Human biodistribution and dosimetry of iodine-123-fluouoalkyl analogs of beta-CIT

被引:9
作者
Abi-Dargham, A
Innis, RB
Wisniewski, G
Baldwin, RM
Neumeyer, JL
Seibyl, JP
机构
[1] YALE UNIV, SCH MED, DEPT PSYCHIAT, W HAVEN, CT 06516 USA
[2] VET ADM MED CTR, W HAVEN, CT 06516 USA
[3] YALE UNIV, SCH MED, DEPT DIAGNOST RADIOL, W HAVEN, CT 06516 USA
[4] RES BIOCHEM INT, NATICK, MA USA
关键词
biodistribution; I-123]FE-CIT; I-123]FP-CIT;
D O I
10.1007/s002590050170
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
Two new N-omega-fluoroalkyl analogs of [I-123]2 beta-carbomethoxy-3 beta-(4-iodophenyl)tropane ([I-123]FE-CIT), the fluoroethyl and fluoropropyl compounds ([I-123]FE-CIT and [(123)]FP-CIT, respectively): have been shown to have faster kinetics and better selectivity for the dopamine transporter than [I-123]beta-CIT. We examined the organ biodistribution and radiation safely of these two compounds in six healthy volunteers who received an injection with each of the two compounds 2 weeks spare, Data were obtained on the Strichman 860 whole-body scanner, Transmission scans were obtained in all subjects prior to the injection of the radiotracer with a line source and used, to derive organ-specific attenuation correction factors, Whole-body planar images were acquired every hour for the first 6 h, and at 24 h, Attenuation-corrected regional conjugate counts were converted into units of activity using a calibration factor obtained for each subject by dividing whole-body conjugate decay-corrected counts from die first acquisition by the injected activity, Radiation dose estimates were on average higher for [I-123]CIT-FE than for [I-123]CIT-FP, with the lower large intestine receiving the highest exposure: 0.15+/-13% mGy/MBq (mean +/-COV) and 0.12+/-14% mGy/MBq for [I-123]FE-CIT and [I-123]FP-CIT, respectively, followed by the upper large intestine and the spleen.
引用
收藏
页码:1422 / 1425
页数:4
相关论文
共 10 条
  • [1] Abi-Dargham A, 1996, J NUCL MED, V37, P1129
  • [2] REGIONAL BRAIN UPTAKE AND PHARMACOKINETICS OF [I-123] N-OMEGA-FLUOROALKYL-2-BETA-CARBOXY-3-BETA-(4-IODOPHENYL)NORTROPANE ESTERS IN BABOONS
    BALDWIN, RM
    ZEAPONCE, Y
    ALTIKRITI, MS
    ZOGHBI, SS
    SEIBYL, JP
    CHARNEY, DS
    HOFFER, PB
    WANG, SY
    MILIUS, RA
    NEUMEYER, JL
    INNIS, RB
    [J]. NUCLEAR MEDICINE AND BIOLOGY, 1995, 22 (02): : 211 - 219
  • [3] Bergstrom KA, 1996, HUM PSYCHOPHARM CLIN, V11, P483, DOI 10.1002/(SICI)1099-1077(199611)11:6<483::AID-HUP818>3.3.CO
  • [4] 2-0
  • [5] Radiosynthesis of [F-18] N-3-fluoropropyl-2-beta-carbomethoxy-3-beta-(4-iodophenyl) nortropane and the first human study with positron emission tomography
    Chaly, T
    Dhawan, V
    Kazumata, K
    Antonini, A
    Margouleff, C
    Dahl, JR
    Belakhlef, A
    Margouleff, D
    Yee, A
    Wang, SY
    Tamagnan, G
    Neumeyer, JL
    Eidelberg, D
    [J]. NUCLEAR MEDICINE AND BIOLOGY, 1996, 23 (08): : 999 - 1004
  • [6] SEVERE DEPLETION OF COCAINE RECOGNITION SITES ASSOCIATED WITH THE DOPAMINE TRANSPORTER IN PARKINSONS-DISEASED STRIATUM
    KAUFMAN, MJ
    MADRAS, BK
    [J]. SYNAPSE, 1991, 9 (01) : 43 - 49
  • [7] COMPARISON OF I-123 LABELED 2-BETA-CARBOMETHOXY-3-BETA-(4-IODOPHENYL)TROPANE AND 2-BETA-CARBOMETHOXY-3-BETA-(4-IODOPHENYL)-N-(3-FLUOROPROPYL)NORTROPANE FOR IMAGING OF THE DOPAMINE TRANSPORTER IN THE LIVING HUMAN BRAIN
    KUIKKA, JT
    BERGSTROM, KA
    AHONEN, A
    HILTUNEN, J
    HAUKKA, J
    LANSIMIES, E
    WANG, SY
    NEUMEYER, JL
    [J]. EUROPEAN JOURNAL OF NUCLEAR MEDICINE, 1995, 22 (04): : 356 - 360
  • [8] N-OMEGA-FLUOROALKYL ANALOGS OF (1R)-2-BETA-CARBOMETHOXY-3-BETA-(4-IODOPHENYL)-TROPANE (BETA-CIT) - RADIOTRACERS FOR POSITRON EMISSION TOMOGRAPHY AND SINGLE-PHOTON EMISSION COMPUTED-TOMOGRAPHY IMAGING OF DOPAMINE TRANSPORTERS
    NEUMEYER, JL
    WANG, SY
    GAO, YG
    MILIUS, RA
    KULA, NS
    CAMPBELL, A
    BALDESSARINI, RJ
    ZEAPONCE, Y
    BALDWIN, RM
    INNIS, RB
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 1994, 37 (11) : 1558 - 1561
  • [9] SEIBYL JP, 1994, J NUCL MED, V35, P764
  • [10] VOLKOW N D, 1992, Journal of Nuclear Medicine, V33, P888