Abstract

AQUINO-MIRANDA, Guillermo  and  ARIAS-MONTANO, José-Antonio. Neuromodulation and histamine: regulation by H₃ receptors of neurotransmitter release. Salud Ment [online]. 2012, vol.35, n.4, pp.345-352. ISSN 0185-3325.

Histamine regulates at the pre- and post-synaptic levels several functions of the mammalian Nervous System, in which three (H₁, H₂, and H₃) out of the four G protein-coupled histamine receptors cloned so far are widely distributed. The histamine H₃ receptor (H₃R) was first identified as an auto-receptor controlling histamine synthesis and release, but several lines of evidence have shown the H₃R to regulate as a hetero-receptor the release of a number of neuroactive substances, namely acetylcholine, 5-hydroxytryptamine (5-HT, serotonin), noradrenaline, dopamine, glutamate, y-aminobutyric acid (GABA) and the neuropeptides sustance P and calcitonin gene-related peptide (CGRP). H₃R-mediated regulation of the release of these neurotransmitters and neuro-modulators, both in normal and pathological conditions, suggest that drugs acting at the receptor may have therapeutic use in a number of diseases such as sleep disorders, ischemia-induced cardiac arrhythmias, migraine, obesity, Alzheimer's disease and schizophrenia.

Keywords : Histamine; H₃ receptor; neuromodulation; hetero-receptors; synaptic transmission; signaling.

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