H3 agonist
H3 histamine receptor agonist
- Presynaptic autoreceptors → ↓ histamine release in the CNS
- Also dampens release of other transmitters via heteroreceptors
- Inhibits release of other neurotransmitters via H3 presynaptic heteroreceptors (on cholinergic, noradrenergic, serotonergic, dopaminergic, and GABAergic neurons)
- The braking system that H3 antagonist wake-promoters release
- None available for clinical use
Drugs with this mechanism (1)
- Histamine — Endogenous amine mediating arousal, allergy, and gastric acid.
Self-check
- How do presynaptic H3 autoreceptors affect CNS histamine release?
They reduce it. - Is H3-mediated release suppression limited to histamine?
No; heteroreceptors also dampen other transmitters.
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