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Research ArticleMinireview—A Latin American Perspective On G Protein-Coupled Receptors

The Histamine H3 Receptor: Structure, Pharmacology, and Function

Gustavo Nieto-Alamilla, Ricardo Márquez-Gómez, Ana-Maricela García-Gálvez, Guadalupe-Elide Morales-Figueroa and José-Antonio Arias-Montaño
Molecular Pharmacology November 2016, 90 (5) 649-673; DOI: https://doi.org/10.1124/mol.116.104752
Gustavo Nieto-Alamilla
Departamento de Fisiología, Biofísica y Neurociencias, Centro de Investigación y de Estudios Avanzados (Cinvestav-IPN), Zacatenco, Ciudad de México, México
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Ricardo Márquez-Gómez
Departamento de Fisiología, Biofísica y Neurociencias, Centro de Investigación y de Estudios Avanzados (Cinvestav-IPN), Zacatenco, Ciudad de México, México
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Ana-Maricela García-Gálvez
Departamento de Fisiología, Biofísica y Neurociencias, Centro de Investigación y de Estudios Avanzados (Cinvestav-IPN), Zacatenco, Ciudad de México, México
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Guadalupe-Elide Morales-Figueroa
Departamento de Fisiología, Biofísica y Neurociencias, Centro de Investigación y de Estudios Avanzados (Cinvestav-IPN), Zacatenco, Ciudad de México, México
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José-Antonio Arias-Montaño
Departamento de Fisiología, Biofísica y Neurociencias, Centro de Investigación y de Estudios Avanzados (Cinvestav-IPN), Zacatenco, Ciudad de México, México
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Abstract

Among the four G protein–coupled receptors (H1–H4) identified as mediators of the biologic effects of histamine, the H3 receptor (H3R) is distinguished for its almost exclusive expression in the nervous system and the large variety of isoforms generated by alternative splicing of the corresponding mRNA. Additionally, it exhibits dual functionality as autoreceptor and heteroreceptor, and this enables H3Rs to modulate the histaminergic and other neurotransmitter systems. The cloning of the H3R cDNA in 1999 by Lovenberg et al. allowed for detailed studies of its molecular aspects. In this work, we review the characteristics of the H3R, namely, its structure, constitutive activity, isoforms, signal transduction pathways, regional differences in expression and localization, selective agonists, antagonists and inverse agonists, dimerization with other neurotransmitter receptors, and the main presynaptic and postsynaptic effects resulting from its activation. The H3R has attracted interest as a potential drug target for the treatment of several important neurologic and psychiatric disorders, such as Alzheimer and Parkinson diseases, Gilles de la Tourette syndrome, and addiction.

Footnotes

    • Received April 15, 2016.
    • Accepted August 24, 2016.
  • Research in J.-A. A.-M.’s laboratory is supported by Cinvestav and the Mexican Council for Science and Technology (Conacyt).

  • dx.doi.org/10.1124/mol.116.104752.

  • Copyright © 2016 by The American Society for Pharmacology and Experimental Therapeutics
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Molecular Pharmacology: 90 (5)
Molecular Pharmacology
Vol. 90, Issue 5
1 Nov 2016
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Research ArticleMinireview—A Latin American Perspective On G Protein-Coupled Receptors

Histamine H3 Receptor

Gustavo Nieto-Alamilla, Ricardo Márquez-Gómez, Ana-Maricela García-Gálvez, Guadalupe-Elide Morales-Figueroa and José-Antonio Arias-Montaño
Molecular Pharmacology November 1, 2016, 90 (5) 649-673; DOI: https://doi.org/10.1124/mol.116.104752

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Research ArticleMinireview—A Latin American Perspective On G Protein-Coupled Receptors

Histamine H3 Receptor

Gustavo Nieto-Alamilla, Ricardo Márquez-Gómez, Ana-Maricela García-Gálvez, Guadalupe-Elide Morales-Figueroa and José-Antonio Arias-Montaño
Molecular Pharmacology November 1, 2016, 90 (5) 649-673; DOI: https://doi.org/10.1124/mol.116.104752
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    • Introduction
    • The Brain Histaminergic System
    • The Histamine H3 Receptor
    • Pharmacology
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  • Gβγ Pathways in Oncogenic GPCR Signaling
  • CRF Receptor’s Interacting Proteins
  • Histamine Receptor Pharmacology
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