Phaclofen
Based on 1 Customer Validation
Phaclofen is a selective GABAB receptor antagonist. Phaclofen is a peripheral and central baclofen antagonist. Phaclofen maybe a potential compound in determining the physiological significance of central and peripheral bicuculline-insensitive receptors with which GABA and (-)-baclofen interact.
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- Pureza: 99.91%
- No. CAS: 114012-12-3
- Fòrmula: C9H13ClNO3P
- Peso molecular:249.63
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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
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
GABAB receptor[1]
The GABAB antagonist phaclofen (500 µM) partly prevents the effect of 1 µM of (R＋) baclofen[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Phaclofen (2 mg/kg; s.c) antagonizes the effects of 6 mg/kg R(＋) baclofen in dorsal striatum[5].
Phaclofen (100 nmol; intrathecal injection) antagonizes the depressant effect of baclofen. Phaclofen (100 nmol) is devoid of stimulatory or depressant effects on spinal reflexes[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague–Dawley rats (180–250 g)[4]
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Dosage:2 mg/kg
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Administration:I.p．
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Result:Fewer neuropeptide Y-like immunoreactive fibers were detected in the stimulated cuneate nucleus.
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Animal Model:Male Wistar rats (280–320 g)[5]
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Dosage:2 mg/kg
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Administration:S.c.
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Result:Antagonized the effects of 6 mg/kg R(＋) baclofen in dorsal striatum.
Chemical Information
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No. CAS 114012-12-3
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Appearance Solid
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Peso molecular 249.63
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Fòrmula C9H13ClNO3P
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Color White to off-white
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SMILES
ClC1=CC=C(C(CN)CP(O)(O)=O)C=C1
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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
1M NaOH : 50 mg/mL (200.30 mM; Need ultrasonic)
DMSO : < 1 mg/mL (insoluble or slightly soluble)
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)
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Johnson CM, et al. The antitussive cloperastine improves breathing abnormalities in a Rett Syndrome mouse model by blocking presynaptic GIRK channels and enhancing GABA release. Neuropharmacology. 2020;176:108214. [Content Brief]
[2]. Kerr DI, et al. Phaclofen: a peripheral and central baclofen antagonist. Brain Res. 1987;405(1):150-154. [Content Brief]
[3]. Wüllner U, et al. Phaclofen antagonizes the depressant effect of baclofen on spinal reflex transmission in rats. Brain Res. 1989;496(1-2):341-344. [Content Brief]
[4]. Chen SH, et al. Changes in GABA and GABA(B) receptor expressions are involved in neuropathy in the rat cuneate nucleus following median nerve transection. Synapse.2012; 66(6):561-572. [Content Brief]
[5]. Abellán MT, et al. Dual control of dorsal raphe serotonergic neurons by GABA(B) receptors. Electrophysiological and microdialysis studies. Synapse. 2000;36(1):21-34. [Content Brief]
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 |
|---|---|---|---|---|---|
| 1M NaOH | 1 mM | 4.0059 mL | 20.0296 mL | 40.0593 mL | 100.1482 mL |
| 5 mM | 0.8012 mL | 4.0059 mL | 8.0119 mL | 20.0296 mL | |
| 10 mM | 0.4006 mL | 2.0030 mL | 4.0059 mL | 10.0148 mL | |
| 15 mM | 0.2671 mL | 1.3353 mL | 2.6706 mL | 6.6765 mL | |
| 20 mM | 0.2003 mL | 1.0015 mL | 2.0030 mL | 5.0074 mL | |
| 25 mM | 0.1602 mL | 0.8012 mL | 1.6024 mL | 4.0059 mL | |
| 30 mM | 0.1335 mL | 0.6677 mL | 1.3353 mL | 3.3383 mL | |
| 40 mM | 0.1001 mL | 0.5007 mL | 1.0015 mL | 2.5037 mL | |
| 50 mM | 0.0801 mL | 0.4006 mL | 0.8012 mL | 2.0030 mL | |
| 60 mM | 0.0668 mL | 0.3338 mL | 0.6677 mL | 1.6691 mL | |
| 80 mM | 0.0501 mL | 0.2504 mL | 0.5007 mL | 1.2519 mL | |
| 100 mM | 0.0401 mL | 0.2003 mL | 0.4006 mL | 1.0015 mL |
Phaclofen Related Classifications
HY-100798 Related Classifications
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