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Nefazodone hydrochloride

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Chemical Structure| 82752-99-6 同义名 : 萘法唑酮盐酸盐 ;BMY-13754;MJ-13754-1;Nefazodone (hydrochloride);BMY-13754-1
CAS号 : 82752-99-6
货号 : A989627
分子式 : C25H33Cl2N5O2
纯度 : 98%
分子量 : 506.468
MDL号 : MFCD00935760
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(98.72 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 2 mg/mL(3.95 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 Nefazodone HCl (Serzone), a potent antagonist of 5-HT2A receptors, is a new antidepressant. Nefazodone also binds to the norepinephrine transporter in vitro and in acute ex vivo studies. Acute administration of nefazodone (30, 100, and 150 mg/kg) antagonized PCA-induced depletion of cortical 5-HT concentrations in a dose-dependent manner at 1, 2, and 3 hours post-treatment. Acute administration of nefazodone (100 and 150 mg/kg s.c.) significantly increased the Km for [3H]-5-HT uptake in rat cortical synaptosomes from 60 nM in controls to 230 and 242 nM in nefazodone-treated rats, respectively. Subchronic administration of nefazodone (100 and 150 mg/kg, s.c., b.i.d. x 5.5 days) reduced [3H]-5-HT uptake by 24% and 29%, respectively. Sub-chronic dosing with fluoxetine (5 mg/kg, s.c., b.i.d. x 5.5 days) reduced [3H]-5-HT uptake by 65%[3]. NEF (Nefazodone) is absorbed throughout the length of the gastro-intestinal tract which supports the development of an extended-release formulation of NEF. The exposure to the metabolites (relative to NEF) was lower from the distal intestinal site compared to the proximal and oral site which may be explained by a reduced first pass of NEF by the cytochrome P450 3A4 in the distal intestine[4].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02977299 Treatment Resistant Major Depr... 展开 >>essive Disorder 收起 << Phase 4 Recruiting January 2022 -
NCT00000286 Cocaine-Related Disorders Phase 2 Completed - United States, Minnesota ... 展开 >> University of Minnesota Minneapolis, Minnesota, United States, 55455 收起 <<
NCT00249509 Marijuana Abuse Phase 2 Completed - United States, New York ... 展开 >> New York State Psychiatric Institute New York, New York, United States, 10032 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.97mL

0.39mL

0.20mL

9.87mL

1.97mL

0.99mL

19.74mL

3.95mL

1.97mL
参考文献

[1]Davis R, Whittington R, et al. Nefazodone. A review of its pharmacology and clinical efficacy in the management of major depression. Drugs. 1997 Apr;53(4):608-36.

[2]Eison AS, Eison MS, et al. Nefazodone: preclinical pharmacology of a new antidepressant. Psychopharmacol Bull. 1990;26(3):311-5.

[3]Owens MJ, Ieni JR, Knight DL, Winders K, Nemeroff CB. The serotonergic antidepressant nefazodone inhibits the serotonin transporter: in vivo and ex vivo studies. Life Sci. 1995;57(24):PL373‐PL380

[4]Marathe PH, Salazar DE, Greene DS, Brennan J, Shukla UA, Barbhaiya RH. Absorption and presystemic metabolism of nefazodone administered at different regions in the gastrointestinal tract of humans. Pharm Res. 1995;12(11):1716‐1721