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Allosteric Modulators of Dopamine D2 Receptors for Fine-Tuning of Dopaminergic Neurotransmission in CNS Diseases: Overview, Pharmacology, Structural Aspects and Synthesis

Authors :
Agnieszka A. Kaczor
Tomasz M. Wróbel
Damian Bartuzi
Source :
Molecules, Vol 28, Iss 1, p 178 (2022)
Publication Year :
2022
Publisher :
MDPI AG, 2022.

Abstract

Allosteric modulation of G protein-coupled receptors (GPCRs) is nowadays a hot topic in medicinal chemistry. Allosteric modulators, i.e., compounds which bind in a receptor site topologically distinct from orthosteric sites, exhibit a number of advantages. They are more selective, safer and display a ceiling effect which prevents overdosing. Allosteric modulators of dopamine D2 receptor are potential drugs against a number of psychiatric and neurological diseases, such as schizophrenia and Parkinson’s disease. In this review, an insightful summary of current research on D2 receptor modulators is presented, ranging from their pharmacology and structural aspects of ligand-receptor interactions to their synthesis.

Details

Language :
English
ISSN :
14203049
Volume :
28
Issue :
1
Database :
Directory of Open Access Journals
Journal :
Molecules
Publication Type :
Academic Journal
Accession number :
edsdoj.3723876c7fb04968ae4c87dcd67ceb5b
Document Type :
article
Full Text :
https://doi.org/10.3390/molecules28010178