Trimipramine maleate

Trimipramine maleate Elisa Q. 2020-07-11T20:20:00+08:00

Trimipramine maleate

Trimipramine maleate 是 5-HT 受体的拮抗剂，其对 5-HT1C，5-HT2 和 5-HT1A 受体的 pKi 值分别为 6.39，8.10，4.66。

中文名：马来酸三甲丙咪嗪

英文名：Trimipramine maleate

CAS 号： 521-78-8

分子式：C₂₄H₃₀N₂O₄

分子量：410.506

纯度：>98.0%

Description	Trimipramine maleate is a 5-HT receptor antagonist, with pKis of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively.
Target	5-HT Receptor；sPLA2
In Vitro	Trimipramine displays much higher affinity for 5-HT2 than for 5-HT1C receptors[1].
In Vivo	The chronic administration of Trimipramine (5 mg/kg/day), as delivered by the osmotic minipump in 14 days produce significant increases in the regional concentration of 5-HT. The increases are highest in the frontal cortex and the hippocampus, followed by the olfactory tubercles and the hypothalamus. The Trimipramine treatment also produces marked increases in brain 5-HIAA concentrations ranging from 63% in the hippocampus to 25% in the nucleus accumbens with intermediate values for the hypothalamus, olfactory tubercles, frontal cortex and nucleus accumbens. Trimipramine treatment produces significant increases in DA concentrations in the nucleus accumbens, striaturn, and olfactory tubercles reaching 43, 21 and 11% respectively. Chronic administration of Trimipramine produces a marked reduction in the number of frontal cortex 5-HT2 and striatal DA D2 receptors. The chronic administration of Trimipramine produces an increase in the brain regional level of monoamines and metabolites indicating a greater synthesis rate for DA and 5-HT coinciding with an adaptive down regulation of 5-HT2 and DA D2 receptors[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. [2]. Juorio AV, et al. The effects of chronic trimipramine treatment on biogenic amine metabolism and on dopamine D2, 5-HT2 and tryptamine binding sites in rat brain. Gen Pharmacol. 1990;21(5):759-62.

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