Befiradol
Based on 1 Customer Validation
Befiradol (NLX-112) is a highly selective 5-HT1A receptor agonist that acts on both presynaptic and postsynaptic sites. Befiradol attenuates fentanyl-induced respiratory depression in neonatal and adult rats. Befiradol reduces the duration of fentanyl-induced analgesia and sedation in adult rats. Befiradol can be used in studies related to opioid-induced respiratory depression.
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- Pureza: 99.53%
- No. CAS: 208110-64-9
- Fòrmula: C20H22ClF2N3O
- Peso molecular:393.86
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Actividad biológica
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5-HT1A Receptor |
Befiradol (1-30 μM) does not alleviate DAMGO-induced respiratory depression or alter baseline respiratory rhythm in vitro neonatal rat brainstem-spinal cord preparations[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Befiradol (0.1-0.4 mg/kg; intravenous injection; single bolus) dose-dependently attenuates fentanyl-induced respiratory depression and sedation in adult rats, but also significantly reduces fentanyl-induced analgesic effects at effective doses[1].
Befiradol (0.2 mg/kg; subcutaneous injection; single bolus dose) induces hyperventilation, hyperalgesia and behavioral syndrome in normal adult rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (neonatal, 3 to 4 days after birth)[1]
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Dosage:0.6 mg/kg
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Administration:s.c.; single bolus
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Result:Increased relative respiratory frequency to 39.2% of control (vs. saline 24.2% of control).
Increased relative tidal volume to 76.1% of control (vs. saline 52.2% of control).
Increased relative minute ventilation to 29.3% of control (vs. saline 12.4% of control).
Alleviated fentanyl-induced respiratory depression over 20 minutes.
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Animal Model:Sprague-Dawley (adult male, 290 to 360 g)[1]
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Dosage:0.1, 0.2, 0.4 mg/kg
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Administration:i.v.; single bolus
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Result:At 0.1 mg/kg, increased relative minute ventilation to 37.4% of control (vs. saline 18.7% of control) and oxygen saturation to 59.5% (vs. saline 45.7%) 4 minutes post-administration; alleviation lasted less than 10 minutes.
At 0.2 mg/kg, increased relative minute ventilation to 53.7% of control (vs. saline 18.7% of control) and oxygen saturation to 75.4% (vs. saline 45.7%) 4 minutes post-administration; alleviation lasted beyond fentanyl infusion duration.
At 0.4 mg/kg, increased relative minute ventilation to 65.8% of control (vs. saline 18.7% of control) and oxygen saturation to 78.5% (vs. saline 45.7%) 4 minutes post-administration; alleviation lasted beyond fentanyl infusion duration.
At 0.2 mg/kg, reduced duration of analgesia via tail clamping to 28.4 min (vs. saline 52.4 min) and via thermal paw withdrawal to 90.4 min (vs. saline 130.5 min).
At 0.2 mg/kg, reduced duration of fentanyl-induced sedation to 39.8 min (vs. saline 58 min).
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 208110-64-9
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Appearance Solid
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Peso molecular 393.86
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Fòrmula C20H22ClF2N3O
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Color White to off-white
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SMILES
O=C(C1=CC=C(F)C(Cl)=C1)N2CCC(CNCC3=NC=C(C)C=C3)(F)CC2
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Synonyms
NLX-112; F13640
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 50 mg/mL (126.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.35 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.35 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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. 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5390 mL | 12.6949 mL | 25.3897 mL | 63.4743 mL |
| 5 mM | 0.5078 mL | 2.5390 mL | 5.0779 mL | 12.6949 mL | |
| 10 mM | 0.2539 mL | 1.2695 mL | 2.5390 mL | 6.3474 mL | |
| 15 mM | 0.1693 mL | 0.8463 mL | 1.6926 mL | 4.2316 mL | |
| 20 mM | 0.1269 mL | 0.6347 mL | 1.2695 mL | 3.1737 mL | |
| 25 mM | 0.1016 mL | 0.5078 mL | 1.0156 mL | 2.5390 mL | |
| 30 mM | 0.0846 mL | 0.4232 mL | 0.8463 mL | 2.1158 mL | |
| 40 mM | 0.0635 mL | 0.3174 mL | 0.6347 mL | 1.5869 mL | |
| 50 mM | 0.0508 mL | 0.2539 mL | 0.5078 mL | 1.2695 mL | |
| 60 mM | 0.0423 mL | 0.2116 mL | 0.4232 mL | 1.0579 mL | |
| 80 mM | 0.0317 mL | 0.1587 mL | 0.3174 mL | 0.7934 mL | |
| 100 mM | 0.0254 mL | 0.1269 mL | 0.2539 mL | 0.6347 mL |
Befiradol Related Classifications
HY-14785 Related Classifications
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- Befiradol
- 208110-64-9
- NLX-112
- F13640
- NLX112
- NLX 112
- F13640
- F 13640
- F-13640
- 5-HT Receptor
- fentanyl-induced respiratory depression
- preB?tzinger complex
- fentanyl-induced sedation
- adult rats
- hyperventilation
- hyperalgesia
- neonatal rats
- fentanyl-induced analgesia
- DAMGO-induced respiratory depression
- Inhibitor
- inhibitor
- inhibit