Interaction of a muscarinic cholinergic agonist on acetylcholine and dopamine receptors in the monkey brain studied with positron emission tomography |
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Authors: | Hartvig Per Nordberg Agneta Torstenson Richard Sjöberg Pernilla Fasth Karl Johan Långström Bengt |
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Institution: | Uppsala University PET Centre and Hospital Pharmacy, University Hospital, University of Uppsala, Huddinge, Sweden. per.hartvig@pet.uu.se |
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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 (11)C]-N-methyl-4-piperidinylbenzilate ((11)C]NMP), and the effects on nicotine receptor binding were measured with (S)-(11)C-methyl]nicotine. Changes in the binding of the D(2) dopamine receptor antagonist (11)C]raclopride were measured as well. The binding of (11)C]NMP increased in most brain regions with the infusion of increasing doses of milameline from 0.5 to 10 microg/kg/h. (S)-(11)C-methyl]nicotine binding was unchanged or increased somewhat. Binding of (11)C]raclopride to the D(2) dopaminergic receptors in the striatum of the brain increased by 10 +/- 4% following 2 microg/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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