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Dopamine D3 Receptor Antagonists as Potential Therapeutics for the Treatment of Neurological Diseases
D3 receptors represent a major focus of current drug design and development of therapeutics for dopamine-related pathological states. Their close homology with the D2 receptor subtype makes the development of D3 selective antagonists a challenging task. In this review, we explore the relevance and t...
Autores principales: | , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Frontiers Media S.A.
2016
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5050208/ https://www.ncbi.nlm.nih.gov/pubmed/27761108 http://dx.doi.org/10.3389/fnins.2016.00451 |
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author | Maramai, Samuele Gemma, Sandra Brogi, Simone Campiani, Giuseppe Butini, Stefania Stark, Holger Brindisi, Margherita |
author_facet | Maramai, Samuele Gemma, Sandra Brogi, Simone Campiani, Giuseppe Butini, Stefania Stark, Holger Brindisi, Margherita |
author_sort | Maramai, Samuele |
collection | PubMed |
description | D3 receptors represent a major focus of current drug design and development of therapeutics for dopamine-related pathological states. Their close homology with the D2 receptor subtype makes the development of D3 selective antagonists a challenging task. In this review, we explore the relevance and therapeutic utility of D3 antagonists or partial agonists endowed with multireceptor affinity profile in the field of central nervous system disorders such as schizophrenia and drug abuse. In fact, the peculiar distribution and low brain abundance of D3 receptors make them a valuable target for the development of drugs devoid of motor side effects classically elicited by D2 antagonists. Recent research efforts were devoted to the conception of chemical templates possibly endowed with a multi-target profile, especially with regards to other G-protein-coupled receptors (GPCRs). A comprehensive overview of the recent literature in the field is herein provided. In particular, the evolution of the chemical templates has been tracked, according to the growing advancements in both the structural information and the refinement of the key pharmacophoric elements. The receptor/multireceptor affinity and functional profiles for the examined compounds have been covered, together with their most significant pharmacological applications. |
format | Online Article Text |
id | pubmed-5050208 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2016 |
publisher | Frontiers Media S.A. |
record_format | MEDLINE/PubMed |
spelling | pubmed-50502082016-10-19 Dopamine D3 Receptor Antagonists as Potential Therapeutics for the Treatment of Neurological Diseases Maramai, Samuele Gemma, Sandra Brogi, Simone Campiani, Giuseppe Butini, Stefania Stark, Holger Brindisi, Margherita Front Neurosci Pharmacology D3 receptors represent a major focus of current drug design and development of therapeutics for dopamine-related pathological states. Their close homology with the D2 receptor subtype makes the development of D3 selective antagonists a challenging task. In this review, we explore the relevance and therapeutic utility of D3 antagonists or partial agonists endowed with multireceptor affinity profile in the field of central nervous system disorders such as schizophrenia and drug abuse. In fact, the peculiar distribution and low brain abundance of D3 receptors make them a valuable target for the development of drugs devoid of motor side effects classically elicited by D2 antagonists. Recent research efforts were devoted to the conception of chemical templates possibly endowed with a multi-target profile, especially with regards to other G-protein-coupled receptors (GPCRs). A comprehensive overview of the recent literature in the field is herein provided. In particular, the evolution of the chemical templates has been tracked, according to the growing advancements in both the structural information and the refinement of the key pharmacophoric elements. The receptor/multireceptor affinity and functional profiles for the examined compounds have been covered, together with their most significant pharmacological applications. Frontiers Media S.A. 2016-10-05 /pmc/articles/PMC5050208/ /pubmed/27761108 http://dx.doi.org/10.3389/fnins.2016.00451 Text en Copyright © 2016 Maramai, Gemma, Brogi, Campiani, Butini, Stark and Brindisi. http://creativecommons.org/licenses/by/4.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms. |
spellingShingle | Pharmacology Maramai, Samuele Gemma, Sandra Brogi, Simone Campiani, Giuseppe Butini, Stefania Stark, Holger Brindisi, Margherita Dopamine D3 Receptor Antagonists as Potential Therapeutics for the Treatment of Neurological Diseases |
title | Dopamine D3 Receptor Antagonists as Potential Therapeutics for the Treatment of Neurological Diseases |
title_full | Dopamine D3 Receptor Antagonists as Potential Therapeutics for the Treatment of Neurological Diseases |
title_fullStr | Dopamine D3 Receptor Antagonists as Potential Therapeutics for the Treatment of Neurological Diseases |
title_full_unstemmed | Dopamine D3 Receptor Antagonists as Potential Therapeutics for the Treatment of Neurological Diseases |
title_short | Dopamine D3 Receptor Antagonists as Potential Therapeutics for the Treatment of Neurological Diseases |
title_sort | dopamine d3 receptor antagonists as potential therapeutics for the treatment of neurological diseases |
topic | Pharmacology |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5050208/ https://www.ncbi.nlm.nih.gov/pubmed/27761108 http://dx.doi.org/10.3389/fnins.2016.00451 |
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