Trimipramine (maleate)
(Synonyms: 三甲丙咪嗪马来酸盐) 目录号 : GC17488
A tricyclic antidepressant
Cas No.:521-78-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | Rats[2]Male Wistar rats weighing 220-250 g at the beginning of the experiment are used. The animals, housed in groups of 6-8 have free access to food and water and are kept on a 12 hr light/dark cycle (light on at 6a.m.) at a temperature. The rats are anaesthetized with pentobarbital (50 mg/kg i.p.) and an osmotic minipump is implanted subcutaneously in the dorsal thoracic interscapular region. Each pump delivers 5 mg/kg/day of Trimipramine or amitriptyline. Control rats are implanted with pumps filled with 0.9%, saline. The total volume of solution in the pump is sufficient for at least 14 days delivery of drugs. After implantation, the incision is cleaned and sutured and the animals kept warm until they recovered from anaesthesia[2]. |
References: [1]. Jenck F, et al. Evidence for a role of 5-HT1C receptors in the antiserotonergic properties of some antidepressant drugs. Eur J Pharmacol. 1993 Feb 9;231(2):223-9. | |
Trimipramine (maleate) is a potent antagonist of histamine H1 receptor, serotonin 5-HT2A, and α1-adrenergic receptors [1].
The histamine H1 receptor is widely expressed tissues, such as smooth muscles, vascular endothelial cells, heart, and the central nervous system. Histamine H1 receptor (H1R) antagonists are very effective drugs alleviating the symptoms of allergic reactions [2]. 5-HT2A receptor shows constitutive activity. Variations in5-HT2A receptor can produce profound alterations in cognitive states [3]. The adrenergic receptors play an important role in modulating sympathetic nervous system activity as well as a site of action for many therapeutic agents. The α1-adrenergic receptor is the prime mediators of smooth muscle contraction and hypertrophic growth. The α1-adrenergic receptor plays an essential role in smooth muscle, growth, neurological, and cardiovascular function [4].
Trimipramine (maleate) is a tricyclic antidepressant compound that antagonizes several types of neurotransmitter receptors. Trimipramine potently antagonized the activity of histamine H1 serotonin 5-HT2A, and α1-adrenergic receptors with the Kd value of 0.27 nM, 24 nM, and 24 nM, respectively. Trimipramine moderately antagonized the activity of dopamine D2 with the Kd of 180 nM. Trimipramine inhibited the activity of muscarinic acetylcholine with the Kd of 58 nM. Trimipramine weakly inhibited the activity of 5-HT2C, D1, α2-adrenergic receptors (Kd = 680 nM) [1]. Trimipramine (maleate) was a weak to moderate reuptake inhibitor of serotonin (Ki = 149 nM for SERT), and an extremely weak inhibitor of norepinephrine (Ki = 2.5 μM for NET) and dopamine (Ki = 3.8 μM for DAT) reuptake in slices of rat cerebral cortex [5,6].
References:
[1] Richelson E, Nelson A. Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro[J]. Journal of Pharmacology and Experimental Therapeutics, 1984, 230(1): 94-102.
[2] Shimamura T, Shiroishi M, Weyand S, et al. Structure of the human histamine H1 receptor complex with doxepin[J]. Nature, 2011, 475(7354): 65-70.
[3] Harvey J A. Role of the serotonin 5-HT2A receptor in learning[J]. Learning & Memory, 2003, 10(5): 355-362.
[4] Piascik M T, Perez D M. α1-Adrenergic receptors: new insights and directions[J]. Journal of Pharmacology and Experimental Therapeutics, 2001, 298(2): 403-410.
[5] Gross G, Xie X, Gastpar M. Trimipramine: pharmacological reevaluation and comparison with clozapine[J]. Neuropharmacology, 1991, 30(11): 1159-1166.
[6] Tatsumi M, Groshan K, Blakely R D, et al. Pharmacological profile of antidepressants and related compounds at human monoamine transporters[J]. European journal of pharmacology, 1997, 340(2): 249-258.
| Cas No. | 521-78-8 | SDF | |
| 别名 | 三甲丙咪嗪马来酸盐 | ||
| 化学名 | 10,11-dihydro-N,N,β-trimethyl-5H-dibenz[b,f]azepine-5-propanamine(2Z)-2-butenedioate | ||
| Canonical SMILES | CN(C)CC(C)CN1C2=C(C=CC=C2)CCC3=C1C=CC=C3.OC(/C=C\C(O)=O)=O | ||
| 分子式 | C20H26N2 • C4H4O4 | 分子量 | 410.5 |
| 溶解度 | ≥ 18.5mg/mL in DMSO | 储存条件 | Store at -20°C |
| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4361 mL | 12.1803 mL | 24.3605 mL |
| 5 mM | 0.4872 mL | 2.4361 mL | 4.8721 mL |
| 10 mM | 0.2436 mL | 1.218 mL | 2.4361 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。
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