Nefazodone_product_DataBase

Bioactivity

Nefazodone is an orally active phenylpiperazine antidepressant. Nefazodone can potently and selectively block postsynaptic 5-HT2A 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[1][2][3].

Target

5-HT receptor, Noradrenaline, CYP3A4

Invitro

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].

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[3]. Animal Model:

Name

Nefazodone

CAS

83366-66-9

Formula

C25H32ClN5O2

Molar Mass

470.01

Appearance

Oil

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Pure form	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[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.

PeptideDB

Nefazodone

CAS: 83366-66-9 F: C25H32ClN5O2 W: 470.01