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

被引：1

作者：

Pazur, Ethan J. ^{[1
]}

Kalatanova, Anna ^{[2
]}

Tasker, Nikhil R. ^{[1
]}

Vainionpaa, Katri ^{[2
]}

Leinonen, Henri ^{[2
]}

Wipf, Peter ^{[1
,2
]}

机构：

[1] Univ Pittsburgh, Dept Chem, Pittsburgh, PA 15260 USA

[2] Univ Eastern Finland, Sch Pharm, Yliopistonrinne 3, Kuopio 70211, Finland

来源：

ACS MEDICINAL CHEMISTRY LETTERS | 2024年

基金：

芬兰科学院;

关键词：

Serotonin Receptor Agonists; 5-HTR; Ergot Alkaloids; Iso-dimethyltryptamines; LIRD; Ophthalmology; Retinal Diseases; MACULAR DEGENERATION; STARGARDT DISEASE; DAMAGE; MICE; SUSCEPTIBILITY; PHARMACOLOGY; RETINOPATHY; DISCOVERY; APOPTOSIS; COMPONENT;

D O I：

10.1021/acsmedchemlett.4c00130

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：1049 / 1056

页数：8

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