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Allosteric Modulators of Dopamine D(2) Receptors for Fine-Tuning of Dopaminergic Neurotransmission in CNS Diseases: Overview, Pharmacology, Structural Aspects and Synthesis

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...

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Detalles Bibliográficos
Autores principales: Kaczor, Agnieszka A., Wróbel, Tomasz M., Bartuzi, Damian
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9822192/
https://www.ncbi.nlm.nih.gov/pubmed/36615372
http://dx.doi.org/10.3390/molecules28010178
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author Kaczor, Agnieszka A.
Wróbel, Tomasz M.
Bartuzi, Damian
author_facet Kaczor, Agnieszka A.
Wróbel, Tomasz M.
Bartuzi, Damian
author_sort Kaczor, Agnieszka A.
collection PubMed
description 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 D(2) 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 D(2) receptor modulators is presented, ranging from their pharmacology and structural aspects of ligand-receptor interactions to their synthesis.
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spelling pubmed-98221922023-01-07 Allosteric Modulators of Dopamine D(2) Receptors for Fine-Tuning of Dopaminergic Neurotransmission in CNS Diseases: Overview, Pharmacology, Structural Aspects and Synthesis Kaczor, Agnieszka A. Wróbel, Tomasz M. Bartuzi, Damian Molecules Review 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 D(2) 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 D(2) receptor modulators is presented, ranging from their pharmacology and structural aspects of ligand-receptor interactions to their synthesis. MDPI 2022-12-25 /pmc/articles/PMC9822192/ /pubmed/36615372 http://dx.doi.org/10.3390/molecules28010178 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Review
Kaczor, Agnieszka A.
Wróbel, Tomasz M.
Bartuzi, Damian
Allosteric Modulators of Dopamine D(2) Receptors for Fine-Tuning of Dopaminergic Neurotransmission in CNS Diseases: Overview, Pharmacology, Structural Aspects and Synthesis
title Allosteric Modulators of Dopamine D(2) Receptors for Fine-Tuning of Dopaminergic Neurotransmission in CNS Diseases: Overview, Pharmacology, Structural Aspects and Synthesis
title_full Allosteric Modulators of Dopamine D(2) Receptors for Fine-Tuning of Dopaminergic Neurotransmission in CNS Diseases: Overview, Pharmacology, Structural Aspects and Synthesis
title_fullStr Allosteric Modulators of Dopamine D(2) Receptors for Fine-Tuning of Dopaminergic Neurotransmission in CNS Diseases: Overview, Pharmacology, Structural Aspects and Synthesis
title_full_unstemmed Allosteric Modulators of Dopamine D(2) Receptors for Fine-Tuning of Dopaminergic Neurotransmission in CNS Diseases: Overview, Pharmacology, Structural Aspects and Synthesis
title_short Allosteric Modulators of Dopamine D(2) Receptors for Fine-Tuning of Dopaminergic Neurotransmission in CNS Diseases: Overview, Pharmacology, Structural Aspects and Synthesis
title_sort allosteric modulators of dopamine d(2) receptors for fine-tuning of dopaminergic neurotransmission in cns diseases: overview, pharmacology, structural aspects and synthesis
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9822192/
https://www.ncbi.nlm.nih.gov/pubmed/36615372
http://dx.doi.org/10.3390/molecules28010178
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