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5-iodo A-85380 is an agonist of α4β2 and α6β2 subunit-containing nicotinic acetylcholine receptors (nAChRs).1 It activates α-conotoxin MII-sensitive and -insensitive dopamine release in rat striatal synaptosomes, markers of α4β2 and α6β2 subunit-containing nAChR activation, respectively (EC50s = 12.7 and ~35 nM, respectively). In vivo, 5-iodo A-85380 (0.37 µmol/kg per day) decreases the total number of abnormal involuntary movements (AIMs) in a rat model of L-DOPA-induced Parkinson’s disease.2
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1. Functional responses and subunit composition of presynaptic nicotinic receptor subtypes explored using the novel agonist 5-
2. Nicotinic receptor agonists decrease L-