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Histaminergic system in brain disorders: lessons from the translational approach and future perspectives
Diego Baronio1, Taylor Gonchoroski2, Kamila Castro1
1Translational Research Group in Autism Spectrum Disorders (GETTEA), Ramiro Barcelos, 2350 - Santa Cecília, Porto Alegre, RS 90035-903 Brazil ; Postgraduate Program in Child and Adolescent Health, Federal University of Rio Grande do Sul, Porto Alegre, RS Brazil ; Research Group in Neuroglial Plasticity, Department of Biochemistry, Federal University of Rio Grande do Sul, Porto Alegre, RS Brazil.
Abstract:
Histamine and its receptors were first described as part of immune and gastrointestinal systems, but their presence in the central nervous system and importance in behavior are gaining more attention. The histaminergic system modulates different processes including wakefulness, feeding, and learning and memory consolidation. Histamine receptors (H1R, H2R, H3R, and H4R) belong to the rhodopsin-like family of G protein-coupled receptors, present constitutive activity, and are subjected to inverse agonist action. The involvement of the histaminergic system in brain disorders, such as Alzheimer's disease, schizophrenia, sleep disorders, drug dependence, and Parkinson's disease, is largely studied. Data obtained from preclinical studies point antagonists of histamine receptors as promising alternatives to treat brain disorders. Thus, clinical trials are currently ongoing to assess the effects of these drugs on humans. This review summarizes the role of histaminergic system in brain disorders, as well as the effects of different histamine antagonists on animal models and humans.
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