Gepirone
Based on 1 Customer Validation
Gepirone is a selective and affinitive 5-HT1A agonist. Gepirone binds selectively to 5-HT1A receptor binding site. Gepirone acts as an antidepressant agent can be used for anxiety and major depressive disorder research.
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 : 99.88%
- CAS 番号: 83928-76-1
- 分子式: C19H29N5O2
- 分子量:359.47
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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5-HT Receptor アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
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5-HT1A Receptor |
体内実験
Gepirone (10, 15 mg/kg for subcutaneous injection, 2, 7, or 14 days) activates the normosensitive postsynaptic 5-HT1A receptor in Male Sprague-Dawley rats[2].
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[1]
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Dosage:0, 0.1, 0.3, 1 and 3 mg/kg
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Administration:Intraperitoneal injection (i.p.)
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Result:Increases in lordotic activity at lower doses.
Inhibited lordosis by the 0.3 and 1.0 mg/kg doses and further inhibition was produced by the 3.0 mg/kg dose.
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Animal Model:Male Sprague-Dawley rats[2]
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Dosage:10, 15 mg/kg
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Administration:Subcutaneous injection (s.c.)
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Result:Decreased the number of spontaneously active 5-HT neurons and firing rate.
Not modified with long-term treatment with ED50 value of 10.1±0.5 μg/kg in controls and 9.7 ±1.9 μg/kg in treated rats.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 83928-76-1
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性状 Solid
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分子量 359.47
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分子式 C19H29N5O2
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Color White to light yellow
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SMILES
O=C(CC(C)(C)C1)N(CCCCN2CCN(C3=NC=CC=N3)CC2)C1=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
体外:
Ethanol : 33.33 mg/mL (92.72 mM; Need ultrasonic)
DMSO : 33.33 mg/mL (92.72 mM; ultrasonic and warming and heat to 60°C; 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 (protect from light). 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 (protect from light). 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 (271 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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取扱説明書 (2659 KB)
参考文献
[1]. Mendelson SD, et al. Effects of 5-HT1A selective anxiolytics on lordosis behavior: interactions with progesterone. Eur J Pharmacol. 1986 Dec 16;132(2-3):323-6. [Content Brief]
[2]. Blier P, et al. Modification of 5-HT neuron properties by sustained administration of the 5-HT1A agonist gepirone: electrophysiological studies in the rat brain. Synapse. 1987;1(5):470-80. [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 (protect from light). 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 |
|---|---|---|---|---|---|
| Ethanol / DMSO | 1 mM | 2.7819 mL | 13.9094 mL | 27.8187 mL | 69.5468 mL |
| 5 mM | 0.5564 mL | 2.7819 mL | 5.5637 mL | 13.9094 mL | |
| 10 mM | 0.2782 mL | 1.3909 mL | 2.7819 mL | 6.9547 mL | |
| 15 mM | 0.1855 mL | 0.9273 mL | 1.8546 mL | 4.6365 mL | |
| 20 mM | 0.1391 mL | 0.6955 mL | 1.3909 mL | 3.4773 mL | |
| 25 mM | 0.1113 mL | 0.5564 mL | 1.1127 mL | 2.7819 mL | |
| 30 mM | 0.0927 mL | 0.4636 mL | 0.9273 mL | 2.3182 mL | |
| 40 mM | 0.0695 mL | 0.3477 mL | 0.6955 mL | 1.7387 mL | |
| 50 mM | 0.0556 mL | 0.2782 mL | 0.5564 mL | 1.3909 mL | |
| 60 mM | 0.0464 mL | 0.2318 mL | 0.4636 mL | 1.1591 mL | |
| 80 mM | 0.0348 mL | 0.1739 mL | 0.3477 mL | 0.8693 mL |
Gepirone 関連分類
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