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产品总数：61445
| 中文名称 |
Nefazodone
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|---|---|
| 中文别名 |
耐法唑酮;奈法唑酮;2-[3-[4-(3-氯苯基)-1-哌嗪基]丙基]-5-乙基-2,4-二氢-4-(2-苯氧基乙基)-3H-1,2,4-噻唑-3-酮;2-[3-[4-(3-氯苯基)-1-哌嗪基]丙基]-5-乙基-2,4-二氢-4-(2-苯氧基乙基)-3H-1,2,4-三唑-3-酮;2-[3-[4-(3-氯苯基)-1-哌嗪基]丙基]-5-乙基-2,4-二氢-4-(2-苯氧乙基)-3H-1,2,4-三唑-3-酮
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| 英文名称 |
Nefazodone
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| 英文别名 |
1-(3-(4-(3-Chlorophenyl)piperazin-1-yl)propyl)-3-ethyl-4-(2-phenoxyethyl)-1H-1,2,4-triazol-5(4H)-one;2-[3-[4-(3-chlorophenyl)piperazin-1-yl]propyl]-5-ethyl-4-(2-phenoxyethyl)-1,2,4-triazol-3-one;3H-1,2,4-Triazol-3-one, 2-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-5-ethyl-2,4-dihydro-4-(2-phenoxyethyl)-;Nefazodone;2-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-5-ethyl-4-(2-phenoxyethyl)-2H-1,2,4-triazol-3(4H)-one;2-<3-<4-(3-chlorophenyl)-1-piperazinyl>propyl>-5-ethyl-2,4-dihydro-4-(2-phenoxyethyl)-3H-1,2,4-triazolin-3-one;Nefazodona [Spanish];Nefazodone (INN);Nefazodone Hcl;Nefazodonum;Nefazodonum [Latin];UNII-59H4FCV1TF;2-[3-[4-(3-Chlorophenyl)-1-piperazinyl]propyl]-5-ethyl-2,4-dihydro-4-(2-phenoxyethyl)-3H-1,2,4-triazol-3-one
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| Cas No. |
83366-66-9
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| 分子式 |
C25H32N5O2Cl
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| 分子量 |
470.01
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| 包装储存 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 详情描述 |
Nefazodone 是一种具有口服活性的苯基哌嗪类抗抑郁剂。Nefazodone 可有效、选择性地阻断突触后 5-HT2A 受体，适度抑制 5-HT 和去甲肾上腺素 (noradrenaline) 再摄取。Nefazodone 还可以缓解应激反应对小鼠免疫系统的不良影响。Nefazodone 对 CYP3A4 同工酶具有较高的亲和力，表明其存在一定的药物-药物相互作用风险。
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| 产品详情 |
Nefazodone 是一种具有口服活性的苯基哌嗪类抗抑郁剂。Nefazodone 可有效、选择性地阻断突触后 5-HT2A 受体，适度抑制 5-HT 和去甲肾上腺素 (noradrenaline) 再摄取。Nefazodone 还可以缓解应激反应对小鼠免疫系统的不良影响。Nefazodone 对 CYP3A4 同工酶具有较高的亲和力，表明其存在一定的药物-药物相互作用风险。
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|---|---|
| 生物活性 |
Nefazodone is an orally active phenylpiperazine antidepressant. Nefazodone can potently and selectively block postsynaptic 5-HT 2A receptors, and moderately inhibit 5-HT and noradrenaline reuptake. Nefazodone can also relieve the adverse effects of stress on the the immune system of mice. Nefazodone has a high affinity for CYP3A4 isoenzyme, which indicates that it has certain risk of drug-drug interaction.
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| IC50 & Target[1][2] |
5-HT receptor, Noradrenaline, CYP3A4
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| 体外研究(In Vitro) |
Nefazodone collapses mitochondrial membrane potential, and imposes oxidative stress, as detected via glutathione depletion, leading to cell death.Nefazodone (200 μM; 24 h) depletes 100% of ATP in both, glucose and galactose-grown HepG2 cells.Nefazodone (6.25, 12.5 and 25 μM; 0-120 min) profoundly inhibits oxygen consumption (OCR) in HepG2. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 体内研究(In Vivo) |
Nefazodone (10 mg/kg; s.c.; for 16 days) is effective to counter the adverse effects of stress on the the immune system of mice. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: Female
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| ClinicalTrial |
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| 参考文献 |
[1]. Davis R, et al. A review of its pharmacology and clinical efficacy in the management of major depression. Drugs. 1997 Apr;53(4):608-36.[2]. Dykens JA, et al. In vitro assessment of mitochondrial dysfunction and cytotoxicity of nefazodone, trazodone, and buspirone. Toxicol Sci. 2008 Jun;103(2):335-45.
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| 溶解度数据 |
In Vitro: DMSO : 125 mg/mL (265.95 mM; Need ultrasonic)配制储备液
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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。
2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。
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