Nefazodone

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，表明其存在一定的活性分子-活性分子相互作用风险。

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货号: ajcf20780
CAS: 83366-66-9
别名: 奈法唑酮
分子式: C25H32ClN5O2
分子量: 470.01
纯度: >98%
溶解度: DMSO : 125 mg/mL (265.95 mM; Need ultrasonic)
储存: Store at -20°C
库存: 现货

Background

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 agent-agent interaction^[1]^[2]^[3].

Nefazodone collapses mitochondrial membrane potential, and imposes oxidative stress, as detected via glutathione depletion, leading to cell death^[2].
Nefazodone (200 μM; 24 h) depletes 100% of ATP in both, glucose and galactose-grown HepG2 cells^[2].
Nefazodone (6.25, 12.5 and 25 μM; 0-120 min) profoundly inhibits oxygen consumption (OCR) in HepG2^[2].

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^[3].

Animal Model:	Female BALB/c mice (7-12 weeks old; stress model; subjected to a broad band noise at 100 dB daily for 5 s every minute during a 1- or 3-h period around midnight)^[3]
Dosage:	10 mg/kg
Administration:	s.c.; for 16 days
Result:	Attenuated the reduction of tmus, spleen and peripheral blood cellularity caused by stress.

[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.
[3]. Freire-Garabal M, et al. Effects of nefazodone on the immune system of mice. Eur Neuropsychopharmacol. 2000 Jul;10(4):255-64.