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Histamine H3 Receptor (None)
- Target
- None
- Molecular classification
- G-protein-coupled receptor, GPCR, Class A GPCR
01
Overview
The histamine H3 receptor is a Gi/o-coupled GPCR primarily located presynaptically in the CNS, functioning as an autoreceptor on histaminergic neurons and as a heteroreceptor modulating the release of other neurotransmitters. It plays a key role in regulating histamine synthesis and release, as well as influencing cognitive processes, sleep-wake cycles, and food intake. Its constitutive activity makes it a target for inverse agonists in conditions like narcolepsy.
02
Mechanism of action
H3 receptor antagonists/inverse agonists enhance wakefulness/cognition by disinhibiting neuronal signaling suppressed by constitutive/agonist-driven H3R activity.
03
Biological functions
AutoreceptionHeteroreceptionNeurotransmitter release modulationInhibition of adenylate cyclase activityRegulation of impulse flowModulation of cognitive processesSleep-wake regulationSatiety/food intake control
04
Disease associations
NarcolepsyExcessive daytime sleepinessCognitive disordersDementiasEpileptic seizuresAttention-deficit/hyperactivity disorder (ADHD)Schizophrenia
05
Interacting drugs
Histamine
1 more in the full profile.
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