产品说明书
Doxepin HCl
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同义名 : | 盐酸多塞平 (异构体混合物) ;Doxepin (hydrochloride);Doxepin Hydrochloride |
| CAS号 : | 1229-29-4 | |
| 货号 : | A783435 | |
| 分子式 : | C19H22ClNO | |
| 纯度 : | 98% | |
| 分子量 : | 315.837 | |
| MDL号 : | MFCD00079135 | |
| 存储条件： |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 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) |
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| 动物实验配方： |
| 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]. | ||
| 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 << |
| 实验方案 | |||
|---|---|---|---|
| 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 |
| 参考文献 |
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