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5-HT2A 受体拮抗剂 M100907 减少 5-羟色胺合成：一项放射自显影研究。

5-HT2A receptor antagonist M100907 reduces serotonin synthesis: an autoradiographic study.

机构信息

Cone Neurosurgical Research Laboratory, Department of Neurology and Neurosurgery, Montreal Neurological Institute, McGill University, 3801 University Street, Montreal, Quebec, Canada H3A 2B4.

出版信息

Brain Res Bull. 2012 Jan 4;87(1):44-9. doi: 10.1016/j.brainresbull.2011.10.009. Epub 2011 Oct 25.

DOI:10.1016/j.brainresbull.2011.10.009
PMID:22056993
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3653840/
Abstract

The effects of the administration of the serotonin (5-HT)(2A) antagonist, M100907, on 5-HT synthesis rates, were evaluated using the α-[(14)C]methyl-l-tryptophan (α-MTrp) autoradiographic method. In the treatment study, M100907 (10mg/kg) was injected intraperitoneally 30 min before the α-MTrp injection (30 μCi over 2 min). A single dose of M100907 caused a significant decrease in the synthesis in the anterior olfactory nucleus, accumbens nucleus, frontal cortex, sensory-motor cortex, cingulate cortex, medial caudate-putamen, dorsal thalamus, substantia nigra, inferior collicus, raphe magnus nucleus, superior olive, and raphe pallidus nucleus. These data suggest that the terminal 5-HT(2A) receptors are involved in the regulation of 5-HT synthesis in the entire brain. Further, 5-HT synthesis is likely regulated by the 5-HT(2A) antagonistic property of M100907 in the cortices, anterior olfactory nucleus, caudate putamen, and nucleus accumbens.

摘要

采用α-[(14)C]甲基-l-色氨酸（α-MTrp）放射自显影法评估了 5-羟色胺（5-HT）（2A）拮抗剂 M100907 对 5-HT 合成率的影响。在治疗研究中，M100907（10mg/kg）在α-MTrp 注射前 30 分钟（2 分钟内 30μCi）腹腔内注射。单次给予 M100907 可显著降低前嗅核、伏隔核、额叶皮质、感觉运动皮质、扣带回皮质、内侧尾壳核、背侧丘脑、黑质、下丘、中缝大核、上橄榄核和苍白球核的合成。这些数据表明，终端 5-HT（2A）受体参与了整个大脑中 5-HT 合成的调节。此外，5-HT 的合成可能受到 M100907 在皮质、前嗅核、尾壳核和伏隔核中的 5-HT（2A）拮抗特性的调节。

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