Abstract
The effects on the binding to cholinergic and dopaminergic receptors in the brain during continuous intravenous infusion of the muscarinic cholinergic receptor agonist milameline (CI-979) were studied in the rhesus monkey by means of positron emission tomography. Binding to milameline cholinergic receptors was quantified using the muscarinic receptor antagonist [<sup>11</sup>C]-N-methyl-4-piperidinylbenzilate ([<sup>11</sup>C]NMP), and the effects on nicotine receptor binding were measured with (S)-[<sup>11</sup>C-methyl]nicotine. Changes in the binding of the D<sub>2</sub> dopamine receptor antagonist [<sup>11</sup>C]raclopride were measured as well. The binding of [<sup>11</sup>C]NMP increased in most brain regions with the infusion of increasing doses of milameline from 0.5 to 10 µg/kg/h. (S)-[<sup>11</sup>C-methyl]nicotine binding was unchanged or increased somewhat. Binding of [<sup>11</sup>C]raclopride to the D<sub>2</sub> dopaminergic receptors in the striatum of the brain increased by 10 ± 4% following 2 µg/kg/h of milameline. The results suggest a possible action of milameline both on presynaptic muscarinic receptor subtypes as well as dopamine levels dependent on the receptor reserve of the muscarinic receptor subtypes.
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