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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.91%
- CAS 番号: 114012-12-3
- 分子式: C9H13ClNO3P
- 分子量:249.63
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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.
化学情報
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CAS 番号 114012-12-3
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性状 Solid
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分子量 249.63
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (276 KB)
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取扱説明書 (2659 KB)
参考文献
[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 関連分類
HY-100798 関連分類
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