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Trimipramine maleate

CAS No. : 521-78-8

MCE 站：Trimipramine maleate

产品活性：Trimipramine maleate 是 5-HT 受体的拮抗剂，其对 5-HT_1C，5-HT₂ 和 5-HT_1A 受体的 pK_i 值分别为 6.39，8.10，4.66。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Anti-infection

作用靶点：5-HT Receptor  |  Bacterial

In Vitro: Trimipramine displays much higher affinity for 5-HT₂ than for 5-HT_1C receptors.

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.

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