Comparative evaluation in nonhuman primates of five PET radiotracers for imaging the serotonin transporters: [11C]McN 5652, [11C]ADAM, [11C]DASB, [11C]DAPA, and [11C]AFM

Journal of Cerebral Blood Flow and Metabolism

Volumn 22, Issue 11, 2002, Pages 1377-1398

  Huang, Yiyun ^a   Hwang, Dah Ren ^a   Narendran, Raj ^a   Sudo, Yasuhiko ^a   Chatterjee, Rano ^a   Bae, Sung A ^a   Mawlawi, Osama ^a   Kegeles, Lawrence S ^a   Wilson, Alan A ^a   Kung, Hank F ^a   Laruelle, Marc ^a  

^a NEW YORK STATE PSYCHIATRIC INSTITUTE   (United States)

Author keywords

Brain imaging; Kinetic analysis; Positron emission tomography; Serotonin transporters; SSRI

Indexed keywords

1,2,3,5,6,10B HEXAHYDRO 6 (4 METHYLTHIOPHENYL)PYRROLO[2,1 A]ISOQUINOLINE; 1,2,3,5,6,10B HEXAHYDRO 6 (4 METHYLTHIOPHENYL)PYRROLO[2,1 A]ISOQUINOLINE C 11; 2 [2 (DIMETHYLAMINOMETHYLPHENYLTHIO)] 5 FLUOROMETHYLPHENYLAMINE C 11; 2 [2 (DIMETHYLAMINOMETHYLPHENYLTHIO)] 5 IODOPHENYLAMINE C 11; 3 AMINO 4 [2 (DIMETHYLAMINOMETHYLPHENYLTHIO)]BENZONITRILE C 11; 5 BROMO 2 [2 (DIMETHYLAMINOMETHYLPHENYLTHIO)]PHENYLAMINE C 11; ANILINE DERIVATIVE; BENZYLAMINE DERIVATIVE; CARBON 11; SEROTONIN TRANSPORTER; TRACER; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; BRAIN REGION; COMPARTMENT MODEL; CONTROLLED STUDY; DRUG CLEARANCE; DRUG PROTEIN BINDING; DRUG UPTAKE; LIPOPHILICITY; MALE; NONHUMAN; PARTITION COEFFICIENT; POSITRON EMISSION TOMOGRAPHY; PRIMATE; PRIORITY JOURNAL; RAT; RELIABILITY; SIGNAL NOISE RATIO;

EID: 0036842463     PISSN: 0271678X     EISSN: None     Source Type: Journal    
DOI: 10.1097/01.WCB.0000040948.67415.05     Document Type: Article

References (77)

1. Abi-Dargham A, Laruelle M, Seibyl J, Rattner Z, Baldwin RM, Zoghbi SS, Zea-Ponce Y, Bremner JD, Hyde TM, Charney DS, Hoffer PB, Innis RB (1994) SPECT measurement of benzodiazepine receptors in human brain with [I-123]iomazenil: Kinetic and equilibrium paradigms. J Nucl Med 35:228-238
2. Abi-Dargham A, Krystal JH, Anjilvel S, Scanley BE, Zoghbi S, Baldwin RM, Rajeevan N, Ellis S, Petrakis IL, Seibyl JP, Charney DS, Laruelle M, Innis RB (1998) Alterations of benzodiazepine receptors in type II alcoholic subjects measured with SPECT and [I-123]iomazenil. Am J Psychiatry 155:1550-1555
3. 11C]NNC 756. Synapse 32:93-109
4. 18F]fallypride. J Nucl Med 41:139P.
5. 11C]NNC 112 in humans: Validation and reproducibility. J Cereb Blood Flow Metab 20:225-243
6. 123I]IDAM. Eur J Nucl Med 26:854-861
7. 123I]ODAM. Eur J Nucl Med 26:1359-1362
8. 123I]ADAM and SPECT. J Nucl Med 42:1556-1562
9. 3H]paroxetine binding to serotonin uptake sites in human brain tissue. Brain Res 486:261-268
10. Bergstrom KA, Halldin C, Hall H, Lundkvist C, Ginovart N, Swahn CG, Farde L (1997) In vitro and in vivo characterisation of norbeta-CIT: A potential radioligand for visualisation of the serotonin transporter in the brain. Eur J Nucl Med 24:596-601
11. Brix G, Zaers J, Adam LE, Bellemann ME, Ostertag H, Trojan H, Haberkorn U, Doll J, Oberdorfer F, Lorenz WJ (1997) Performance evaluation of a whole-body PET scanner using the NEMA protocol. National Electrical Manufacturers Association. J Nucl Med 38:1614-1623
12. 11C](+)McN-5652: Assessment of methods. J Cereb Blood Flow Metab 20:253-262
13. 18F]cyclofoxy and positron emission tomography. J Cereb Blood Flow Metab 13:24-42
14. 125I]ADAM to serotonin transporters in rat brain. Synapse 38:403-412
15. 3H]paroxetine. Neuroscience 27:473-496
16. 11C]citalopram. Int J Rad Appl Instrum [A] 41:541-543
17. 3H]paroxetine binding is altered in the hippocampus but not the frontal cortex or caudate nucleus from subjects with schizophrenia. J Neurochem 64:1197-1202
18. Elfving B, Bjornholm B, Ebert B, Knudsen GM (2001) Binding characteristics of selective serotonin reuptake inhibitors with relation to emission tomography studies. Synapse 41:203-211
19. Gandelman MS, Baldwin RM, Zoghbi SS, Zea-Ponce Y, Innis RB (1994) Evaluation of ultrafiltration for the free fraction determination of single photon emission computerized tomography (SPECT) radiotracers: β-CIT, IBF and iomazenil. J Pharm Sci 83:1014-1019
20. 11C]DASB binding to the human serotonin transporter: Modeling strategies. J Cereb Blood Flow Metab 21:1342-1353
21. Gurevich EV, Joyce JN (1997) Alterations in the cortical serotonergic system in schizophrenia: A postmortem study. Biol Psychiatry 42:529-545
22. 11C]cyanoimipramine. Int J Rad Appl Instrum [B] 14:587-592
23. Heinz A, Ragan P, Jones DW, Hommer D, Williams W, Knable MB, Gorey JG, Doty L, Geyer C, Lee KS, Coppola R, Weinberger DR, Linnoila M (1998) Reduced central serotonin transporters in alcoholism. Am J Psychiatry 155:1544-1549
24. 11C]DASB. Eur J Nucl Med 27:1719-1722
25. Huang Y, Mahmood K, Simpson NR, Mason NS, Mathis CA (1998) Stereoconservative synthesis of the enantiomerically pure precursors of [C-11](+)-McN 5652 and [C-11](-)-McN 5652. J Labelled Comp Radiopharm 41:9-17
26. Huang Y, Bae S-A, Zhu Z, Guo N, Hwang DR, Laruelle M (2001) Fluorinated analogues of ADAM as new PET radioligands for the serotonin transporter: Synthesis and pharmacological evaluation. J Labelled Comp Radiopharm 44:S18-S20
27. 11C]DAPA). Nucl Med Biol (in press)
28. Hume SP, Pascali C, Pike VW, Turton DR, Ahier RG, Myers R, Bateman DM, Cremer JE, Manjil LG, Dolan R (1991) Citalopram: Labeling with carbon-11 and evaluation in rat as a potential radioligand for in vivo PET studies of 5-HT re-uptake sites. Int J Rad Appl Instrum [B] 18:339-351
29. 11C](+)McN5652. Biol Psychiatry 51:715-722
30. 11C]McN5652. J Cereb Blood Flow Metab 22:490-501
31. Jacobsen LK, Staley JK, Malison RT, Zoghbi SS, Seibyl JP, Kosten TR, Innis RB (2000) Elevated central serotonin transporter binding availability in acutely abstinent cocaine-dependent patients. Am J Psychiatry 157:1134-1140
32. Jagust WJ, Eberling JL, Biegon A, Taylor SE, VanBrocklin HF, Jordan S, Hanrahan SM, Roberts JA, Brennan KM, Mathis CA (1996) Iodine-123-5-iodo-6-nitroquipazine: SPECT radiotracer to image the serotonin transporter. J Nucl Med 37:1207-1214
33. Joyce JN, Shane A, Lexow N, Winokur A, Casanova MF, Kleinman JE (1993) Serotonin uptake sites and serotonin receptors are altered in the limbic system of schizophrenics. Neuropsychopharmacology 8:315-336
34. 123I]IDAM as a novel single-photon emission tomography tracer for serotonin transporters. Eur J Nucl Med 26:844-853
35. 11C]raclopride studies. J Cereb Blood Flow Metab 16:42-52
36. 3H]paroxetine binding, a marker of serotonin uptake sites. Biol Psychiatry 24:299-309
37. Laruelle M, Abi-Dargham A, Casanova MF, Toti R, Weinberger DR, Kleinman JE (1993a) Selective abnormalities of prefrontal serotonergic receptors in schizophrenia: A postmortem study. Arch Gen Psychiatry 50:810-818
38. 123I]β-CIT: Pharmacological characterization of brain uptake in nonhuman primates. Synapse 13:295-309
39. 123I]β-CIT in vivo binding to dopamine transporters in healthy subjects. J Cereb Blood Flow Metab 14:982-994
40. 2 receptors in healthy subjects. J Nucl Med 35:743-754
41. 123I]iomazenil binding to benzodiazepine receptors in nonhuman primates. I. Kinetic modeling of single bolus experiments. J Cereb Blood Flow Metab 14:439-452
42. 123I]beta-CIT. Biol Psychiatry 47:371-379
43. 11C]-sertraline. Int J Rad Appl Instrum [A] 40:147-151
44. 11C]dapoxetine.HCl, a serotonin re-uptake inhibitor: Biodistribution in rat and preliminary PET imaging in the monkey. Nucl Med Biol 21:669-675
45. Lundkvist C, Loc'h C, Halldin C, Bottlaender M, Ottaviani M, Coulon C, Fuseau C, Mathis C, Farde L, Maziere B (1999) Characterization of bromine-76-labeled 5-bromo-6-nitroquipazine for PET studies of the serotonin transporter. Nucl Med Biol 26:501-507
46. 123I]-2 beta-carbomethoxy-3 beta-(4-iodophenyl)tropane and single photon emission computed tomography. Biol Psychiatry 44:1090-1098
47. Mawlawi O, Martinez D, Slifstein M, Broft A, Chatterjee R, Hwang DR, Huang Y, Simpson N, Ngo K, Van Heertum R, Laruelle M (2001a) Imaging human mesolimbic dopamine transmission with positron emission tomography Part I: Accuracy and precision of D2 receptor parameter measurements in ventral striatum. J Cereb Blood Flow Metab 21:1034-1057
48. 11C]MDL 100907: Validation and reproducibility. J Nucl Med 42:112p
49. McCann UD, Szabo Z, Scheffel U, Dannals RF, Ricaurte GA (1998) Positron emission tomographic evidence of toxic effect of MDMA ("Ecstasy") on brain serotonin neurons in human beings. Lancet 352:1433-1437
50. 11C]DASB PET imaging study. Am J Psychiatry 158:1843-1849
51. Mintun MA, Raichle ME, Kilbourn MR, Wooten GF, Welch MJ (1984) A quantitative model for the in vivo assessment of drug binding sites with positron emission tomography. Ann Neurol 15:217-227
52. Nelson DR, Palmer KJ, Johnson AM (1991) The monoamine uptake inhibitory properties of iodo-6′-paroxetine. Biol Psychiatry 29:632S
53. 123I]2β-carbomethoxy-3β-(4-iodophenyl)tropane (B-CIT): High affinity SPECT radiotracer of monoamine reuptake sites in brain. J Med Chem 34:3144-3146
54. 123I]IDAM, 5-iodo-2-((2-((dimethylamino)methyl)phenyl)thio)benzyl alcohol. J Med Chem 42:333-335
55. Oya S, Choi S, Hou C, Mu M, Kung M, Acton PD, Siciliano M, Kung HF (2000) 2-((2-((dimethylamino)methyl)phenyl)thio)-5-iodophenylamine (ADAM): An improved serotonin transporter ligand. Nucl Med Biol 27:249-254
56. 11C]McN 5652. J Nucl Med 41:1465-1477
57. 3H-imipramine. Prog Neuropsychopharmacol Biol Psychiatry 14:61-72
58. Rochat B, Baumann P, Audus KL (1999) Transport mechanisms for the antidepressant citalopram in brain microvessel endothelium. Brain Res 831:229-236
59. 3H-paroxetine in human brain. J Neural Transm 104:89-96
60. Rowland M, Tozer TN (1989) Clinical Pharmacokinetics. 2nd Ed. Philadelphia: Lea & Febiger
61. Scheffel U, Dannals RF, Suehiro M, Ricaurte GA, Carroll FI, Kuhar MJ, Wagner H Jr (1994) Development of PET/SPECT ligands for the serotonin transporter. NIDA Res Monogr 138:111-130
62. Shank RP, Vaught JL, Pelley KA, Setler PE, McComsey DF, Maryanoff BE (1988) McN-5652: A highly potent inhibitor of serotonin uptake. J Pharmacol Exp Ther 247:1032-1038
63. 11C]venlafaxine: Serotonin uptake inhibition, biodistribution and binding in living pig brain. Eur Neuropsychopharmacol 7:195-200
64. 11C](+)McN5652 as a radiotracer for imaging serotonin uptake sites with PET. Life Sci 53:883-892
65. Suehiro M, Scheffel U, Dannals RF, Ravert HT, Ricaurte GA, Wagner H Jr (1993b) A PET radiotracer for studying serotonin uptake sites: Carbon-11-McN-5652Z. J Nucl Med 34:120-127
66. 11C]McN5652. J Cereb Blood Flow Metab 15:798-805
67. 11C](+)McN5652. Synapse 20:37-43
68. 11C]McN5652: A serotonin transporter radioligand. J Cereb Blood Flow Metab 19:967-981
69. Tiihonen J, Kuikka JT, Bergstrom KA, Karhu J, Viinamaki H, Lehtonen J, Hallikainen T, Yang JW, Hakola P (1997) Singlephoton emission tomography imaging of monoamine transporters in impulsive violent behaviour. Eur J Nucl Med 24:1253-1260
70. 11C]ADAM: A potent radioligand for the serotonin transporter exploration by PET. J Labelled Comp Radiopharm 44:113-120
71. 123I]-beta-CIT SPECT imaging shows reduced brain serotonin transporter availability in drug-free depressed patients with seasonal affective disorder. Biol Psychiatry 47:482-489
72. Wilson AA, Houle S (1999) Radiosynthesis of carbon-11 labelled N-methyl-2(arylthio)benzylamines: Potential radiotracers for the serotonin reuptake receptor. J Labelled Comp Radiopharm 42:1277-1288
73. 11C-labeled 2-(phenylthio)araalkylamines. J Med Chem 43:3103-3110
74. Wilson AA, Jin L, Garcia A, DaSilva JN, Houle S (2001) An admonition when measuring the lipophilicity of radiotracers using counting techniques. Appl Radiat Isot 54:203-208
75. Woods RP, Mazziotta JC, Cherry SR (1993) MRI-PET registration with automated algorithm. J Comput Assist Tomogr 17:536-546
76. 11C]LY257327 as a tracer for 5-HT transporters. Nucl Med Biol 24:251-254
77. Zhuang Z, Choi S, Hou C, Mu M, Kung M, Acton PD, Kung HF (2000) A novel serotonin transporter ligand: (5-iodo-2-(2-dimethylaminomethylphenoxy)-benzyl alcohol. Nucl Med Biol 27:169-175