Radiosynthesis of 3-{[4-(4-[18F]fluorobenzyl)]piperazin-1-yl}methyl-1H-pyrrolo[2,3-b]pyridine: A potential dopamine D4 receptor imaging agent

Verfasser / Beitragende:
[Tian Hai-Bin, Yin Duan-Zhi, Li Jun-Ling, Zhang Lan, Zhang Cun-Fu, Wang Yong-Xian, Zhou Wei]
Ort, Verlag, Jahr:
2003
Enthalten in:
Radiochimica Acta/International journal for chemical aspects of nuclear science and technology, 91/4/2003(2003-04-01), 241-245
Format:
Artikel (online)
ID: 378867571
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024 7 0 |a 10.1524/ract.91.4.241.19967  |2 doi 
035 |a (NATIONALLICENCE)gruyter-10.1524/ract.91.4.241.19967 
245 0 0 |a Radiosynthesis of 3-{[4-(4-[18F]fluorobenzyl)]piperazin-1-yl}methyl-1H-pyrrolo[2,3-b]pyridine: A potential dopamine D4 receptor imaging agent  |h [Elektronische Daten]  |c [Tian Hai-Bin, Yin Duan-Zhi, Li Jun-Ling, Zhang Lan, Zhang Cun-Fu, Wang Yong-Xian, Zhou Wei] 
520 3 |a The dopamine D4 receptor (D4R) is expressed in low density in various extrastriatal brain regions. This receptor subtype is discussed in relation to the pathophysiology and treatment of schizophrenia but to date no selective positron emission tomography (PET) ligand is available to study its distribution in vivo . The 7-azaindole derivative 3-{[4-(4-iodophenyl)piperazin-1-yl]-methyl}-1H-pyrrolo[2,3-b]pyridine (L-750,667) is a novel, high-affinity (Ki=0.51nM) and selective D4R ligand. L-750,667 analogue 3-{[4-(4-[18F]fluorobenzyl)]piperazin-1-yl}methyl-1H-pyrrolo[2,3-b]-pyridine was prepared by reacting 3-(piperazin-1-yl)-methyl-1H-pyrrolo[2,3-b]pyridine with 4-[18F]fluorobenzaldehyde, which was labeled with no carrier added [18F]fluoride. The radiochemical yield of 3-{[4-(4-[18F]fluorobenzyl)]piperazin-1-yl}methyl-1H-pyrrolo[2,3-b]pyridine was 12.0 at end of synthesis (EOS), and the synthesis time was 73min. The labeled benzaldehydes may be useful precursors for the radiosyntheses of other complex radiotracers for PET. 
540 |a © 2003 Oldenbourg Wissenschaftsverlag GmbH 
690 7 |a Laboratory techniques, experiments  |2 nationallicence 
690 7 |a Analytical chemistry  |2 nationallicence 
690 7 |a Inorganic chemistry  |2 nationallicence 
700 1 |a Hai-Bin  |D Tian  |4 aut 
700 1 |a Duan-Zhi  |D Yin  |4 aut 
700 1 |a Jun-Ling  |D Li  |4 aut 
700 1 |a Lan  |D Zhang  |4 aut 
700 1 |a Cun-Fu  |D Zhang  |4 aut 
700 1 |a Yong-Xian  |D Wang  |4 aut 
700 1 |a Wei  |D Zhou  |4 aut 
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