| CAS NO: | 521-78-8 |
| 包装 | 价格(元) |
| 1g | 电议 |
| 5g | 电议 |
| Storage | Store at -20°C |
| M.Wt | 410.5 |
| Cas No. | 521-78-8 |
| Formula | C20H26N2·C4H4O4 |
| Solubility | insoluble in H2O; ≥13.02 mg/mL in EtOH; ≥18.5 mg/mL in DMSO |
| Chemical Name | 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 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
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.
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