title: The Histamine H3 Receptor: Structure, Pharmacology, and Function.
abstract: Among the four G protein-coupled receptors (H1-H4) identified as mediators of the biologic effects of histamine, the H3receptor (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.
authors: Departamento de Fisiología, Biofísica y Neurociencias, Centro de Investigación y de Estudios Avanzados (Cinvestav-IPN), Zacatenco, Ciudad de México, México.
authors: Gustavo
authors: G
authors: Nieto-Alamilla
authors: Departamento de Fisiología, Biofísica y Neurociencias, Centro de Investigación y de Estudios Avanzados (Cinvestav-IPN), Zacatenco, Ciudad de México, México.
authors: Ricardo
authors: R
authors: Márquez-Gómez
authors: Departamento de Fisiología, Biofísica y Neurociencias, Centro de Investigación y de Estudios Avanzados (Cinvestav-IPN), Zacatenco, Ciudad de México, México.
authors: Ana-Maricela
authors: AM
authors: García-Gálvez
authors: Departamento de Fisiología, Biofísica y Neurociencias, Centro de Investigación y de Estudios Avanzados (Cinvestav-IPN), Zacatenco, Ciudad de México, México.
authors: Guadalupe-Elide
authors: GE
authors: Morales-Figueroa
authors: Departamento de Fisiología, Biofísica y Neurociencias, Centro de Investigación y de Estudios Avanzados (Cinvestav-IPN), Zacatenco, Ciudad de México, México jaarias@fisio.cinvestav.mx.
authors: José-Antonio
authors: JA
authors: Arias-Montaño
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D001921:Brain / Q000378:metabolism; D006632:Histamine / Q000378:metabolism; D006801:Humans; D008954:Models, Biological; D011618:Psychotic Disorders / Q000378:metabolism; D018100:Receptors, Histamine H3 / Q000737:chemistry* / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D018100:Receptors, Histamine H3; D006632:Histamine