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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...
Autores principales: | , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2022
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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. |
format | Online Article Text |
id | pubmed-9822192 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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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