[(11)C]SL25.1188, a new reversible radioligand to study the monoamine oxidase type B with PET: preclinical characterisation in nonhuman primate.
作者： Wadad Saba , Héric Valette , Marie-Anne Peyronneau , Yann Bramoullé , Christine Coulon
DOI: 10.1002/SYN.20703
关键词: Hippocampus 、 Cortex (anatomy) 、 Monoamine oxidase B 、 Temporal cortex 、 Internal medicine 、 Lazabemide 、 Endocrinology 、 Anesthesia 、 Striatum 、 Radioligand 、 Chemistry 、 In vivo
摘要: [(11)C]SL-25.1188 [(S)-5-methoxymethyl-3-[6-(4,4,4-trifluorobutoxy)-benzo[d]isoxazol-3-yl]-oxazolidin-2-one], an oxazolidinone derivative, was characterized in baboons as a radioligand for the vivo visualization of MAO-B using positron emission tomography (PET). After i.v. injection, [(11)C]SL25.1188 presented rapid phase distribution blood (about 5 min), followed by T(1/2) elimination 85 +/- 14 min. Plasma metabolism analysis showed that is stable at least 30 Brain uptake with highest one observed striatum and thalamus, lowest pons. Calculated volumes (V(T)) were follows: = 10.3, thalamus 10.9, hippocampus 8.9, temporal cortex 7.7, occipital 7.2, parietal 7.4, frontal white matter pons 6.1. Pretreatment deprenyl (2 mg/kg, i.v.) or lazabemide (0.5 reduced V(T) values all brain areas up to 50%. In displacement experiments, injection SL25.1188 (1 2 i.v., respectively) strongly specific (85-100%), while lesser (55-70% binding depending on area). Therefore, reversible binding, high very slow plasma metabolism, suggesting this potent tool study MAO-B.
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