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

IsoDMT analogs with heterocyclic substitutions at the indole C(3) were prepared in a hydrogen-autotransfer (HA) alkylation and tested in combination with natural and unnatural clavine alkaloids in a model of light-induced retinal degeneration for protection against retinal degeneration. As assessed with OCT and ERG, three compounds showed better efficacy than positive-control bromocriptine at equivalent systemically administered doses. These studies provide further insight into the role that 5-HT receptors play in ocular diseases.