Befiradol hydrochloride
Based on 1 Customer Validation
Befiradol (NLX-112) hydrochloride is a highly selective 5-HT1A receptor agonist that acts on both presynaptic and postsynaptic sites. Befiradol hydrochloride attenuates fentanyl-induced respiratory depression in neonatal and adult rats. Befiradol reduces the duration of fentanyl-induced analgesia and sedation in adult rats. Befiradol hydrochloride can be used in studies related to opioid-induced respiratory depression.
For research use only. We do not sell to patients.
- Purity: 99.93%
- CAS No.: 2436760-81-3
- Formula: C20H23Cl2F2N3O
- Molecular Weight:430.32
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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5-HT1A Receptor |
Befiradol (1-30 μM) hydrochloride 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) hydrochloride 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) hydrochloride 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).
Chemical Information
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CAS No. 2436760-81-3
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Appearance Solid
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Molecular Weight 430.32
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Formula C20H23Cl2F2N3O
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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.Cl
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Synonyms
NLX-112 hydrochloride; F 13640 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 125 mg/mL (290.48 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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: ≥ 2.08 mg/mL (4.83 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.83 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Purity & Documentation
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Data Sheet (273 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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Handling Instructions (2659 KB)
References
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 (sealed storage, away from moisture). 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 | 2.3239 mL | 11.6193 mL | 23.2385 mL | 58.0963 mL |
| 5 mM | 0.4648 mL | 2.3239 mL | 4.6477 mL | 11.6193 mL | |
| 10 mM | 0.2324 mL | 1.1619 mL | 2.3239 mL | 5.8096 mL | |
| 15 mM | 0.1549 mL | 0.7746 mL | 1.5492 mL | 3.8731 mL | |
| 20 mM | 0.1162 mL | 0.5810 mL | 1.1619 mL | 2.9048 mL | |
| 25 mM | 0.0930 mL | 0.4648 mL | 0.9295 mL | 2.3239 mL | |
| 30 mM | 0.0775 mL | 0.3873 mL | 0.7746 mL | 1.9365 mL | |
| 40 mM | 0.0581 mL | 0.2905 mL | 0.5810 mL | 1.4524 mL | |
| 50 mM | 0.0465 mL | 0.2324 mL | 0.4648 mL | 1.1619 mL | |
| 60 mM | 0.0387 mL | 0.1937 mL | 0.3873 mL | 0.9683 mL | |
| 80 mM | 0.0290 mL | 0.1452 mL | 0.2905 mL | 0.7262 mL | |
| 100 mM | 0.0232 mL | 0.1162 mL | 0.2324 mL | 0.5810 mL |
Befiradol hydrochloride Related Classifications
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