光诱导视网膜变性模型中异二甲基色胺的合成与生物学分析

Synthesis and Biological Analysis of Iso-dimethyltryptamines in a Model of Light-Induced Retinal Degeneration.

作者信息

Pazur Ethan J, Kalatanova Anna, Tasker Nikhil R, Vainionpää Katri, Leinonen Henri, Wipf Peter

机构信息

Department of Chemistry, University of Pittsburgh, Pittsburgh, Pennsylvania 15260, United States.

Yliopistonrinne 3, Canthia, School of Pharmacy, University of Eastern Finland, 70211 Kuopio, Finland.

出版信息

ACS Med Chem Lett. 2024 Jun 13;15(7):1049-1056. doi: 10.1021/acsmedchemlett.4c00130. eCollection 2024 Jul 11.

Iso-dimethyltryptamine (isoDMT) analogues with heterocyclic substitutions at the indole C(3) were prepared in a hydrogen autotransfer alkylation and tested in combination with natural and unnatural clavine alkaloids in a model of light-induced retinal degeneration for protection against retinal degeneration. On the basis of measurements with optical coherence tomography and electroretinography, three compounds showed better efficacy than the positive control bromocriptine at equivalent systemically administered doses. These studies provide further insights into the role of serotonin receptors and their potential therapeutic applications in ocular diseases.