Biodistribution and dosimetry of TRODAT-1: A technetium-99m tropane for imaging dopamine transporters

Journal of Nuclear Medicine

Volumn 39, Issue 12, 1998, Pages 2069-2076

  Mozley, P David ^a   Stubbs, James B ^b   Plössl, Karl ^b   Dresel, Stefan H ^b   Barraclough, Eleathea D ^b   Alavi, Abass ^b   Araujo, Luis I ^b   Kung, Hank F ^b  

^a UNIVERSITY OF PENNSYLVANIA   (United States)

^b NONE

Author keywords

Brain; Computed tomography; Technetium 99m; TRODAT 1

Indexed keywords

[2 [[2 [[[3 (4 CHLOROPHENYL) 8 METHYL 8 AZABICYCLO[3.2.1]OCT 2 YL]METHYL](2 MERCAPTOETHYL)AMINO]ETHYL]AMINO]ETHANETHIOLATO]OXOTECHNETIUM TC 99M; PERTECHNETIC ACID TC 99M; TECHNETIUM 99M; TROPANE DERIVATIVE;

ADULT; ARTICLE; CLINICAL ARTICLE; CLINICAL TRIAL; COGNITION; DOPAMINE UPTAKE; DOSIMETRY; DRUG DISTRIBUTION; DRUG EXCRETION; DRUG SAFETY; FEMALE; GASTROINTESTINAL TRACT FUNCTION; HUMAN; ISOTOPE LABELING; MALE; PRIORITY JOURNAL; SINGLE PHOTON EMISSION COMPUTER TOMOGRAPHY;

ADULT; BRAIN; CARRIER PROTEINS; DOPAMINE PLASMA MEMBRANE TRANSPORT PROTEINS; FEMALE; HUMANS; IMAGE PROCESSING, COMPUTER-ASSISTED; INJECTIONS, INTRAVENOUS; KINETICS; MALE; MEMBRANE GLYCOPROTEINS; MEMBRANE TRANSPORT PROTEINS; MIDDLE AGED; NERVE TISSUE PROTEINS; ORGANOTECHNETIUM COMPOUNDS; RADIOPHARMACEUTICALS; REPRODUCIBILITY OF RESULTS; TISSUE DISTRIBUTION; TOMOGRAPHY, EMISSION-COMPUTED, SINGLE-PHOTON; TROPANES;

EID: 0032407607     PISSN: 01615505     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (74)

1. McHugh PR. The neuropsychiatry of basal ganglia disorders: a triadic syndrome and its explanation. Neuropsychiatry Neuropsychol Behav Neurol 1989;2:239-247.
2. Alexander GE, Crutcher MD, DeLong MR. Basal ganglia-thalamocortical circuits: parallel substrates for motor, oculomotor, "prefrontal" and "limbic" function. In: Uylings HBM, Van Edin CG, De Bruin JPC, Corner MA, Feenstra MGP, eds. Progress in brain research, vol 85. New York: Elsevier Science Publishers; 1990:119-146.
3. Smith GP, Schneider LH. Relationships between mesolimbic dopamine function and eating behavior. Ann New York Acad Sci 1988;537:254-261.
4. Leibowitz SF, Rossakis C. Mapping study of brain dopamine- and epinephrine-sensitive sites which cause feeding suppression in the rat. Pharmacological characterization of perifornical hypothalamic dopamine receptors mediating feeding inhibition in the rat. Brain Res 1979a;172:101-113;
5. Leibowitz SF, Rossakis C. Brain Res 1979b;172:115-130.
6. Silverstone JT, Fincham J, Wells B, Kyriakides M. The effect of the dopamine receptor blocking drug pimozide on the stimulant and anorectic actions of dextroamphetamine in man. Neuropharm 1980;19:1235-1237.
7. Cooper JR, Bloom FE, Roth RH. The biological basis of neuropharmacology, 6th ed. New York: Oxford University Press; 1991:292-294.
8. Fowler JS, Volkow KD, Wolf AP, et al. Mapping cocaine binding sites in human and baboon brain in vivo. Synapse 1989;4:371-377.
9. Carroll FI, Abram P, Lewin AH, Parham K, Boja JW, Kuhar MJ. Isopropyl and phenyl esters of 3b-(4-substituted phenyl)tropan-2b-carboxylic acids. Potent and selective compounds for the dopamine transporter. J Med Chem 1992;35:2497-2500.
10. Johanson CE, Fischman, M. The pharmacology of cocaine related to its abuse. Pharmacol Rev 1989;41:3-52.
11. Carroll FI, Scheffel U, Dannals RF, Boja JW, Kuhar MJ. Development of imaging agents for the dopamine transporter. Med Res Rev 1995b;15:419-444.
12. 3H cocaine in striatum and its relationship to the dopamine transporter. Membrane Biochem 1988; 7:87-106.
13. Fowler JS, Volkow ND, MacGregor RR, et al. Comparative PET studies of the kinetics and distribution of cocaine and cocaethylene in baboon brain. Synapse 1992;12:220-227.
14. Abraham P, Pitner JB, Lewin AH, Boja JW, Kuhar MJ, Carroll FI. N-modified analogues of cocaine: synthesis and inhibition of binding to the cocaine receptor. J Med Chem 1992;35:141-144.
15. Goodman MM, Kung M-P, Kabalka GW, Kung HF, Switzer R. Synthesis and characterization of radioiodinated N-(3-iodopropen-l-yl)-2b-carbomethoxy-3b-(4-chlorophenyl)tropanes: potential dopamine reuptake site imaging agents. J Med Chem 1994;37:1535-1542.
16. Scheffel U, Dannals RF, Wong DF, Yokoi F, Carroll FI, Kuhar MJ. Dopamine transporter imaging with novel, selective cocaine analogs. Neuroreport 1992;3:969-972.
17. Carroll FI, Lewin AH, Boja JW, Kuhar MJ. Cocaine receptor: biochemical characterization and structure-activity relationships of cocaine analogues at the dopamine transporter. J Med Chem 1992;35:969-981.
18. Wang S, Gao Y, Laruelle M, et al. Enantioselectivity of cocaine recognition sites: binding of (1S)- and (1R)-2 beta-carbomethoxy-3 beta-(4-iodophenyl)tropane (beta-CIT) to monoamine transporters. J Med Chem 1993;36:1914-1917.
19. Meltzer PC, Liang AY, Brownell AL, Elmaleh DR, Madras BK. Substituted 3-phenyltropane analogs of cocaine: synthesis, inhibition of binding at cocaine recognition sites, and positron emission tomography imaging. J Med Chem 1993;36:855-862.
20. 3H-2β-carbomethoxy-3β-(4-fluorophenyl)tropane. Mol Pharmacol 1989; 36:518-524.
21. Boja J, Carroll F, Rahman M, Philip A, Lewin A, Kuhar M. New, potent cocaine analogs: ligand binding and transport studies in rat striatum. Eur J Pharmacol 1990;184:329-332.
22. Ritz M, Boja J, Grigoriadis D, et al. Hydrogen-3-WIN 35,065-2: a ligand for cocaine receptors in striatum. J Neurochem 1990;55:1556-1562.
23. Kozikowski AP, Roberti M, Xiang L, et al. Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. J Med Chem 1992;35: 4764-4766.
24. 125I]RTI-55: in vitro binding and autoradiographic characterization. J Neurochem 1994;62:549-546.
25. Shaya EK, Scheffel U, Dannals RF, et al. In vivo imaging of dopamine reuptake sites in the primate brain using single photon emission computed tomography (SPECT) and iodine-123 labeled RTI-55. Synapse 1992;10:169-172.
26. Neumeyer JL, Wang S, Milius RA, et al. Iodine-123-2b-carbomethoxy-3b-(4-iodophenyl)tropane: high-affinity SPECT radiotracer of monoamine reuptake sites in brain. J Med Chem 1991;34:3144-3146.
27. Neumeyer JL, Wang S, Gao Y, et al. N-w-fluoroalkyl analogs of (1R)-2b-carbomethoxy-3b-(4-iodophenyl)-tropane (b-CIT): radiotracers for positron emission tomography and single photon emission computed tomography imaging of dopamine transporters. J Med Chem 1994;37:1558-1561.
28. 123I CIT. Eur J Pharmacol 1991;200:369-370.
29. Boja W, Patel A, Carroll FI, et al. Iodine-125-RTI-55: a potent ligand for dopamine transporters. Eur J Pharmacol 1991;194:133-134.
30. 125I-RTI-55 to dopamine transporter: pharmacology and regional distribution with autoradiography. Synapse 1992;12:37-46.
31. 123I]B-CIT: pharmacological characterization of uptake in nonhuman primates. Synapse 1993;13:295-305.
32. Aronson B, Enmon JL, Izenwasser S, et al. Synthesis and ligand binding of h6-(2b-carbomethoxy-3b-phenyltropane) transition metal complexes. J Med Chem 1996;39:1560-1563.
33. Carroll FI, Mascarella SW, Kuzemko MA, et al. Synthesis, ligand binding, and QSAR (CoMFA and classical) study of 3b-(3′-substituted phenyl)-, 3b-(4′-substituted phenyl)-, and 3b-(3′,4′-disubstituted phenyl)tropane-2b-carboxylic acid methyl esters. J Med Chem 1994;37:2865-2873.
34. Neumeyer JL, Tamagnan G, Wang S, et al. N-substituted analogs of 2 beta-carbomethoxy-3 beta-(4′-iodophenyl)tropane (beta-CIT) with selective affinity to dopamine or serotonin transporters in rat forebrain. J Med Chem 1996;39:543-548.
35. Volkow ND, Fowler JS, Wang GJ, et al. Decreased dopamine transporters with age in healthy human subjects. Ann Neurol 1994;36:237-239.
36. I23I]IPT and single-photon emission tomography. Eur J Nucl Med 1997;24:415-421.
37. 11C-WIN 35,428 reveals marked declines in mild Parkinson's disease [see comments]. Ann Neurol 1993;34:423-431.
38. Innis RB, Seibyl JP, Scanley BE, et al. Single photon emission computed tomographic imaging demonstrates loss of striatal dopamine transporters in Parkinson's disease. Proc Natl Acad Sci USA 1993;90:11965-11969.
39. Innis RB. Single photon emission tomography imaging of dopamine terminal innervation: a potential clinical tool in Parkinson's disease [Editorial]. Eur J Nucl Med 1994;21:1-5.
40. Volkow ND, Ding YS, Fowler JS, et al. A new PET ligand for the dopamine transporter: studies in the human brain. J Nucl Med 1995;36:2162-2168.
41. 11C-WIN35,428. Synapse 1993; 15:130-142.
42. Yu D-W, Galley SJ, Wolf AP, et al. Synthesis of carbon-11-labeled iodinated cocaine derivatives and their distribution in baboon brain measured using positron emission tomography. J Med Chem 1992;35:2178-2183.
43. Kuikka JT, Akerman K, Bergstrom KA, et al. Iodine-123-labeled N-(2-fluoroethyl)-2b-carbomethoxy-3b-(4-iodophenyl)nortropane for dopamine transporter imaging in the living human brain. Eur J Nucl Med 1995;22:682-686.
44. Meegalla SK, Plossl K, Kung M-P, et al. Technetium-99m labeled tropanes as dopamine transporter imaging agents. Bioconj Chem 1996;7:421-429.
45. Meltzer PC, Blundell P, Jones AG, et al. A technetium-99m SPECT imaging agent which targets the dopamine transporter in primate brain. J Med Chem 1997;40:1835-1844.
46. Madras BK, Jones AG, Mahmood A, et al. Technepine: a high affinity technetium-99m probe to label the dopamine transporter in brain by SPECT imaging. Synapse 1996;22:239-246.
47. 99mTc imaging ligand for dopamine transporter. Tetrahedron Lett 1996;37:4353-4356.
48. 99mTc [Abstract]. J Nucl Med 1997;38:100P.
49. Steigman J, Eckelman WC. The chemistry of technetium in medicine. Washington, DC: National Academy; 1992.
50. Sorenson JA, Phelps ME. Physics in nuclear medicine, 2nd ed. Philadelphia: WB Saunders Co.; 1987.
51. 99mTc-labeled tropanes as dopamine transporter imaging agents. J Med Chem 1997;40:9-17.
52. Kung M-P, Stevenson DA, Plössl K, et al. Technetium-99m TRODAT-1: a novel technetium-99m complex as a dopamine transporter imaging agent. Eur J Nucl Med 1997;24:372-380.
53. 99mTc TRODAT-1: a novel compound for imaging the dopamine transporter. J Nucl Med 1999: in press.
54. Kung HF, Kim H-J, Kung M-P, Meegalla SK, Plössl K, Lee H-K. Imaging of dopamine transporters in humans with technetium-99m TRODAT-1. Eur J Nucl Med 1996;23:1527-1530.
55. Sorenson JA, Phelps ME. Internal radiation dosimetry. In: Physics in nuclear medicine, 2nd ed. Philadelphia: WB Saunders Co.; 1987:197-218.
56. Mozley PD, Zhu XW, Kung HF, et al. The dosimetry of 3-Iodo-Schering 23390: quantification of the radiation burden to healthy humans. J Nucl Med 1993;34:208-213.
57. 123I IBF: a potent radioligand for imaging the D2 dopamine receptor. J Nucl Med 1993;34:1910-1917.
58. Mozley PD, Stubbs JB, Kim H-J, et al. Dosimetry of a D2/D3 dopamine receptor antagonist that can be used with PET or SPECT. J Nucl Med 1995;35:1322-1331.
59. Mozley PD, Stubbs JB, Kim H-J, et al. Dosimetry of an iodine-123-labeled tropane to image dopamine transporters. J Nucl Med 1996;37:151-159.
60. 123I dynamic SPECT imaging [Abstract]. J Nucl Med 1993;34:190P.
61. Chang LT. A method for attenuation correction in radionuclide computed tomography. IEEE Trans Nucl Sci 1978;NS-25:638-643.
62. Cloutier RJ, Smith SA, Watson EE, Snyder WS, Warner GG. Dose to the fetus from radionuclides in the bladder. Health Physics 1973;25:147-161.
63. International Commission on Radiation Protection. ICRP publication 30. Limits for intake of radionuclides by workers. New York: Pergamon Press; 1979.
64. International Commission on Radiation Protection. ICRP publication 23. Report of the task group on reference man. Oxford: Pergamon Press; 1979.
65. Loevinger R, Berman M. MIRD pamphlet no. 1, revised. A revised schema for calculating the absorbed dose from biologically distributed radionuclides. New York: Society of Nuclear Medicine; 1975.
66. Cristy M, Eckerman K. Specific absorbed fractions of energy at various ages from internal photon sources. ORNL/TM-8381. Oak Ridge, TN: Oak Ridge National Laboratory Press; 1987.
67. Snyder WS, Ford MR, Warner GG, Watson SB. MIRD pamplet no. 11. "S" absorbed dose per unit cumulated activity for selected radionuclides and organs. New York: Society of Nuclear Medicine; 1975.
68. Lange RA, Cigarroa RG, Yancey CW Jr, et al. Cocaine-induced coronary-artery vasoconstriction. New Engl J Med 1989;321:1157-62.
69. Moliterno DJ, Willard JE, Lange RA, et al. Coronary-artery vasoconstriction induced by cocaine, cigarette smoking, or both. N Eng J Med 1994;330:454-459.
70. 123I-labeled IPT. J Nucl Med 1996;37:151-160.
71. Gatley S. Estimation of upper limits on human radiation absorbed doses from carbon-II-labeled compounds. J Nucl Med 1993;34:2208-2210.
72. Selikson MH, Jaggi J, Mozley PD, et al. A proposal for minimum detectable compartment in MIRD dosimetry modeling. Phys Med Biol 1997;42:1605-1617.
73. National Council of Radiation Protection and Measurements. NCRP report no. 39. Basic radiation protection criteria. Washington, DC: National Council of Radiation Protection and Measurements; 1971.
74. Food and Drug Administration, HHS. Radioactive drugs for certain research uses. Code of Federal Regulations 21. ch. 1 (4-1-89 ed.) part 361.1. paragraph (b) (3) (i). Washington, DC: Food and Drug Adminsitration; 1989:206.