The @entity505 -11 labeled enantiomers of nicotinic @entity934 receptor (nAChR) ligand @entity69943 have been synthesized to study the neuronal nicotinic @entity934 receptors (nAChRs). In vivo evaluations were performed in @entity19 and @entity1707 using positron emission tomography (PET). The radioligands displayed a strong enantioselectivity. The (-)-enantiomer showed high uptake in the brain while the (+)-enantiomer was rapidly washed out. In metabolite studies in @entity19 >65% unchanged ligand was found in the blood after 60 minutes. No metabolites were found in the brain. After intravenous application of @entity69943 in the @entity1707 specific accumulation in the thalamus was seen. Blocking experiments with @entity10446 showed specific binding consistent with labeling of the alpha4beta2-nAChR-subtype in the brain. Quantitative kinetic modeling of radiotracers in the @entity1707 brain was performed using the arterial input function. The brain uptake of the (-)-isomer was best fitted by a three-compartment model. High distribution volumes were found in the thalamus (DV(TOT) = 66.617, DV(S) = 59.910) versus a low uptake in the cerebellum (DV(TOT) = 8.605m, DV(S) = 1.898). The binding characteristics suggest @entity69943 to be suited for PET imaging studies, but high @entity137 prevents routine use in @entity1 .

Synthesis and in vivo studies of the stereoisomers of XXXX .

@entity1 :: ('9606', 'Species') :: ['humans'] @entity1707 :: ('9823', 'Species') :: ['pig'] @entity69943 :: ('MESH:C440009', 'Chemical') :: ['N-[11C]methyl-homoepibatidine', 'N-[11C]methyl-(-)-homoepibatidine'] @entity137 :: ('MESH:D064420', 'Disease') :: ['toxicity'] @entity19 :: ('10090', 'Species') :: ['mice'] @entity10446 :: ('MESH:C004712', 'Chemical') :: ['cytisine'] @entity505 :: ('MESH:D002244', 'Chemical') :: ['carbon'] @entity934 :: ('MESH:D000109', 'Chemical') :: ['acetylcholine']
@entity69943 :: (MESH:C440009,Chemical) :: ['N-[11C]methyl-homoepibatidine']
