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CAS No. : 521-78-8
MCE 国际站:Trimipramine maleate
产品活性: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。Trimipramine maleate 也是一种靶向人去甲肾上腺素 (hNAT)、血清素 (hSERT) 和有机阳离子转运体 (hOCT1、hOCT2) 的有选择性和强效的抑制剂,其 IC50 值分别为 4.99 μM、2.11 μM、3.72 μM、8.00 μM。Trimipramine maleate 具有血管活性和抗焦虑作用。
研究领域:GPCR/G Protein | Neuronal Signaling | Anti-infection
作用靶点:5-HT Receptor | Bacterial
In Vitro: Trimipramine maleate displays much higher affinity for 5-HT2 than for 5-HT1C receptors.
?Trimipramine maleate is a moderate inhibitor of the human NAT and SERT, with the IC50 values of 4.99 μM and 2.11 μM, respectively.
?SERT and NAT could represent a target for the antidepressant effects of trimipramine maleate (1 mM, 0.1 mM, 0.01 mM, 1 μM, 0.1 μM; 10 min; HEK293 cells).
In Vivo: Trimipramine maleate (5 mg/kg/d; 14 d; chronic administration) acts as functions in rats:1. Increasing concentration of regional 5-HT. 5-HT is highest in the frontal cortex and the hippocampus, followed by the olfactory tubercles and the hypothalamus. 2. Decreasing the number of frontal cortex 5-HT2 and striatal DA D2 receptors. 3. Increasing in the brain regional level of monoamines and metabolites. thus indicates a greater synthesis rate for dopamine (DA) and 5-HT coinciding with an adaptive down regulation of 5-HT2 and DA D2 receptors.
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