Route of Administration: Po Experimental Results: Self-management is inhibited Pharmacokinetic Study:** Two groups of Sprague-Dawley rats (n=6 per group) received a single oral dose (30 mg/kg, based on anhydrous free base equivalents) of either fenobam free base or fenobam sulfate. Fenobam free base was first dissolved in 10% DMSO and then brought to final concentration in 40% hydroxypropyl-β-cyclodextrin (BCD). Fenobam sulfate was dissolved in 40% BCD. Blood samples were collected via jugular vein catheter at multiple time points up to 24 hours post-dose. Plasma was analyzed for fenobam concentration using a validated LC-MS/MS method. [3] **Cocaine Self-Administration:** Male Long-Evans rats were trained to self-administer intravenous cocaine (0.5 or 1 mg/kg/infusion) under a fixed-ratio (FR) schedule. Once stable self-administration was established, animals received oral fenobam sulfate (0, 30, or 60 mg/kg, dissolved in 40% BCD) 30 minutes prior to the test session. A within-session, multiple-dose cocaine self-administration paradigm was also used to test effects across a range of cocaine doses. [3] **Sucrose Self-Administration:** Similar to cocaine self-administration, rats were trained to self-administer oral 5% sucrose solution. Oral fenobam sulfate (0, 30, or 60 mg/kg) was administered 30 minutes prior to test sessions. [3] **Reinstatement Tests:** Animals were first trained to self-administer cocaine or sucrose, then underwent extinction training. On reinstatement test days, animals received oral fenobam sulfate (0, 30, or 60 mg/kg) 30 minutes prior to a priming injection of cocaine (10 mg/kg, i.p.) or non-contingent sucrose deliveries. Lever presses were recorded under extinction conditions (no drug/cue delivery). [3] **Locomotor Activity:** Naive rats were habituated to locomotor chambers. On test days, baseline activity was recorded for 1 hour, then animals received oral fenobam sulfate (0, 30, or 60 mg/kg, dissolved in 40% BCD). Locomotor activity was recorded for an additional 3 hours. [3] |
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| References |
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| Additional Infomation |
1-(3-Chlorophenyl)-3-(3-methyl-5-oxo-4H-imidazol-2-yl)urea is a type of urea compound. Fennobam is being investigated in the clinical trial NCT00637221 (an open-label study investigating the safety and efficacy of anhydrous fennobam 50 mg to 150 mg in adult patients with Fragile X syndrome for pre-pulse inhibition testing and continuous operational tasks).
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| Exact Mass |
266.057
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|---|---|
| CAS # |
57653-26-6
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| PubChem CID |
135659063
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| Appearance |
White to off-white solid powder
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| Density |
1.47 g/cm3
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| Index of Refraction |
1.668
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| LogP |
1.126
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
18
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| Complexity |
385
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN1CC(=O)NC1=NC(=O)NC2=CC(=CC=C2)Cl
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| InChi Key |
DWPQODZAOSWNHB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H11ClN4O2/c1-16-6-9(17)14-10(16)15-11(18)13-8-4-2-3-7(12)5-8/h2-5H,6H2,1H3,(H2,13,14,15,17,18)
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| Chemical Name |
(3Z)-1-(3-chlorophenyl)-3-(1-methyl-4-oxoimidazolidin-2-ylidene)urea
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| Synonyms |
Fenobam NPL2009 NPL-2009
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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 : ~100 mg/mL (~374.98 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.) |
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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01806415 | COMPLETED | Drug: Fenobam Drug: Placebo |
Healthy | Washington University School of Medicine | 2013-05 | Phase 1 |
| NCT01981395 | COMPLETED | Drug: Fenobam Drug: Placebo |
Allodynia Hyperalgesia |
Laura Cavallone | 2014-01 | Phase 1 |
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