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  • 1
    Electronic Resource
    Electronic Resource
    PET examination of [11C]NNC 687 and [11C]NNC 756 as new radioligands for the D1-dopamine receptor (1993)
    Springer
    Psychopharmacology 113 (1993), S. 149-156 
    Details
    ISSN: 1432-2072
    Keywords: Positron emission tomography ; D1-dopamine receptors ; NNC 687 ; NNC 756 ; Cynomolgus monkey ; Human
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The benzazepines NNC 687 and NNC 756 have in animal studies been described as selective D1-dopamine receptor antagonists. Both compounds have been labeled with11C for examination by positron emission tomography (PET). In the present study central receptor binding was studied in monkeys and healthy men. After IV injection of both radioligands in Cynomolgus monkeys radioactivity accumulated markedly in the striatum, a region with a high density of D1-dopamine receptors. This striatal uptake was displaced by high doses of the selective D1-antagonist SCH 23390 (2 mg/kg) but not by the 5HT2-antagonist ketanserin (1.5 mg/kg) or the selective D2-antagonist raclopride (3 mg/kg). The cortical uptake after injection of [11C]NNC 687 was not reduced in displacement experiments with ketanserin. The cortical uptake of [11C]NNC 756 was reduced in displacement and protection experiments with ketanserin by 24–28% (1.5 mg/kg), whereas no reduction could be demonstrated on striatal uptake. In healthy males both compounds accumulated markedly in the striatum. For [11C]NNC 687 the ratio of radioactivity in the putamen to cerebellum was about 1.5. For [11C]NNC 756 the ratio was about 5. This ratio of 5 for [11C]NNC 756 is the highest obtained so far for PET radioligands for the D1-dopamine receptor.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF02245691
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  • 2
    Electronic Resource
    Electronic Resource
    Preparation of a potential positron emission tomographic radioligand for the dopamine transporter (1994)
    Springer
    European journal of nuclear medicine 21 (1994), S. 131-137 
    Details
    ISSN: 1619-7089
    Keywords: Dopamine transporter ; NNC 12-0722 ; Carbon-11 ; Positron emission tomography ; In vitro autoradiography
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract NNC 12-0722 (1-[2-(bis(4-fluorophenyl)methoxy)ethyl]-4-methyl piperazine) is a new selective inhibitor of the dopamine transporter. [11C]NNC 12-0722 was prepared by N-methylation of the desmethyl compound with [11C]methyl iodide. The total radiochemical yield of [11C]NNC 12-0722 was 40%–50% with an overall synthesis time of 30–35 min. The radiochemical purity was higher than 99% and the specific radioactivity about 1500 Ci/mmol (55 GBq/μmol). Autoradiographic examination of [11C]NNC 12-0722 binding on whole hemisphere cryosections from human brain post mortem demonstrated specific binding in the caudate nucleus and putamen. In a positron emission tomographic examination of [11C]NNC 12-0722 in a cynomolgus monkey there was a rapid uptake of radioactivity in the brain. In the striatum, a region with a high density of dopamine transporters, the radioactivity was two times higher than in the cerebellum. These results indicate that [11C]NNC 12-0722 may be a useful radioligand for labelling of the dopamine transporter in man.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00175760
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    Paper (German National Licenses)
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