Synthesis and in Vivo studies of [C-11]N-methylepibatidine: comparison of the stereoisomers.
The carbon-11-labelled nicotinic acetylcholine receptor (nAChR) agonist N-methylepibatidine was evaluated in vitro and in vivo as a possible positron emission tomography (PET)-tracer for nicotinic receptors in the central nervous system (CNS). The racemic mixture and both enantiomers of N-methylepibatidine were compared. Biodistribution and metabolites for blood and brain of [C-11]N-methylepibatidine were determined in mice. Whole body rat PET data were acquired for both stereoisomers. The regional distribution of the N-methyl-(-)-epibatidine in the brain was determined by a PET scan in a pig. Characteristic differences were found for the in vivo behavior of the stereoisomers of [C-11]N-methylepibatidine.
Patt
J T
JT
Department of Radiology, University Hospital of Zürich, Switzerland.
Spang
J E
JE
Westera
G
G
Buck
A
A
Schubiger
P A
PA
D000818:Animals; D001921:Brain / Q000378:metabolism*; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000097:blood / Q000378:metabolism* / Q000633:toxicity; D002250:Carbon Radioisotopes; D002851:Chromatography, High Pressure Liquid; D005260:Female; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D018722:Nicotinic Agonists / Q000097:blood / Q000378:metabolism* / Q000633:toxicity; D011725:Pyridines / Q000097:blood / Q000378:metabolism* / Q000633:toxicity; D051381:Rats; D013237:Stereoisomerism; D014018:Tissue Distribution; D014055:Tomography, Emission-Computed; D018675:Toxicity Tests
D019086:Bridged Bicyclo Compounds, Heterocyclic; D002250:Carbon Radioisotopes; C119662:N-methylepibatidine; D018722:Nicotinic Agonists; D011725:Pyridines; C082748:epibatidine