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Synonyms | F 11440 | Storage (From the date of receipt) |
3 years -20°C powder | |
化学式 | C16H23N7O2 |
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分子量 | 345.40 | CAS No. | 179756-58-2 | |
Solubility (25°C)* | 体外 | DMSO | 69 mg/mL (199.76 mM) | |
Ethanol | 39 mg/mL (112.91 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | Eptapirone (F11440) is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential.The affinity (pKi) of F11440 for 5-HT1A binding sites is 8.33. |
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in vitro | The affinity of Eptapirone for 5-HT1A binding sites (pKi, 8.33) is higher than that of buspirone (pKi, 7.50), and somewhat lower than that of flesinoxan (pKi, 8.91). In HeLa cells expressing human 5-HT1A receptors, Eptapirone decreases the forskolin-induced increase in AMP, and, based on its maximal effect, is found to have an intrinsic activity of 1.0 relative to that of 5-HT, which is significantly higher than that of buspirone (0.49), ipsapirone (0.46) and flesinoxan (0.93).[1] |
in vivo | In vivo, Eptapirone (F11440) is 4- to 20-fold more potent than flesinoxan, and 30- to 60-fold more potent than buspirone, in exerting 5-HT1A agonist activity at pre- and postsynaptic receptors in rats (measured by, for example, its ability to decrease hippocampal extracellular serotonin (5-HT) levels and to increase plasma corticosterone levels, respectively). Eptapironeproduced anxiolytic- and antidepressant-like effects in animal models (i.e., increased punished responding in a pigeon conflict procedure and decreased immobility in a rat forced swimming test, respectively) that are more substantial than those of buspirone, ipsapirone and flesinoxan. [1] |
細胞アッセイ | 細胞株 | HeLa cells |
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濃度 | -- | |
反応時間 | 10 min | |
実験の流れ | Cells are preincubated with DMEM, 10 mM HEPES for 10 min at room temperature. Drugs, at concentrations ranging from 0.1 nM to 100 M, and appropriate vehicle controls, are then added in DMEM, 10 mM HEPES, 100 M forskolin and 100 M IBMX to the cells. Antagonists are added at the same time as the agonists. At the end of the treatment (10 min, room temperature), the reaction is stopped by aspiration of the medium and addition of 0.1 N HCl. Cellular extract is diluted 1:500 or 1:400 in radioimmunoassay buffer, and cAMP content is measured by using a commercially available kit. |
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動物実験 | 動物モデル | Male Sprague-Dawley rats (160 to 200 g); Male Dunkin-Hartley guinea pigs (310 to 490 ); Male White Carneau pigeons (500 to 650 g) |
投薬量 | 0.16 mg/kg | |
投与方法 | i.p. |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。