Characterization of [123I]IDAM as a novel single-photon emission tomography tracer for serotonin transporters

European Journal of Nuclear Medicine

Volumn 26, Issue 8, 1999, Pages 844-853

  Kung, Mei Ping ^a   Hou, Catherine ^a   Oya, Shunichi ^a   Mu, Mu ^a   Acton, Paul D ^a   Kung, Hank F ^a  

^a UNIVERSITY OF PENNSYLVANIA   (United States)

Author keywords

Autoradiography; Brain imaging; Receptor binding; Selective serotonin reuptake inhibitors; Serotonergic neuron

Indexed keywords

ANTIDEPRESSANT AGENT; BENZYL ALCOHOL DERIVATIVE; CHLORAMPHETAMINE; DOPAMINE; IODINE 123; NORADRENALIN; PROTEIN; SEROTONIN TRANSPORTER; SEROTONIN UPTAKE INHIBITOR; TRACER; 5 IODO 2 ((2 ((METHYLAMINO)METHYL)PHENYL)THIO)BENZYL ALCOHOL; 5-IODO-2-((2-((METHYLAMINO)METHYL)PHENYL)THIO)BENZYL ALCOHOL; CARRIER PROTEIN; DIAGNOSTIC AGENT; MEMBRANE PROTEIN; NERVE PROTEIN; RADIOACTIVE IODINE; RADIOPHARMACEUTICAL AGENT; SEROTONIN; SLC6A4 PROTEIN, HUMAN; SLC6A4 PROTEIN, RAT; SULFIDE;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; AUTORADIOGRAPHY; BINDING AFFINITY; BRAIN; BRAIN HOMOGENATE; BRAIN REGION; CELL LINE; DORSAL RAPHE NUCLEUS; FRONTAL CORTEX; GLOBUS PALLIDUS; GRAY MATTER; HUMAN; HYPOTHALAMUS; IN VITRO STUDY; IN VIVO STUDY; INTERPEDUNCULAR NUCLEUS; LOCUS CERULEUS; MALE; MEDIAN RAPHE NUCLEUS; MEMBRANE; NONHUMAN; OLFACTORY BULB; RAT; SCATCHARD PLOT; SEPTUM NUCLEUS; SEROTONINERGIC NERVE CELL; SINGLE PHOTON EMISSION COMPUTER TOMOGRAPHY; SUBSTANTIA NIGRA; SUPERIOR COLLICULUS; THALAMUS NUCLEUS; TISSUE DISTRIBUTION; ANIMAL; BINDING SITE; BRAIN LEVEL; METABOLISM; SCINTISCANNING; SPRAGUE DAWLEY RAT;

ANIMALS; AUTORADIOGRAPHY; BENZYL ALCOHOLS; BINDING SITES; BRAIN; BRAIN CHEMISTRY; CARRIER PROTEINS; HUMANS; IODINE RADIOISOTOPES; MALE; MEMBRANE GLYCOPROTEINS; MEMBRANE TRANSPORT PROTEINS; NERVE TISSUE PROTEINS; RADIOPHARMACEUTICALS; RATS; RATS, SPRAGUE-DAWLEY; SEROTONIN; SEROTONIN PLASMA MEMBRANE TRANSPORT PROTEINS; SULFIDES; TOMOGRAPHY, EMISSION-COMPUTED, SINGLE-PHOTON;

EID: 0032586820     PISSN: 03406997     EISSN: None     Source Type: Journal    
DOI: 10.1007/s002590050458     Document Type: Article

References (52)

1. 1A-mediated responses: effect of treatments that modify serotonergic neurotransmission. Ann NY Acad Sci 1990; 600: 460-475.
2. 2. Gozlan H, Hamon M. Pharmacology and molecular biology of central 5-HT receptors. In: Hamon M, Ollat T, Thiebot H, eds Anxiety: neurobiology, clinic and therapeutic perspectures. Colloque INSERM/John Libbey Eurotext; 1993: 232: 141-150.
3. 3. Frazer A. Antidepressants. J Clin Psychiatry 1997; 6: 9-25.
4. 4. Coryell W. The treatment of psychotic depression. J Clin Psychiatry 1998; 1: 22-27.
5. 5. Heninger GR, Delgado PL, Charney DS. The revised monoamine theory of depression: a modulatory role for monoamines, based on new findings from monoamine depletion experiments in humans. Pharmacopsychiatry 1996; 29: 2-11.
6. 6. Fuller RW. Serotonin uptake inhibitors: uses in clinical therapy and in laboratory research. Prog Drug Res 1995; 45: 167-204.
7. 7. Wong DT, Bymaster FP. Development of antidepressant drugs. Fluoxetine (Prozac) and other selective serotonin uptake inhibitors. Adv Exp Med Biol 1995; 363: 77-95.
8. 8. Holliday SM, Plosker GL. Paroxetine. A review of its pharmacology, therapeutic use in depression and therapeutic potential in diabetic neuropathy. Drugs Aging 1993; 3: 278-299.
9. 11C] sertraline. Int J Radiat Appl Inst [A] 1989; 40: 147-151.
10. 3H-imipramine binding in rat cerebral cortex. Eur J Pharmacol 1979; 54: 307-308.
11. 3H]-imipramine. J Pharmacol Exp Ther 1987; 242: 364-371.
12. 3H]paroxetine binding to rat cortical membranes. Eur J Pharmacol 1985; 118: 107-114.
13. 3H]6-nitroquipazine binding to the 5-hydroxytryptamine transport system in rat lung. Biochem Pharmacol 1991; 41: 1679-1682.
14. 3H]6-nitroquipazine to cortical membranes in the rat: inhibition by 5-hydroxytryptamine and 5-hydroxytryptamine uptake inhibitors. Neuropharmacology 1991; 30: 113-117.
15. 15. Perry EK, Marshall EF, Blessed G, Tomlinson BE, Perry RH. Decreased imiprimine binding in the brains of patients with depressive illness. Br J Psychiatry 1983; 142: 188-192.
16. 16. Mann JJ. The neurobiology of suicide. Nature Med 1998; 4: 25-30.
17. 11C](+)MCN5652. Synapse 1995; 20: 37-43.
18. 18. Szabo Z, Mohamadiyeh M, Scheffel U, Matthews WB, Ravert HT, Szabo K, Palmon S, Dannals RF. Impulse-response function and kinetic-model of C-11-labeled (+)MCN5652. J Nucl Med 1996; 37: 125.
19. 11C]MCN5652 extraction of characteristic images by artificial neural-network analysis. Behav Brain Res 1995; 73: 221-224.
20. 11C]McN5652. J Cereb Blood Flow Metab 1995; 15: 798-805.
21. 21. Suehiro M, Scheffel U, Dannals RF, Ravert HT, Ricaurte GA, Wagner HN. A PET radiotracer for studying serotonin uptake sites: carbon-11-McN-5652Z. J Nucl Med 1993; 34: 120-127.
22. 22. Suehiro M, Musachio JL, Dannals RF, Mathews WB, Ravert HT, Scheffel U, Wagner HN. An improved method for the synthesis of radiolabeled MCN5652 via thioester precursors. Nucl Med Biol 1995; 22: 543-545.
23. 23. Kung M-P, Chumpradit S, Billings JJ, Kung HF. 4-Iodotomoxetine: a novel ligand for serotonin uptake sites. Life Sci 1992; 51: 95-106.
24. 125I]5-Iodo-6-nitroquipazine: a potent and selective ligand for the 5-hydroxytryptamine uptake complex II in vivo studies in rats. Brain Res 1993; 619: 236-246.
25. 125I]5-Iodo-6-nitroquipazine: a potent and selective ligand for the 5-hydroxytryptamine uptake complex I in vitro studies. Brain Res 1993; 619: 229-235.
26. 26. Mathis CA, Biegon A, Taylor SE, Enas JD, Hanrahan SM. [I-125]5-Iodo-6-nitro-2-piperazinylquinoline: a potent and selective ligand for the serotonin uptake complex. Eur J Pharmacol 1992; 210: 103-104.
27. 27. Jagust WJ, Eberling JL, Biegon A, Taylor SE, VanBrocklin HF, Jordon S, Hanrahan SM, Roberts JA, Brennan KM, Mathis CA. Iodine-123-5-iodo-6-nitroquipazine: SPECT radiotracer to image the serotonin transporter. J Nucl Med 1996; 37: 1207-1214.
28. 123I]beta-CIT binding to dopamine and serotonin transporters. Eur J Nucl Med 1996; 23: 431-436.
29. 29. Kuikka JT, Tiihonen J, Bergstrom KA, Karhu J, Hartikainen P, Viinamaki H, Lansimies E, Lehtonen J, Hakola P. Imaging of serotonin and dopamine transporters in the living human brain. Eur J Nucl Med 1995; 22: 346-350.
30. 30. Tiihonen J, Kuikka JT, Bergstrom KA, Karhu J, Viinamaki H, Lehtonen J, Hallikainen T, Yang J, Hakola P. Single-photon emission tomography imaging of monoamine transporters in impulsive violent behaviour. Eur J Nucl Med 1997; 24: 1253-1260.
31. 31. Pirker W, Asenbaum S, Kasper S, Walter H, Angelberger P, Koch G, Pozzera A, Deecke L, Podreka I, Brucke T. Beta-CIT SPECT demonstrates blockade of 5HT-uptake sites by citalopram in the human brain in vivo. J Neural Transm Gen Sec 1995; 100: 247-256.
32. 32. Bergstrom KA, Halldin C, Hall H, Lundkvist C, Ginovart N, Swahn CG, Farde L. In vitro and in vivo characterisation of nor-beta-CIT: a potential radioligand for visualisation of the serotonin transporter in the brain. Eur J Nucl Med 1997; 24: 596-601.
33. 33. Blough BE, Abraham P, Mills AC, Lewin AH, Boja JW, Scheffel U, Kuhar MJ, Carroll FI. 3 Beta-(4-ethyl-3-iodophenyl)nortropane-2 beta-carboxylic acid methyl ester as a high-affinity selective ligand for the serotonin transporter. J Med Chem 1997; 40: 3861-3864.
34. 34. Hiltunen J, Akerman KK, Kuikka JT, Bergstrom KA, Halldin C, Nikula T, Rasanen P, Tiihonen J, Vauhkonen M, Karhu J, Kupila J, Lansimies E, Farde L. Iodine-123 labeled nor-beta-CIT as a potential tracer for serotonin transporter imaging in the human brain with single-photon emission tomography. Eur J Nucl Med 1998; 25: 19-23.
35. 35. Ferris RM, Brieaddy L, Mehta N, Hollingsworth E, Rigdon G, Wang C, Soroko F, Wastila W, Cooper B. Parmacological properties of 403U76, a new chemical class of 5-hydroxytryptamine-and noradrenaline-reuptake inhibitor. J Pharm Pharmacol 1995; 47: 775-781.
36. 36. Brieaddy LE. Substituted diphenylsulfides as serotonin uptake inhibitors. Patent, WO 93/12080, 1993.
37. 37. Mehta NB, Hollingsworth CE, Brieaddy LE, Cooper BR. Halogen substituted diphenylsulfides. Patent, EP 0 402 097 A1, 1990.
38. 123I] IDAM, 5-iodo-2-((2-((dimethylamino)methyl)phenyl)thio)benzyl alcohol. J Med Chem 1999; 42: 333-335.
39. 39. Kung M-P, Essman WD, Frederick D, Meegalla S, Goodman M, Mu M, Lucki I, Kung HF. IPT: a novel iodinated ligand for the CNS dopamine transporter. Synapse 1995; 20: 316-324.
40. 40. Srebnik M, Ramachandran PV, Brown HC. Chiral synthesis via orbanoboranes. 18 selective reductions, 43 diisopinocampheylchloroborane as an excellent chiral reducing reagent for synthesis of halo alcohols of high enantiomeric purity. A highly enantioselective synthesis of both optical isomers of tomoxetine, fluoxetine and nisoxetine. J Med Chem 1988; 53: 2916-2920.
41. 2 receptor imaging agent. J Nucl Med 1990; 31: 648-654.
42. 42. Gu H, Wall SC, Rudnick G. Stable expression of biogenic amine transporters reveals differences in inhibitor sensitivity, kinetics, and ion dependence. J Biol Chem 1994; 269: 7124-7130.
43. 43. Hou C, Kung MP, Mu M, Kung HF. Evaluation of IPT and Re-TRODAT-1 in cell lines expressing monoamine transporters. [abstract 241.21]. Society for Neuroscience Program 28th Annual Meeting, Los Angeles, CA 1998; 112.
44. 44. Lowry OH, Rosebrough NJ, Farr AL, Randall RJ. Protein measurement with Folin phenol reagent. J Biol Chem 1951; 193: 265-275.
45. 45. Munson PJ, Rodbard D. LIGAND: a versatile computerized approach for characterization of ligand binding system. Anal Biochem 1980; 107: 220-239.
46. 46. Sanders-Bush E, Massari VJ. Actions of drugs that deplete serotonin. Fed Proc 1977; 36: 2149-2153.
47. 47. Kohler C, Ross SB, Srebro B, Ogren S-O. Long-term biochemical and behavioral effects of p-chloroamphetamine in the rat. Ann NY Acad Sci 1978; 305: 645-663.
48. 48. Paxinos G, Watson C. The rat brain in stereotaxic coordinates. New York: Academic Press, 1986.
49. 3H] paroxetine. Neuroscience 1988; 27: 473-496.
50. 3H]cyanoimipramine. Brain Res 1988; 454: 78-88.
51. 3H-paroxetine-labeled serotonin uptake sites in rat brain. Synapse 1987; 1: 488-496.
52. 3H]imipramine localization and relationship to serotonin transporter. J Pharmacol Exp Ther 1990; 252: 410-418.