|1-(3-(4-(3-氯苯基)哌嗪-1-基)丙基)-3-乙基-4-(2-苯氧基乙基)-1H-1,2,4-三唑-5(4H)-酮盐酸盐|CsnPharm

CAS No.: 82752-99-6

奈法唑酮盐酸盐 Catalog No. CSN13092

Synonyms: BMY-13754;MJ-13754-1

Nefazodone HCl is a 5-HT2A receptor antagonist with Ki of 5.8 nM and an inhibitor of serotonin and noradrenalin uptake with IC50s of 290 and 300 nM respectively, it is an antidepressant drug.

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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... more >>essive Disorder Collapse <<	Phase 4	Recruiting	January 2022	-
NCT00000286	Cocaine-Related Disorders	Phase 2	Completed	-	United States, Minnesota ... more >> University of Minnesota Minneapolis, Minnesota, United States, 55455 Collapse <<
NCT00249509	Marijuana Abuse	Phase 2	Completed	-	United States, New York ... more >> New York State Psychiatric Institute New York, New York, United States, 10032 Collapse <<

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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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9745 mL
- 9.8723 mL
- 19.7445 mL
- 5 mM
- 0.3949 mL
- 1.9745 mL
- 3.9489 mL
- 10 mM
- 0.1974 mL
- 0.9872 mL
- 1.9745 mL

技术信息

CAS号

82752-99-6

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H33Cl2N5O2

运输

蓝冰

分子量

506.47

别名

BMY-13754;MJ-13754-1

溶解度

DMSO	56.0 mg/mL (110.6 mM)
Water	insoluble

动物实验配方

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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... more >>essive Disorder Collapse <<	Phase 4	Recruiting	January 2022	-
NCT00000286	Cocaine-Related Disorders	Phase 2	Completed	-	United States, Minnesota ... more >> University of Minnesota Minneapolis, Minnesota, United States, 55455 Collapse <<
NCT00249509	Marijuana Abuse	Phase 2	Completed	-	United States, New York ... more >> New York State Psychiatric Institute New York, New York, United States, 10032 Collapse <<
NCT00231348	Social Anxiety Disorder (SAD)	Phase 4	Completed	-	United States, Georgia ... more >> Emory University Depatment of Psychiatry and Behavioral Sciences Atlanta, Georgia, United States, 30322 Collapse <<
NCT00015210	Cocaine-Related Disorders ... more >> Substance-Related Disorders Collapse <<	Phase 2	Completed	-	United States, Massachusetts ... more >> Boston University Boston, Massachusetts, United States, 02118 Collapse <<
NCT00000293	Cocaine-Related Disorders	Phase 3	Completed	-	United States, Minnesota ... more >> University of Minnesota Minneapolis, Minnesota, United States, 55455 Collapse <<
NCT00000286	Cocaine-Related Disorders	Phase 2	Completed	-	United States, Minnesota ... more >> University of Minnesota Minneapolis, Minnesota, United States, 55455 Collapse <<
NCT02977299	Treatment Resistant Major Depr... more >>essive Disorder Collapse <<	Phase 4	Recruiting	January 2022	-
NCT00231348	Social Anxiety Disorder (SAD)	Phase 4	Completed	-	United States, Georgia ... more >> Emory University Depatment of Psychiatry and Behavioral Sciences Atlanta, Georgia, United States, 30322 Collapse <<
NCT00249509	Marijuana Abuse	Phase 2	Completed	-	United States, New York ... more >> New York State Psychiatric Institute New York, New York, United States, 10032 Collapse <<
NCT00015210	Cocaine-Related Disorders ... more >> Substance-Related Disorders Collapse <<	Phase 2	Completed	-	United States, Massachusetts ... more >> Boston University Boston, Massachusetts, United States, 02118 Collapse <<
NCT00000293	Cocaine-Related Disorders	Phase 3	Completed	-	United States, Minnesota ... more >> University of Minnesota Minneapolis, Minnesota, United States, 55455 Collapse <<

奈法唑酮盐酸盐 Catalog No. CSN13092

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