Current knowledge and perspectives on histamine H1 and H2 receptor pharmacology: Functional selectivity, receptor crosstalk, and repositioning of classic histaminergic ligands
- Autores
- Monczor, Federico; Fernandez, Natalia Cristina
- Año de publicación
- 2016
- Idioma
- inglés
- Tipo de recurso
- artículo
- Estado
- versión publicada
- Descripción
- H1 and H2 histamine receptor antagonists, although developed many decades ago, are still effective for the treatment of allergic and gastric acid-related conditions. This article focuses on novel aspects of the pharmacology and molecular mechanisms of histamine receptors that should be contemplated for optimizing current therapies, repositioning histaminergic ligands for new therapeutic uses, or even including agonists of the histaminergic system in the treatment of different pathologies such as leukemia or neurodegenerative disorders. In recent years, new signaling phenomena related to H1 and H2 receptors have been described that make them suitable for novel therapeutic approaches. Crosstalk between histamine receptors and other membrane or nuclear receptors can be envisaged as a way to modulate other signaling pathways and to potentiate the efficacy of drugs acting on different receptors. Likewise, biased signaling at histamine receptors seems to be a pharmacological feature that can be exploited to investigate nontraditional therapeutic uses for H1 and H2 biased agonists in malignancies such as acute myeloid leukemia and to avoid undesired side effects when used in standard treatments. It is hoped that the molecular mechanisms discussed in this reviewcontribute to a better understanding of the different aspects involved in histamine receptor pharmacology, which in turn will contribute to increased drug efficacy, avoidance of adverse effects, or repositioning of histaminergic ligands.
Fil: Monczor, Federico. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Investigaciones Farmacológicas. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Instituto de Investigaciones Farmacológicas; Argentina
Fil: Fernandez, Natalia Cristina. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Investigaciones Farmacológicas. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Instituto de Investigaciones Farmacológicas; Argentina - Materia
-
Repourposing
Cross-Talk
Histamine
Biased - Nivel de accesibilidad
- acceso abierto
- Condiciones de uso
- https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
- Repositorio
- Institución
- Consejo Nacional de Investigaciones Científicas y Técnicas
- OAI Identificador
- oai:ri.conicet.gov.ar:11336/40457
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Current knowledge and perspectives on histamine H1 and H2 receptor pharmacology: Functional selectivity, receptor crosstalk, and repositioning of classic histaminergic ligandsMonczor, FedericoFernandez, Natalia CristinaRepourposingCross-TalkHistamineBiasedhttps://purl.org/becyt/ford/3.1https://purl.org/becyt/ford/3H1 and H2 histamine receptor antagonists, although developed many decades ago, are still effective for the treatment of allergic and gastric acid-related conditions. This article focuses on novel aspects of the pharmacology and molecular mechanisms of histamine receptors that should be contemplated for optimizing current therapies, repositioning histaminergic ligands for new therapeutic uses, or even including agonists of the histaminergic system in the treatment of different pathologies such as leukemia or neurodegenerative disorders. In recent years, new signaling phenomena related to H1 and H2 receptors have been described that make them suitable for novel therapeutic approaches. Crosstalk between histamine receptors and other membrane or nuclear receptors can be envisaged as a way to modulate other signaling pathways and to potentiate the efficacy of drugs acting on different receptors. Likewise, biased signaling at histamine receptors seems to be a pharmacological feature that can be exploited to investigate nontraditional therapeutic uses for H1 and H2 biased agonists in malignancies such as acute myeloid leukemia and to avoid undesired side effects when used in standard treatments. It is hoped that the molecular mechanisms discussed in this reviewcontribute to a better understanding of the different aspects involved in histamine receptor pharmacology, which in turn will contribute to increased drug efficacy, avoidance of adverse effects, or repositioning of histaminergic ligands.Fil: Monczor, Federico. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Investigaciones Farmacológicas. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Instituto de Investigaciones Farmacológicas; ArgentinaFil: Fernandez, Natalia Cristina. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Investigaciones Farmacológicas. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Instituto de Investigaciones Farmacológicas; ArgentinaAmerican Society for Pharmacology and Experimental Therapeutics2016-11info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/40457Monczor, Federico; Fernandez, Natalia Cristina; Current knowledge and perspectives on histamine H1 and H2 receptor pharmacology: Functional selectivity, receptor crosstalk, and repositioning of classic histaminergic ligands; American Society for Pharmacology and Experimental Therapeutics; Molecular Pharmacology; 90; 5; 11-2016; 640-6480026-895XCONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/doi/10.1124/mol.116.105981info:eu-repo/semantics/altIdentifier/url/http://molpharm.aspetjournals.org/content/90/5/640info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-09-29T10:01:02Zoai:ri.conicet.gov.ar:11336/40457instacron:CONICETInstitucionalhttp://ri.conicet.gov.ar/Organismo científico-tecnológicoNo correspondehttp://ri.conicet.gov.ar/oai/requestdasensio@conicet.gov.ar; lcarlino@conicet.gov.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:34982025-09-29 10:01:02.806CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse |
dc.title.none.fl_str_mv |
Current knowledge and perspectives on histamine H1 and H2 receptor pharmacology: Functional selectivity, receptor crosstalk, and repositioning of classic histaminergic ligands |
title |
Current knowledge and perspectives on histamine H1 and H2 receptor pharmacology: Functional selectivity, receptor crosstalk, and repositioning of classic histaminergic ligands |
spellingShingle |
Current knowledge and perspectives on histamine H1 and H2 receptor pharmacology: Functional selectivity, receptor crosstalk, and repositioning of classic histaminergic ligands Monczor, Federico Repourposing Cross-Talk Histamine Biased |
title_short |
Current knowledge and perspectives on histamine H1 and H2 receptor pharmacology: Functional selectivity, receptor crosstalk, and repositioning of classic histaminergic ligands |
title_full |
Current knowledge and perspectives on histamine H1 and H2 receptor pharmacology: Functional selectivity, receptor crosstalk, and repositioning of classic histaminergic ligands |
title_fullStr |
Current knowledge and perspectives on histamine H1 and H2 receptor pharmacology: Functional selectivity, receptor crosstalk, and repositioning of classic histaminergic ligands |
title_full_unstemmed |
Current knowledge and perspectives on histamine H1 and H2 receptor pharmacology: Functional selectivity, receptor crosstalk, and repositioning of classic histaminergic ligands |
title_sort |
Current knowledge and perspectives on histamine H1 and H2 receptor pharmacology: Functional selectivity, receptor crosstalk, and repositioning of classic histaminergic ligands |
dc.creator.none.fl_str_mv |
Monczor, Federico Fernandez, Natalia Cristina |
author |
Monczor, Federico |
author_facet |
Monczor, Federico Fernandez, Natalia Cristina |
author_role |
author |
author2 |
Fernandez, Natalia Cristina |
author2_role |
author |
dc.subject.none.fl_str_mv |
Repourposing Cross-Talk Histamine Biased |
topic |
Repourposing Cross-Talk Histamine Biased |
purl_subject.fl_str_mv |
https://purl.org/becyt/ford/3.1 https://purl.org/becyt/ford/3 |
dc.description.none.fl_txt_mv |
H1 and H2 histamine receptor antagonists, although developed many decades ago, are still effective for the treatment of allergic and gastric acid-related conditions. This article focuses on novel aspects of the pharmacology and molecular mechanisms of histamine receptors that should be contemplated for optimizing current therapies, repositioning histaminergic ligands for new therapeutic uses, or even including agonists of the histaminergic system in the treatment of different pathologies such as leukemia or neurodegenerative disorders. In recent years, new signaling phenomena related to H1 and H2 receptors have been described that make them suitable for novel therapeutic approaches. Crosstalk between histamine receptors and other membrane or nuclear receptors can be envisaged as a way to modulate other signaling pathways and to potentiate the efficacy of drugs acting on different receptors. Likewise, biased signaling at histamine receptors seems to be a pharmacological feature that can be exploited to investigate nontraditional therapeutic uses for H1 and H2 biased agonists in malignancies such as acute myeloid leukemia and to avoid undesired side effects when used in standard treatments. It is hoped that the molecular mechanisms discussed in this reviewcontribute to a better understanding of the different aspects involved in histamine receptor pharmacology, which in turn will contribute to increased drug efficacy, avoidance of adverse effects, or repositioning of histaminergic ligands. Fil: Monczor, Federico. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Investigaciones Farmacológicas. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Instituto de Investigaciones Farmacológicas; Argentina Fil: Fernandez, Natalia Cristina. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Investigaciones Farmacológicas. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Instituto de Investigaciones Farmacológicas; Argentina |
description |
H1 and H2 histamine receptor antagonists, although developed many decades ago, are still effective for the treatment of allergic and gastric acid-related conditions. This article focuses on novel aspects of the pharmacology and molecular mechanisms of histamine receptors that should be contemplated for optimizing current therapies, repositioning histaminergic ligands for new therapeutic uses, or even including agonists of the histaminergic system in the treatment of different pathologies such as leukemia or neurodegenerative disorders. In recent years, new signaling phenomena related to H1 and H2 receptors have been described that make them suitable for novel therapeutic approaches. Crosstalk between histamine receptors and other membrane or nuclear receptors can be envisaged as a way to modulate other signaling pathways and to potentiate the efficacy of drugs acting on different receptors. Likewise, biased signaling at histamine receptors seems to be a pharmacological feature that can be exploited to investigate nontraditional therapeutic uses for H1 and H2 biased agonists in malignancies such as acute myeloid leukemia and to avoid undesired side effects when used in standard treatments. It is hoped that the molecular mechanisms discussed in this reviewcontribute to a better understanding of the different aspects involved in histamine receptor pharmacology, which in turn will contribute to increased drug efficacy, avoidance of adverse effects, or repositioning of histaminergic ligands. |
publishDate |
2016 |
dc.date.none.fl_str_mv |
2016-11 |
dc.type.none.fl_str_mv |
info:eu-repo/semantics/article info:eu-repo/semantics/publishedVersion http://purl.org/coar/resource_type/c_6501 info:ar-repo/semantics/articulo |
format |
article |
status_str |
publishedVersion |
dc.identifier.none.fl_str_mv |
http://hdl.handle.net/11336/40457 Monczor, Federico; Fernandez, Natalia Cristina; Current knowledge and perspectives on histamine H1 and H2 receptor pharmacology: Functional selectivity, receptor crosstalk, and repositioning of classic histaminergic ligands; American Society for Pharmacology and Experimental Therapeutics; Molecular Pharmacology; 90; 5; 11-2016; 640-648 0026-895X CONICET Digital CONICET |
url |
http://hdl.handle.net/11336/40457 |
identifier_str_mv |
Monczor, Federico; Fernandez, Natalia Cristina; Current knowledge and perspectives on histamine H1 and H2 receptor pharmacology: Functional selectivity, receptor crosstalk, and repositioning of classic histaminergic ligands; American Society for Pharmacology and Experimental Therapeutics; Molecular Pharmacology; 90; 5; 11-2016; 640-648 0026-895X CONICET Digital CONICET |
dc.language.none.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
info:eu-repo/semantics/altIdentifier/doi/10.1124/mol.116.105981 info:eu-repo/semantics/altIdentifier/url/http://molpharm.aspetjournals.org/content/90/5/640 |
dc.rights.none.fl_str_mv |
info:eu-repo/semantics/openAccess https://creativecommons.org/licenses/by-nc-sa/2.5/ar/ |
eu_rights_str_mv |
openAccess |
rights_invalid_str_mv |
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/ |
dc.format.none.fl_str_mv |
application/pdf application/pdf |
dc.publisher.none.fl_str_mv |
American Society for Pharmacology and Experimental Therapeutics |
publisher.none.fl_str_mv |
American Society for Pharmacology and Experimental Therapeutics |
dc.source.none.fl_str_mv |
reponame:CONICET Digital (CONICET) instname:Consejo Nacional de Investigaciones Científicas y Técnicas |
reponame_str |
CONICET Digital (CONICET) |
collection |
CONICET Digital (CONICET) |
instname_str |
Consejo Nacional de Investigaciones Científicas y Técnicas |
repository.name.fl_str_mv |
CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicas |
repository.mail.fl_str_mv |
dasensio@conicet.gov.ar; lcarlino@conicet.gov.ar |
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13.070432 |