Presynaptic autoreceptors → ↓ histamine release in the CNS
Also dampens release of other transmitters via heteroreceptors
The braking system that H3 antagonist wake-promoters release
Inhibits release of histamine in CNS
Inhibits release of other neurotransmitters via H3 presynaptic heteroreceptors (on cholinergic, noradrenergic, serotonergic, dopaminergic, and GABAergic neurons)
None available for clinical use
Drugs with this mechanism (1)
Histamine — Endogenous amine mediating arousal, allergy, and gastric acid.