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Doxepin HCl/盐酸多塞平 {[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 hydrochloride 是一种具有口服活性的三环类抗抑郁剂，具有多种生物活性。它是一种高选择性的组胺 H1 受体拮抗剂（Kd = 310 pM），并对 H4 受体也有拮抗作用（pKi = 6.79）。此外，Doxepin 可抑制多种 CYP450 酶，尤其是 CYP2C19 和 CYP1A2，并能阻断血清素和去甲肾上腺素的再摄取。该化合物在特应性皮炎、慢性荨麻疹、神经保护及抗氧化应激等研究领域中具有广泛应用价值。

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Doxepin HCl/盐酸多塞平 化学结构 CAS号：1229-29-4
Doxepin HCl/盐酸多塞平 化学结构
CAS号：1229-29-4
Doxepin HCl/盐酸多塞平 3D分子结构
CAS号：1229-29-4
Doxepin HCl/盐酸多塞平 化学结构 CAS号：1229-29-4
Doxepin HCl/盐酸多塞平 3D分子结构 CAS号：1229-29-4
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Doxepin HCl/盐酸多塞平 纯度/质量文件 产品仅供科研

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Doxepin HCl/盐酸多塞平 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/盐酸多塞平 细胞实验

Cell Line
Concentration Treated Time Description References
Primary mouse hepatocytes 30 μmol/L 48 hours Doxepin upregulated FAM3A expression, induced Akt phosphorylation, and suppressed gluconeogenic gene expression. Diabetes. 2020 Jun;69(6):1126-1139
HepG2 cells 30 μmol/L 48 hours Doxepin induced FAM3A expression to suppress gluconeogenesis and lipogenesis. Diabetes. 2020 Jun;69(6):1126-1139

Doxepin HCl/盐酸多塞平 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Obese diabetic mice High-fat diet-induced obese diabetic mouse model Intraperitoneal injection 5 or 10 mg/kg body weight Once daily for 4 weeks Doxepin ameliorated hyperglycemia, steatosis, and obesity, and upregulated FAM3A expression in liver and brown adipose tissues. Diabetes. 2020 Jun;69(6):1126-1139
C57BL6/J mice High-fat diet-induced obesity model Oral gavage 5 mg/kg/day Once daily for eight weeks To investigate the effects of Doxepin on renal damage, glucose intolerance, nonalcoholic fatty liver disease, and urinary chromium loss in obese mice. Results showed that Doxepin exacerbated renal injury, glucose intolerance, and fatty liver disease, and increased urinary chromium loss. Pharmaceuticals (Basel). 2021 Mar 16;14(3):267
ICR mice Pentobarbital-induced sleep model Oral 30 mg/kg Single administration Evaluate the effect of Doxepin on pentobarbital-induced sleep, results showed that Doxepin significantly decreased sleep latency and increased sleep duration. Nutrients. 2017 May 18;9(5):512

Doxepin HCl/盐酸多塞平 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/盐酸多塞平 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/盐酸多塞平 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/盐酸多塞平 技术信息

CAS号1229-29-4
分子式C19H22ClNO
分子量 315.84
SMILES Code CN(C)CC/C=C1C2=CC=CC=C2OCC3=CC=CC=C/13.Cl
MDL No. MFCD00079135
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

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, room temperature
溶解方案

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)

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一

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/盐酸多塞平 纯度/质量文件 | Doxepin HCl/盐酸多塞平 生物活性 | Doxepin HCl/盐酸多塞平 临床数据 | Doxepin HCl/盐酸多塞平 参考文献 | Doxepin HCl/盐酸多塞平 实验方案 | Doxepin HCl/盐酸多塞平 技术信息

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