Evaluation of [C-11]RTI-121 as a selective radioligand for PET studies of the dopamine transporter

被引:16
|
作者
Hume, SP
Luthra, SK
Brown, DJ
OpackaJuffry, J
Osman, S
Ashworth, S
Myers, R
Brady, F
Carroll, FI
Kuhar, MJ
Brooks, DJ
机构
[1] HAMMERSMITH HOSP,ROYAL POSTGRAD MED SCH,MRC CLIN SCI CTR,CYCLOTRON UNIT,NEUROSCI GRP,LONDON W12 0NN,ENGLAND
[2] RES TRIANGLE INST,DEPT ORGAN & MED CHEM,RES TRIANGLE PK,NC 27709
[3] NIDA,NEUROSCI BRANCH,ADDICT RES CTR,BALTIMORE,MD 21224
来源
NUCLEAR MEDICINE AND BIOLOGY | 1996年 / 23卷 / 03期
关键词
dopamine transporter; RTI-121; positron emission tomography;
D O I
10.1016/0969-8051(96)00019-4
中图分类号
R8 [特种医学]; R445 [影像诊断学];
学科分类号
1002 ; 100207 ; 1009 ;
摘要
The cocaine analogue RTI-121 (3 beta-(4-iodophenyl)tropane-2 beta-carboxylic acid isopropyl ester), when labeled with carbon-11, was evaluated in rats as a potential PET ligand for the dopamine transporter. The compound gave in vivo striatum:cerebellum ratios that were similar to those obtained with the related ligand [C-11]RTI-55 (2 beta-(4-iodophenyl)tropane-2 beta-carboxylic acid methyl ester) but showed a much greater selectivity for the dopamine compared with the 5-HT uptake site, The results indicate that [C-11]RTI-121 could be used in preference to [C-11]RTI-55 in man. Experimentally, [C-11]RTI-121 has potential in the quantification of dopamine terminal function in rat models of disease, using a combination of autoradiography, postmortem sampling, and in vivo tomography.
引用
收藏
页码:377 / 384
页数:8
相关论文
共 50 条
  • [41] PET STUDIES WITH (CO2)-C-11 AND C-11 GLUCOSE IN THE FIELD OF PEDIATRIC NEUROLOGY
    SAKURAGAWA, N
    MATSUI, A
    ARIMA, M
    IIO, M
    BRAIN & DEVELOPMENT, 1983, 5 (02): : 161 - 161
  • [42] Synthesis and in vivo evaluation of a C-11 labeled novel dopamine D1 receptor agonist radioligand in baboon
    Easwaramoorthy, Balu
    Neelamegam, Ramesh
    Palatnik, Matthew
    Myung, John
    Abi-Dargham, Anissa
    Slifstein, Mark
    JOURNAL OF NUCLEAR MEDICINE, 2011, 52
  • [43] A radiometabolite study of the serotonin transporter PET radioligand [11C]MADAM
    Gourand, F.
    Emond, P.
    Bergstroem, J. P.
    Takano, A.
    Gulyas, B.
    Guilloteau, D.
    Barre, L.
    Halldin, C.
    NUCLEAR MEDICINE AND BIOLOGY, 2014, 41 (06) : 501 - 506
  • [44] SYNTHESIS AND EVALUATION OF A C-11 LABELED DOPAMINE D2 SELECTIVE IMAGING AGENT
    Vangveravong, S.
    Tu, Z.
    Xu, J.
    Jones, L. A.
    Li, S.
    Taylor, M.
    Luedtke, R. R.
    Mach, R. H.
    JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2009, 52 : S77 - S77
  • [45] PET-characterization of [C-11]PE2I binding to dopamine transporter in the monkey brain.
    Halldin, C
    Guilloteau, D
    Okubo, Y
    Lundkvist, C
    Olsson, H
    Karlsson, P
    Chalon, S
    Emond, P
    Swahn, CG
    Farde, L
    JOURNAL OF NUCLEAR MEDICINE, 1998, 39 (05) : 118P - 118P
  • [46] Comparison of [C-11]cocaine and [C-11]d-threo-methylphenidate for assessing dopamine transporter (DAT) occupancy by cocaine.
    Fowler, JS
    Volkow, ND
    Logan, J
    Gatley, SJ
    Pappas, N
    King, P
    Ding, YS
    Wang, GJ
    JOURNAL OF NUCLEAR MEDICINE, 1997, 38 (05) : 34 - 34
  • [47] Difficulties in dopamine transporter radioligand PET analysis: the example of LBT-999 using [18F] and [11C] labelling Part I: PET studies
    Saba, Wadad
    Peyronneau, Marie-Anne
    Dolle, Frederic
    Goutal, Sebastien
    Bottlaender, Michel
    Valette, Heric
    NUCLEAR MEDICINE AND BIOLOGY, 2012, 39 (02) : 227 - 233
  • [48] Serotonin Transporter Binding in Panic Disorder: A [C-11]DASB PET Study
    Cannon, Dara M.
    Klaver, Jackie M.
    Peck, Summer A.
    Carlson, Paul J.
    Luckenbaugh, Dave
    Ichise, Masanori
    Drevets, Wayne C.
    BIOLOGICAL PSYCHIATRY, 2009, 65 (08) : 85S - 85S
  • [49] Synthesis and C-11 labeling of three potent norepinephrine transporter selective ligands ((R)-nisoxetine, lortalamine, and oxaprotiline) for comparative PET studies in baboons
    Lin, KS
    Ding, YS
    BIOORGANIC & MEDICINAL CHEMISTRY, 2005, 13 (15) : 4658 - 4666
  • [50] SELECTIVE D1-DOPAMINE AND D2-DOPAMINE RECEPTOR BLOCKADE BOTH INDUCES AKATHISIA IN HUMANS - A PET STUDY WITH [C-11] SCH-23390 AND [C-11] RACLOPRIDE
    FARDE, L
    PSYCHOPHARMACOLOGY, 1992, 107 (01) : 23 - 29