Neuromodulation and histamine: regulation by H-3 receptors of neurotransmitter release

作者：Aquino Miranda Guillermo; Arias Montano Jose Antonio^*

来源：Salud Mental, 2012, 35(4): 345-352.

• Histamine
• H-3 receptor
• neuromodulation
• hetero-receptors
• synaptic transmission
• signaling

Histamine regulates at the pre- and post-synaptic levels several functions of the mammalian Nervous System, in which three (H-1, H-2, and H-3) out of the four G protein-coupled histamine receptors cloned so for are widely distributed. The histamine H-3 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, gamma-aminobutyric acid (GABA) and the neuropeptides sustance P and calcitonin gene-related peptide (CGRP). H3R-mediated regulation of the release of these neurotransmitters and neuromodulators, 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.

• 出版日期2012-8