Neuronal nAChR agonist
Neuronal nicotinic acetylcholine receptor agonist
- ↑ dopamine, norepinephrine, serotonin, glutamate and GABA release
- If BBB-crossing:
- Reward-circuit activation → reinforcement
- Can enhance attention/cognition and alter sleep
Neuronal nAChR agonist (1/2)
- ↑ Neurotransmitter release (DA, NE, 5-HT, glutamate, GABA)
- Cognitive enhancement
- Activates reward pathways (DA release)
- Neuroprotection (activation of α7 subtype)
- ➔ preclinical evidence
- Alters sleep architecture
- ➔ highest relevance at α4β2 subtype
Neuronal nAChR agonist (2/2)
- ➔ intranasal varenicline (Tyrvaya) stimulates trigeminal–parasympathetic reflex → ↑ tear production
Drugs with this mechanism (7)
- Acetylcholine — Endogenous neurotransmitter at muscarinic and nicotinic receptors.
- Carbachol — Nonselective cholinergic agonist used in ophthalmology.
- Nicotine gum — The addictive alkaloid of tobacco; nicotinic agonist, available OTC for cessation.
- Nicotine inhaler — Nicotine-replacement device absorbed mainly through the mouth and throat; addresses cravings and the hand-to-mouth smoking ritual.
- Nicotine lozenge — Short-acting nicotine replacement for breakthrough cravings; oral irritation is common.
- Nicotine nasal spray — Fast-acting nicotine-replacement spray for breakthrough cravings during smoking cessation.
- Nicotine patch — Steady transdermal nicotine for smoking cessation; pair with a short-acting form for breakthrough craving.
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