Nuclear Medicine and Biology
Volume 33, Issue 3 , Pages 317-323 , April 2006

Inhibition of serotonin transport by (+)McN5652 is noncompetitive

  • René Hummerich

      Affiliations

    • Biochemical Laboratory, Central Institute of Mental Health, 68159 Mannheim, Germany
    • ,
  • Oliver Schulze

      Affiliations

    • Department of Nuclear Medicine, University Medical Center Hamburg-Eppendorf, D–20246 Hamburg, Germany
    • ,
  • Thomas Rädler

      Affiliations

    • Department of Psychiatry and Psychotherapy, University Medical Center Hamburg-Eppendorf, D-20246 Hamburg, Germany
    • ,
  • Pal Mikecz

      Affiliations

    • Department of Nuclear Medicine, University Medical Center Hamburg-Eppendorf, D–20246 Hamburg, Germany
    • ,
  • Matthias Reimold

      Affiliations

    • Department of Nuclear Medicine, University Hospital Tübingen, D-72076 Tübingen, Germany
    • ,
  • Winfried Brenner

      Affiliations

    • Department of Nuclear Medicine, University Medical Center Hamburg-Eppendorf, D–20246 Hamburg, Germany
    • ,
  • Malte Clausen

      Affiliations

    • Department of Nuclear Medicine, University Medical Center Hamburg-Eppendorf, D–20246 Hamburg, Germany
    • ,
  • Patrick Schloss

      Affiliations

    • Biochemical Laboratory, Central Institute of Mental Health, 68159 Mannheim, Germany
    • ,
  • Ralph Buchert

      Affiliations

    • Department of Nuclear Medicine, University Medical Center Hamburg-Eppendorf, D–20246 Hamburg, Germany
    • Corresponding Author InformationCorresponding author. Tel.: +49 40 42803 6106; fax: +49 40 42803 5181.

Received 20 September 2005 ,Revised 14 December 2005 ,Accepted 14 December 2005.

References 

  1. Myhrer T. Neurotransmitter systems involved in learning and memory in the rat: a meta-analysis based on studies of four behavioral tasks. Brain Res Brain Res Rev. 2003;41:268–287
  2. Meltzer HY, Lowy MT. The serotonin hypothesis of depression. Psychopharmacology. In:  Meltzer HY editors. The third generation of progress. NY: Raven Press; 1987;p. 513–526
  3. Schloss P, Henn FA. New insights into the mechanisms of antidepressant therapy. Pharmacol Ther. 2004;102:47–60
  4. Sur C, Betz H, Schloss P. Immunocytochemical detection of the serotonin transporter in rat brain. Neuroscience. 1996;73:217–231
  5. Laruelle M, Baldwin RM, Malison RT, Zea-Ponce Y, Zoghbi SS, al-Tikriti MS, et al. SPECT imaging of dopamine and serotonin transporters with [123I]beta-CIT: pharmacological characterization of brain uptake in nonhuman primates. Synapse. 1993;13:295–309
  6. Brucke T, Kornhuber J, Angelberger P, Asenbaum S, Frassine H, Podreka I. SPECT imaging of dopamine and serotonin transporters with [123I]beta-CIT. Binding kinetics in the human brain. J Neural Transm Gen Sect. 1993;94:137–146
  7. Coenen HH, Dutschka K, Müller SP, Geworski L, Farahati J, Reiners C. N.c.a. radiosynthesis of [123,124I]?-CIT, plasma analysis and pharmacokinetic studies with SPECT and PET. Nucl Med Biol. 1995;22:977–984
  8. Okada T, Fujita M, Shimada S, Sato K, Schloss P, Watanabe Y, et al. Assessment of affinities of beta-CIT, beta-CIT-FE, and beta-CIT-FP for monoamine transporters permanently expressed in cell lines. Nucl Med Biol. 1998;25:53–58
  9. Pirker W, Asenbaum S, Hauk M, Kandlhofer S, Tauscher J, Willeit M, et al. Imaging serotonin and dopamine transporters with 123I-beta-CIT SPECT: binding kinetics and effects of normal aging. J Nucl Med. 2000;41:36–44
  10. 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
  11. Szabo Z, Kao PF, Marenco S, Suehiro M, Ravert HT, Mathews WB, et al. Imaging 5-Ht transporter sites in human brain with C-11 Mcn5652. J Nucl Med. 1994;35:P85
  12. Suehiro M, Musachio JL, Dannals RF, Mathews WB, Ravert HT, Scheffel U, et al. An improved method for the synthesis of radiolabeled McN5652 via thioester precursors. Nucl Med Biol. 1995;22:543–545
  13. Parsey RV, Simpson N, Hwang DR, Silfstein M, Mawlawi O, Kegeles LS, et al. Kinetic modeling of C-11 McN5652, a serotonin transporter radioligand, in human volunteers. J Nucl Med. 1999;40:28P–29P
  14. Wilson AA, Ginovart N, Schmidt M, Meyer JH, Threlkeld PG, Houle S. Novel radiotracers for imaging the serotonin transporter by positron emission tomography: synthesis, radiosynthesis, and in vitro and ex vivo evaluation of (11)C-labeled 2-(phenylthio)araalkylamines. J Med Chem. 2000;43:3103–3110
  15. Houle S, Ginovart N, Hussey D, Meyer JH, Wilson AA. Imaging the serotonin transporter with positron emission tomography: initial human studies with [11C]DAPP and [11C]DASB. Eur J Nucl Med. 2000;27:1719–1722
  16. Wilson AA, Ginovart N, Hussey D, Meyer J, Houle S. In vitro and in vivo characterisation of [11C]-DASB: a probe for in vivo measurements of the serotonin transporter by positron emission tomography. Nucl Med Biol. 2002;29:509–515
  17. Belanger MJ, Simpson NR, Wang T, Van Heertum RL, Mann JJ, Parsey RV. Biodistribution and radiation dosimetry of [11C]DASB in baboons. Nucl Med Biol. 2004;31:1097–1102
  18. Heinz A, Jones DW, Zajicek K, Gorey JG, Juckel G, Higley JD, et al. Depletion and restoration of endogenous monoamines affects beta-CIT binding to serotonin but not dopamine transporters in non-human primates. J Neural Transm Suppl. 2004;29–38
  19. Pogarell O, Hamann C, Popperl G, Juckel G, Chouker M, Zaudig M, et al. Elevated brain serotonin transporter availability in patients with obsessive-compulsive disorder. Biol Psychiatry. 2003;54:1406–1413
  20. Stengler-Wenzke K, Muller U, Angermeyer MC, Sabri O, Hesse S. Reduced serotonin transporter-availability in obsessive-compulsive disorder (OCD). Eur Arch Psychiatry Clin Neurosci. 2004;254:252–255
  21. Hummerich R, Reischl G, Ehrlichmann W, Machulla HJ, Heinz A, Schloss P. DASB — in vitro binding characteristics on human recombinant monoamine transporters with regard to its potential as positron emission tomography (PET) tracer. J Neurochem. 2004;90:1218–1226
  22. Bell C, Abrams J, Nutt D. Tryptophan depletion and its implications for psychiatry. Br J Psychiatry. 2001;178:399–405
  23. Milak MS, Ogden RT, Vinocur DN, Van R, Heertum L, Cooper TB, et al. Effects of tryptophan depletion on the binding of [11C]-DASB to the serotonin transporter in baboons: response to acute serotonin deficiency. Biol Psychiatry. 2005;57:102–106
  24. Laruelle M. Imaging synaptic neurotransmission with in vivo binding competition techniques: a critical review. J Cereb Blood Flow Metab. 2000;20:423–451
  25. Lundquist P, Wilking H, Hoglund AU, Sandell J, Bergstrom M, Hartvig P, et al. Potential of [(11)C]DASB for measuring endogenous serotonin with PET: binding studies. Nucl Med Biol. 2005;32:129–136
  26. Huang Y, Hwang DR, Narendran R, Sudo Y, Chatterjee R, Bae SA, et al. 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. J Cereb Blood Flow Metab. 2002;22:1377–1398
  27. Frankle WG, Huang Y, Hwang D-R, Talbot PS, Slifstein M, Van Heertum R, et al. Comparative evaluation of serotonin transporter radioligands 11C-DASB and 11C-McN 5652 in healthy humans. J Nucl Med. 2004;45:682–694
  28. Szabo Z, McCann UD, Wilson AA, Scheffel U, Owonikoko T, Mathews WB, et al. Comparison of (+)-C-11-McN5652 and C-11-DASB as serotonin transporter radioligands under various experimental conditions. J Nucl Med. 2002;43:678–692
  29. McCann UD, Szabo Z, Seckin E, Rosenblatt P, Mathews WB, Ravert HT, et al. Quantitative PET studies of the serotonin transporter in MDMA users and controls using [(11)C]McN5652 and [(11)C]DASB. Neuropsychopharmacology. 2005;30:1741–1750
  30. Buchert R, Thomasius R, Nebeling B, Petersen K, Obrocki J, Jenicke L, et al. Long-term effects of “ecstasy” use on serotonin transporters of the brain investigated by PET. J Nucl Med. 2003;44:375–384
  31. Suhara T, Takano A, Sudo Y, Ichimiya T, Inoue M, Yasuno F, et al. High levels of serotonin transporter occupancy with low-dose clomipramine in comparative occupancy study with fluvoxamine using positron emission tomography. Arch Gen Psychiatry. 2003;60:386–391
  32. Szabo Z, Owonikoko T, Peyrot M, Varga J, Mathews WB, Ravert HT, et al. Positron emission tomography imaging of the serotonin transporter in subjects with a history of alcoholism. Biol Psychiatry. 2004;55:766–771
  33. Reivich M, Amsterdam JD, Brunswick DJ, Shiue CY. PET brain imaging with C-11 (+)McN5652 shows increased serotonin transporter availability in major depression. J Affect Disord. 2004;82:321–327
  34. Parsey RV, Castrillon J, Mann JJ. Effects of tryptophan depletion on 11C McN5652 binding in baboons. Neuroimage. 2002;16:S20
  35. Maryanoff BE, McComsey DF, Gardocki JF, Shank RP, Costanzo MJ, Nortey SO, et al. Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships. J Med Chem. 1987;30:1433–1454
  36. Shank RP, Vaught JL, Pelley KA, Setler PE, McComsey DF, Maryanoff BE. McN-5652: a highly potent inhibitor of serotonin uptake. J Pharmacol Exp Ther. 1988;247:1032–1038
  37. Suehiro M, Scheffel U, Ravert HT, Dannals RF, Wagner HN. C-11 (+)Mcn5652 as a radiotracer for imaging serotonin uptake sites with Pet. Life Sci. 1993;53:883–892
  38. Schulze O, Schmidt U, Voss J, Nebeling B, Adiwidjaja G, Scharwachter K. The structure of McN-5652. Bioorg Med Chem. 2001;9:2105–2111
  39. Sur C, Betz H, Schloss P. Distinct effects of imipramine on 5-hydroxytryptamine uptake mediated by the recombinant rat serotonin transporter SERT1. J Neurochem. 1998;70:2545–2553
  40. Elfving B, Bjornholm B, Ebert B, Knudsen GM. Binding characteristics of selective serotonin reuptake inhibitors with relation to emission tomography studies. Synapse. 2001;41:203–211
  41. Fomby TB, Hill RC, Johnson SR. Advanced econometric methods. NY: Springer; 1984;
  42. Swofford DL, Olsen GJ, Waddell PJ, Hillis DM. Phylogenetic inference. In:  Hillis DM,  Moritz C,  Mable BK editor. Molecular systematics. Sunderland: Sinauer Associates; 1996;p. 407–543
  43. Lazareno S, Birdsall NJ. Estimation of competitive antagonist affinity from functional inhibition curves using the Gaddum. Schild and Cheng-Prusoff equations. Br J Pharmacol. 1993;109:1110–1119
  44. O'Riordan C, Phillips OM, Williams DC. Two affinity states for [3H]imipramine binding to the human platelet 5-hydroxytryptamine carrier: an explanation for the allosteric interaction between 5-hydroxytryptamine and imipramine. J Neurochem. 1990;54:1275–1280

PII: S0969-8051(05)00305-7

doi: 10.1016/j.nucmedbio.2005.12.009

Nuclear Medicine and Biology
Volume 33, Issue 3 , Pages 317-323 , April 2006

Article Tools

* Image Usage & Resolution