H3 antagonist
H3 histamine receptor antagonist
- ↑ histamine and other transmitter release (presynaptic auto/heteroreceptors)
- Promotes wakefulness without stimulant abuse liability
- Also enhances cortical acetylcholine and dopamine release
- Increased release of histamine, acetylcholine, norepinephrine
- ➔ approved in other countries for vestibular vertigo
- ➔ available in U.S. from compounding pharmacies, used for tinnitus and mitigation of antipsychotic-induced weight gain
- Improved attention and working memory
- Potential antiepileptic effect
- May enhance metabolism through activation of brown adipose tissue
Drugs with this mechanism (2)
- Betahistine — Histamine analog for Meniere vertigo (not US-approved).
- Pitolisant — H3 inverse agonist wake-promoter; non-scheduled.
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