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盐酸多塞平 /Doxepin HCl {[allProObj[0].p_purity_real_show]}

货号：A783435 同义名： 盐酸多塞平 (异构体混合物) / Doxepin (hydrochloride);Doxepin Hydrochloride

Doxepin HCl, a tricyclic antidepressant, is antagonist of histamine H1 Receptor (Kd = 310 pM) and histamine H4 receptor (pKi = 6.79). It can be used to treat chronic idiopathic urticaria.

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Doxepin HCl 化学结构 CAS号：1229-29-4
Doxepin HCl 化学结构
CAS号：1229-29-4
Doxepin HCl 3D分子结构
CAS号：1229-29-4
Doxepin HCl 化学结构 CAS号：1229-29-4
Doxepin HCl 3D分子结构 CAS号：1229-29-4
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Doxepin HCl 纯度/质量文件 产品仅供科研

货号：A783435 标准纯度： {[allProObj[0].p_purity_real_show]}
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Doxepin HCl 生物活性

描述 Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2[3]. Doxepin hydrochloride is an orally active tricyclic antidepressant agent[4]. In addition, intrathecally administered doxepin, like bupivacaine and lidocaine, produced dose-related spinal anesthetic effects on motor activity, proprioception, and nociception. Doxepin produced spinal anesthetic effects in rats more potent than that of lidocaine and longer than that of bupivacaine and lidocaine[5]. Doxepin displayed a very high affinity for H1 histamine receptor, being 8-fold more potent than mepyramine. Doxepin showed significant H2 blocking activity which was 5 times less potent than that of cimetidine. Doxepin competitively antagonized carbachol in the guinea pig ileum, and was 107 times less potent than atropine[6]. In PC3 cells, doxepin induced a [Ca²⁺](i) rise by evoking PLC-independent Ca²⁺ release from stores including the endoplasmic reticulum and Ca²⁺ entry via PKC-sensitive store-operated Ca²⁺ channels. Doxepin caused cell death that was independent of [Ca²⁺](i) rises[7].

Doxepin HCl 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
NCT02191358 - Completed - United States, California ... 展开 >> Dr. Michael Dao Garden Grove, California, United States, 92844 United States, Colorado Kaiser Permanente Colorado Denver, Colorado, United States, 80011 United States, Kentucky Gill Heart Institute Lexington, Kentucky, United States, 40508 United States, Maryland IRC Clinics Towson, Maryland, United States, 21204 United States, Massachusetts Internal Medicine & Cardiology Associates Fall River, Massachusetts, United States, 02720 Prima CARE Fall River, Massachusetts, United States, 02720 United States, Virginia Carilion Clinic Christiansburg, Virginia, United States, 24073 收起 <<
NCT02374567 Dementia Depr... 展开 >>ession Schizophrenia Psychosomatic Disorders Anxiety Disorders 收起 << Phase 3 Terminated - Germany ... 展开 >> Bezirkskrankenhaus Augsburg Augsburg, Germany Krankenhaus Hedwigshöhe Berlin, Germany Hannover Medical School Hannover, Germany, 30625 Asklepios Fachklinikum Lübben Lübben, Germany Asklepios Fachklinikum Teupitz Teupitz, Germany 收起 <<
NCT02297126 Adverse Drug Reaction Not Applicable Completed - United States, Indiana ... 展开 >> Eskenazi Health System Indianapolis, Indiana, United States, 46250 收起 <<

Doxepin HCl 参考文献

[1]Nguyen T, Shapiro DA, et al. Discovery of a novel member of the histamine receptor family. Mol Pharmacol. 2001 Mar;59(3):427-33.

[2]Luchins DJ. Review of clinical and animal studies comparing the cardiovascular effects of doxepin and other tricyclic antidepressants. Am J Psychiatry. 1983 Aug;140(8):1006-9.

[3]Hajak G, Rodenbeck A, Voderholzer U, Riemann D, Cohrs S, Hohagen F, Berger M, Rüther E. Doxepin in the treatment of primary insomnia: a placebo-controlled, double-blind, polysomnographic study. J Clin Psychiatry. 2001 Jun;62(6):453-63

[4]Singh H, Becker PM. Novel therapeutic usage of low-dose doxepin hydrochloride. Expert Opin Investig Drugs. 2007 Aug;16(8):1295-305

[5]Cheng BC, Chan BR, Chen YW, Chu KS, Cheng KI, Wang JJ, Chu CC. Doxepin has a potent and long-acting spinal anesthetic effect in rats. Kaohsiung J Med Sci. 2006 Feb;22(2):68-74

[6]Figueiredo A, Ribeiro CA, Gonçalo M, Almeida L, Poiares-Baptista A, Teixeira F. Mechanism of action of doxepin in the treatment of chronic urticaria. Fundam Clin Pharmacol. 1990;4(2):147-58

[7]Lu T, Chou CT, Liang WZ, Yu CC, Chang HT, Kuo CC, Chen WC, Kuo DH, Ho CM, Shieh P, Jan CR. Effect of Antidepressant Doxepin on Ca²⁺ Homeostasis and Viability in PC3 Human Prostate Cancer Cells. Chin J Physiol. 2015 Jun 30;58(3):178-87

Doxepin HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.17mL

0.63mL

0.32mL

15.83mL

3.17mL

1.58mL

31.66mL

6.33mL

3.17mL

Doxepin HCl 技术信息

CAS号1229-29-4
分子式C19H22ClNO
分子量 315.837
别名 盐酸多塞平 (异构体混合物) ;Doxepin (hydrochloride);Doxepin Hydrochloride
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature
溶解度

DMSO: 105 mg/mL(332.45 mM)，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: 50 mg/mL(158.31 mM)
动物实验配方

Tags: Doxepin | 1229-29-4 | Histamine Receptor | Cytochrome P450 | GPCR/G Protein | Neuronal Signaling | Immunology/Inflammation | Metabolic Enzyme/Protease | Histamine Receptor | Cytochrome P450 | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Doxepin HCl 纯度/质量文件 | Doxepin HCl 生物活性 | Doxepin HCl 临床数据 | Doxepin HCl 参考文献 | Doxepin HCl 实验方案 | Doxepin HCl 技术信息

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