HRH3
Description
The HRH3 (histamine receptor H3) is a protein-coding gene located on chromosome 20.
The HRH3 gene encodes the histamine H3 receptor, which plays a significant role in the central and peripheral nervous systems. It acts as an autoreceptor on presynaptic histaminergic neurons, regulating histamine turnover through feedback inhibition of synthesis and release. It also acts as an inhibitory heteroreceptor, modulating the release of other neurotransmitters, including dopamine, GABA, acetylcholine, noradrenaline, serotonin, and histamine. The HRH3 gene shares limited homology with H1 and H2 receptor genes, making it a unique and promising target for therapeutic development.
The HRH3 receptor is a G-protein coupled receptor, specifically coupled to the Gi G-protein. This coupling leads to inhibition of cAMP formation and interaction with N-type voltage-gated calcium channels, resulting in reduced calcium influx and neurotransmitter release. Its widespread distribution throughout the cortex and subcortex highlights its ability to modulate a diverse range of neurotransmitters. The receptor is thought to contribute to satiety regulation.
The HRH3 receptor is found in various tissues, including:
- Central nervous system
- Peripheral nervous system
- Heart
- Lungs
- Gastrointestinal tract
- Endothelial cells
The H3 receptor's involvement in neuronal mechanisms related to cognitive disorders and its central nervous system localization makes it a promising target for therapeutic interventions.
HRH3 is also known as GPCR97, HH3R.
Associated Diseases
- narcolepsy-cataplexy syndrome
- narcolepsy
- Parkinson disease
- idiopathic hypersomnia
- esophageal cancer
- schizophrenia
- Alzheimer disease
- C1 inhibitor deficiency
- alcohol dependence
