Doxepin (hydrochloride)
(Synonyms: 盐酸多塞平) 目录号 : GC12892
A tricyclic antidepressant
Cas No.:1229-29-4
Sample solution is provided at 25 µL, 10mM.
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Doxepin, a tricyclic antidepressant, is a potent histamine H1 antagonist [1]. The histamine receptors belong to a family of G protein–coupled receptors activated by their primary endogenous ligand histamine. The H1 receptor has been expressed in smooth muscles, vascular endothelial cells, heart, and the central nervous system [2].
In vitro: Doxepin was a moderately potent competitive inhibitor of serotonin uptake in human blood platelets in vitro, with an inhibitory constant Ki of ～0.2 μM. Doxepin (100 μM) rapidly increased the efflux of serotonin from platelets [1].
In vivo: In rats and dog, oral administration of doxepin was well absorbed and quickly appeared in the blood. Numerous metabolites of doxepin were observed in liver and in urine, only doxepin and demethyl doxepin were found in the rat brain[3]..
Clinical trials: Doxepin has been marketed under many brand names worldwide. The oral topical formulations of doxepin are FDA-approved for the treatment of patients with major depressive disorder, primary insomnia, chronic urticaria, and anxiety [4,5,6].
References:
[1] Lingjrde O. Effect of doxepin on uptake and efflux of serotonin in human blood patelets in vitro[J]. Psychopharmacology, 1976, 47(2): 183-186.
[2] Hill S J, Ganellin C R, Timmerman H, et al. International Union of Pharmacology. XIII. Classification of histamine receptors[J]. Pharmacological reviews, 1997, 49(3): 253-278.
[3] Hobbs D C. Distribution and metabolism of doxepin[J]. Biochemical pharmacology, 1969, 18(8): 1941-1954.
[4] Hajak G, Rodenbeck A, Voderholzer U, et al. Doxepin in the treatment of primary insomnia: a placebo-controlled, double-blind, polysomnographic study[J]. Journal of Clinical Psychiatry, 2001, 62(6): 453-463.
[5] Feighner J P, Cohn J B. Double-blind comparative trials of fluoxetine and doxepin in geriatric patients with major depressive disorder[J]. The Journal of clinical psychiatry, 1985, 46(3 Pt 2): 20-25.
[6] Goldsobel A B, Rohr A S, Siegel S C, et al. Efficacy of doxepin in the treatment of chronic idiopathic urticaria[J]. Journal of allergy and clinical immunology, 1986, 78(5): 867-873.
| Cas No. | 1229-29-4 | SDF | |
| 别名 | 盐酸多塞平 | ||
| 化学名 | 3-(dibenz[b,e]oxepin-11(6H)-ylidene)-N,N-dimethyl-1-propanamine, monohydrochloride | ||
| Canonical SMILES | CN(C)CC/C=C1C2=C(C=CC=C2)COC3=C/1C=CC=C3.Cl | ||
| 分子式 | C19H21NO • HCl | 分子量 | 315.8 |
| 溶解度 | ≥ 15.85mg/mL in DMSO | 储存条件 | Store at RT |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.1666 mL | 15.8328 mL | 31.6656 mL |
| 5 mM | 0.6333 mL | 3.1666 mL | 6.3331 mL |
| 10 mM | 0.3167 mL | 1.5833 mL | 3.1666 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet