Synthesis of 1-benzyl-4-[(5,[11C]6-dimethoxy-1-oxoindan-2-yl)methyl]piperidine:: a promising ligand for visualisation of acetylcholine esterase by PET

被引:0
作者
De Vos, F
Santens, P
Slegers, G
Vermeirsch, H
Dierckx, RA
De Reuck, J
机构
[1] State Univ Ghent, Dept Radiopharm, B-9000 Ghent, Belgium
[2] State Univ Ghent Hosp, Dept Neurol, B-9000 Ghent, Belgium
[3] State Univ Ghent, Dept Morphol, B-9820 Merelbeke, Belgium
[4] State Univ Ghent Hosp, Dept Nucl Med, B-9000 Ghent, Belgium
关键词
C-11; synthesis; acetylcholine esterase; PET; donepezil;
D O I
10.1002/(SICI)1099-1344(200005)43:6<595::AID-JLCR344>3.0.CO;2-B
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
Donepezil (1-benzyl-4-[(5,6-dimethoxy-1-oxoindan-2-yl)methyl-]piperidine), a potent acetylcholine esterase inhibitor, was labelled with [C-11]iodomethane by O-methylation of the O-6'-desmethyl precursor. Synthesis, purification and formulation were performed in approximately 30 min with an average specific activity of 39.5 GBq/mu mol at EOS. The total activity available for applications was 7.5-11.1 GBq.
引用
收藏
页码:595 / 601
页数:7
相关论文
共 22 条
  • [1] BECKER RE, 1991, CHOLINERGIC BASIS AL, V3, P314
  • [2] CROUZEL C, 1987, APPL RADIAT ISOTOPES, V38, P601
  • [3] DAVIES P, 1976, LANCET, V2, P1403
  • [4] DAVIS KL, 1979, NEW ENGL J MED, V301, P946
  • [5] *EUR PHARM COMM, 1994, PROP GUID RES SOLV L
  • [6] PHARMACOKINETICS AND PHARMACODYNAMICS OF PHYSOSTIGMINE AFTER INTRAVENOUS ADMINISTRATION IN BEAGLE DOGS
    GIACOBINI, E
    SOMANI, S
    MCILHANY, M
    DOWNEN, M
    HALLAK, M
    [J]. NEUROPHARMACOLOGY, 1987, 26 (7B) : 831 - 836
  • [7] Irie T, 1996, J NUCL MED, V37, P649
  • [8] Measurement of acetylcholinesterase by positron emission tomography in the brains of healthy controls and patients with Alzheimer's disease
    Iyo, M
    Namba, H
    Fukushi, K
    Shinotoh, H
    Nagatsuka, S
    Suhara, T
    Sudo, Y
    Suzuki, K
    Irie, T
    [J]. LANCET, 1997, 349 (9068) : 1805 - 1809
  • [9] Kilbourn MR, 1996, SYNAPSE, V22, P123, DOI 10.1002/(SICI)1098-2396(199602)22:2<123::AID-SYN5>3.0.CO
  • [10] 2-F