Rat Histamine H3 Receptor (HRH3) Protein

Background

HRH3 is a G protein-coupled receptor primarily expressed in the central nervous system (CNS), particularly in histaminergic neurons, where it functions as an autoreceptor and heteroreceptor. HRH3 regulates the synthesis and release of histamine and modulates the release of other neurotransmitters such as dopamine, acetylcholine, and serotonin. It couples to Gi/o proteins, inhibiting adenylyl cyclase activity and reducing cyclic AMP (cAMP) levels, thereby regulating neuronal excitability and neurotransmission. HRH3 plays a critical role in cognitive processes, including attention, memory, and wakefulness, and is implicated in neurological and psychiatric disorders such as schizophrenia, ADHD, and neurodegenerative diseases like Alzheimer’s. Dysregulation of HRH3 signaling contributes to sleep disorders, cognitive dysfunction, and inflammatory neuropathies. HRH3 antagonists are being explored for therapeutic applications to improve cognition, treat sleep disorders, and manage neuropsychiatric conditions. Its role in presynaptic neurotransmitter modulation positions HRH3 as a promising target for CNS-related therapies.