Neuronal nAChR allosteric potentiator (APL)
Neuronal nicotinic receptor allosteric potentiating ligand
- Allosteric potentiating ligand: sensitizes nAChRs to acetylcholine without activating them
- No nicotine-like reinforcement
- A minor contributor next to acetylcholinesterase inhibition
Drugs with this mechanism (1)
- Galantamine — Cholinesterase inhibitor; also modulates nicotinic receptors.
Self-check
- Which type of experiment distinguishes a pure positive allosteric modulator from an agonist at the same receptor?
Measure receptor response with the compound alone and with an orthosteric agonist. - How does varenicline reduce nicotine reinforcement while providing some nicotinic stimulation?
It partially activates alpha4beta2 receptors while competitively preventing nicotine binding.
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