Structure-based development of caged dopamine D₂/D₃ receptor antagonists.

ABSTRACT: Dopamine is a neurotransmitter of great physiological relevance. Disorders in dopaminergic signal transduction are associated with psychiatric and neurological pathologies such as Parkinson's disease, schizophrenia and substance abuse. Therefore, a detailed understanding of dopaminergic neurotransmission may provide access to novel therapeutic strategies for the treatment of these diseases. Caged compounds with photoremovable groups represent molecular tools to investigate a biological target with high spatiotemporal resolution. Based on the crystal structure of the D₃ receptor in complex with eticlopride, we have developed caged D₂/D₃ receptor ligands by rational design. We initially found that eticlopride, a widely used D₂/D₃ recepto

SUBMITTER: Gienger M 

PROVIDER: S-EPMC6972920 | biostudies-literature | 2020 Jan

REPOSITORIES: biostudies-literature