Brain SPET with Drug Receptors

Part of the Developments in Nuclear Medicine book series (DNUM, volume 25)


The number of radiopharmaceuticals which are used for receptor imaging with PET -and more recently also with SPET -has increased dramatically. The term “receptor-PET” or “receptor-SPET” is not completely correct because the definition of a receptor includes the linkage of a specific binding with the effect on chemical or electrical phenomena within the cell. These chemical/electrical phenomena cannot be visualized by means of the “non-invasive” imaging procedures like PET and SPET.


Multiple System Atrophy Temporal Lobe Epilepsy Single Photon Emission Tomography Receptor Imaging Brain SPECT 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.


Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.


  1. 1.
    Nolte J. The human brain. An introduction to its functional anatomy. 3rd ed. St. Louis: Mosby Year Book, 1992:414–24.Google Scholar
  2. 2.
    Verhoeff NPLG. Pharmacological implications for neuroreceptor imaging. Eur J Nucl Med 1991;18:482–502.PubMedCrossRefGoogle Scholar
  3. 3.
    Maziere B, Maziere M. Where have we got to with neuroreceptor mapping of the human brain? Eur J Nucl Med 1990;16:817–35.PubMedCrossRefGoogle Scholar
  4. 4.
    Stöcklin G. Tracers for metabolic imaging of brain and heart. Eur J Nucl Med 1992;19:527–51.PubMedCrossRefGoogle Scholar
  5. 5.
    Prevett MC, Lammertsma AA, Duncan JS et al. Central benzodiazepine receptor (BZR) quantitation in normal subjects and in primary generalised epilepsy (PGE). J Cereb Blood Flow Metab 1993;13 (Suppl 1):277.Google Scholar
  6. 6.
    Black KL, Ikezaki K, Toga AW. Imaging of brain tumours using peripheral benzodiazepine receptor ligands. J Neurosurg 1989;71:113–8.PubMedCrossRefGoogle Scholar
  7. 7.
    Pappata S, Levasseur M, Samson Y et al. Thalamic and peri-infarct 11C-PK11195 uptake in patients with chronic middle cerebral artery infarcts: a PET study. J Cereb Blood Flow Metab 1993;13 (Suppl 1):346.Google Scholar
  8. 8.
    Shinoto H, Yamasaki T, Inoue O et al. Visualization of specific binding sites of benzodiazepine in human brain. J Nucl Med 1986;27:1593–99.Google Scholar
  9. 9.
    Beer HF, Bläuenstein PA, Hasler PH et al. In vitro and in vivo evaluation of iodine-123-Ro 16–0154: a new imaging agent for SPET investigations of benzodiazepine receptors. J Nucl Med 1990;31:1007–14.PubMedGoogle Scholar
  10. 10.
    Innis RB, Al-Tikriti MS, Zoghbi SS et al. SPET imaging of the benzodiazepinereceptor: feasibility of in vivo potency measurements from stepwise displacement curves. J Nucl Med 1991;32:1754–61.PubMedGoogle Scholar
  11. 11.
    Bartenstein P, Ludolph A, Schober O et al. Benzodiazepine receptors and cerebral blood flow in partial epilepsy. Eur J Nucl Med 1991;18:111–8.PubMedCrossRefGoogle Scholar
  12. 12.
    Kopp J. Apparativ-methodische Grundlagen der Emissions-Computertomographie des ZNS. Nuklearmediziner 1993;16:95–8.Google Scholar
  13. 13.
    Savic I, Persson A, Roland P, Pauli S, Sedvall G, Widen L. In vivo demonstration of reduced benzodiazepine receptor binding in human epileptic foci. Lancet 1988;ii:863–6.CrossRefGoogle Scholar
  14. 14.
    Grünwald F, Hufnagel A, Elger CE, Biersack HJ. Single-Photon-Emis-sionscomputertomographie (SPET) in der Epilepsiediagnostik. Radiologe 1993;33:198–203.PubMedGoogle Scholar
  15. 15.
    Johnson EW, de Lanerolle NC, Kim JH et al. “Central” and “peripheral” benzodiazepine receptors: opposite changes in human epileptogenic tissue. Neurology 1992;42:811–5.PubMedCrossRefGoogle Scholar
  16. 16.
    Hierholzer J, Keske U, Ferstl F et al. Benzodiazepine receptor imaging in patients with epileptic seizures. Eur J Nucl Med 1991; 18:599.Google Scholar
  17. 17.
    Schläpfer TE, Schulthess GK, Schubiger PA, Rösler H, Fisch HU. Relation between hepatic function and wash-out of I-123 iomazenil after displacement with flumazenil from the brain. Eur J Nucl Med 1991; 18:614.Google Scholar
  18. 18.
    Feistel H, Kaschka WP, Ebert D, Joraschky P, Wolf F. Assessment of cerebral benzodiazepine receptor distribution in anxiety disorders -a study with I-123-Iomazenil. J Nucl Med 1993;34:47.Google Scholar
  19. 19.
    Horn R, Miretzky A, Grünwald F, Biersack HJ, Möller HJ. Iomazenil und HMPAO-SPET Untersuchungen bei Patienten mit einem Paniksyndrom. Fortschr Neurol Psychiat 1992;60:105.Google Scholar
  20. 20.
    Steinert H, Wetzel H, Schlegel S et al. SPET imaging of the benzodiazepine receptor occupancy in relation to benzodiazepine medication. J Nucl Med 1992;33:887.Google Scholar
  21. 21.
    Verhoeff NPLG. Neuroreceptor ligand imaging by single photon emission computerised tomography (SPET) [dissertation]. Amsterdam (The Netherlands): Univ. of Amsterdam, 1993.Google Scholar
  22. 22.
    Gottfries CG. Psychopharmakologie -Grundlagen. In: Kisker KP, Lauter H, Meyer JE, Müller C, Strömgren E (eds.). Psychiatrie der Gegenwart,Bd.4, 357–87, Springer Verlag 1987.Google Scholar
  23. 23.
    Cooper JR, Bloom FE, Roth RH. The biochemical basis of neuropharmacology. 6th ed. Oxford University Press 1991Google Scholar
  24. 24.
    Sibley DR, Monsma FJ. Molecular biology of dopamine receptors. Trends Pharmacol Sci 1992;13:61–9.PubMedCrossRefGoogle Scholar
  25. 25.
    Stoof JC, Kebabian JW. Opposing roles for D1 and D2 dopamine receptors in efflux of cyclic AMP from rat neostriatum. Nature 1981;294:366–8.PubMedCrossRefGoogle Scholar
  26. 26.
    Brücke T, Podreka I, Angelberger P, et al. Dopamine D2 receptor imaging with SPET: Studies in different neuropsychiatric disorders. J Cerebr Blood Flow Metabol 1991;11:220–8.CrossRefGoogle Scholar
  27. 27.
    Verhoeff NPLG, van Royen EA, Speelman JD, Borm JJJ, Kapucu O. Differential diagnosis of parkinsonism by I-123 IBZM SPET. J Nucl Med 1992;33:917.Google Scholar
  28. 28.
    Schwarz J, Tatsch K, Arnold G, et al. I-123-iodobenzamide-SPET predicts dopaminergic responsiveness in patients with de novo parkinsonism. Neurology 1992;42:556–61.PubMedCrossRefGoogle Scholar
  29. 29.
    Verhoeff NPLG, Speelman JD, van Royen EA, de Jong JMBV. In vivo dopamine D2-receptors imaging with I-123 iodobenzamide SPET in patients with multiple system atrophy. Eur J Nucl Med 1990; 16:520.Google Scholar
  30. 30.
    Tatsch K, Schwarz J, Oertel WH, Kirsch CM. SPET imaging of dopamine D2 receptors with I-123-IBZM:initial experience in controls and patients with Parkinson’s syndrome and Wilson’s disease. Nucl Med Comm 1991;12:699–707.CrossRefGoogle Scholar
  31. 31.
    Tatsch K, Schwarz J, Kirsch CM. ZNS-SPET: Rezeptorszintigraphie mit 123J-IBZM und 123J-Iomazenil. Nuklearmediziner 1993;16:143–50.Google Scholar
  32. 32.
    Davidson MD, Harvey PD, Bergmann RL, et al. Effects of the D-1 antagonist SKF-38393 combined with haloperidol in schizophrenic patients. Arch Gen Psychiatry 1990;47:190–1.PubMedCrossRefGoogle Scholar
  33. 33.
    Mozley PD, Zhu X, Kung HF, Selikson MH, et al. The dosimetry of iodine-123-labeled TISCH: A SPET Imaging agent for the D1 Dopamine receptor. J Nucl Med 1993;34:208–13.PubMedGoogle Scholar
  34. 34.
    Kung HF, Pan S, Kung MP, Billings J, et al. In vitro and in vivo evaluation of [I-123] IBZM: A potential CNS D-2 dopamine receptor imaging agent. J Nucl Med 1989;30:88–92.PubMedGoogle Scholar
  35. 35.
    Kung HF, Alavi A, Chang W, Kung MP, et al. In vivo SPET imaging of CNS D-2 dopamine receptors: Initial studies with Iodine-123-IBZM in humans. J Nucl Med 1990;31:773–9.Google Scholar
  36. 36.
    Seibyl JP, Woods SW, Zoghbi SS, et al. Dynamic SPET imaging of dopamine D2 receptors in human subjects with iodine-123-IBZM. J Nucl Med 1992;33:1964–71.PubMedGoogle Scholar
  37. 37.
    Cordes M, Henkes H, Laudahn D, et al. Initial experience with SPET examinations using [I-123] IBZM as a D2-dopamine receptor agonist in Parkinson’s disease. Eur J Radiol 1991;12:182–6.PubMedCrossRefGoogle Scholar
  38. 38.
    Mertens J, Bossuyt-Piron C, Bossuyt A, et al. Specific activity: a critical parameter for brain receptor tracers. 2’-I-123-ketanserin as case study. Eur J Nucl Med 1990; 16:540.Google Scholar
  39. 39.
    D’haenen H, Bossuyt A, Mertens J, et al. SPET imaging of serotonin2 receptors in depression. Psychiat Res 1992;45:227–37.CrossRefGoogle Scholar
  40. 40.
    Eckelman WC, Reba RC, Rzeszotarski WJ et al. External imaging of cerebral muscarinic acetylcholine receptors. Science 1984;223:291–2.PubMedCrossRefGoogle Scholar
  41. 41.
    Vaugeois JM, Patterson J, Wyper DJ, et al. In vivo and in vitro binding kinetics of I-123-QNB in the normal human brain. J Cereb Blood Flow Metab 1993;13 (Suppl 1):296.Google Scholar
  42. 42.
    Holman BL, Gibson RE, Hill Tc99m, et al. Muscarinic acetylcholine receptors in Alzheimer’s disease: in vivo imaging with iodine-123-labeled 3-quinuclidinyl-4-iodobenzylate and emission tomography. JAMA 1985;254:3063.PubMedCrossRefGoogle Scholar
  43. 43.
    Weinberger DR, Gibson R, Coppola R et al. The distribution of cerebral muscarinic acetylcholine receptors in vivo in patients with dementia. A controlled study with 123-IQNB and single photon emission computed tomography. Arch Neurol 1991;48:169–76.PubMedCrossRefGoogle Scholar
  44. 44.
    Wyper DJ, Brown D, Patterson J et al. Deficits in iodine-labelled 3-quinuclidinyl benzilate binding in relation to cerebral blood flow in patients with Alzheimer’s disease. Eur J Nucl Med 1993;20:379–86.PubMedCrossRefGoogle Scholar
  45. 45.
    Müller-Gärtner HW, Wilson AA, Dannals RF, Wagner HN, Frost JJ. Imaging muscarinic cholinergic receptors in human brain in vivo with SPET,[I-123]4-iododexetimide, and [I-123]4-iodolevetimide. J Cereb Blood Flow Metab 1992;12:562–70.PubMedCrossRefGoogle Scholar
  46. 46.
    Müller-Gärtner HW, Fisher RS, Lesser RP et al. Decreased binding of I-123 iododexetimide to muscarinic cholinergic receptors in hippocampus in temporal lobe epilepsy. J Nucl Med 1992;33:829.Google Scholar
  47. 47.
    Som P, Wang GJ, Oster ZH, et al. Wholebody distribution of a new selective muscarinic antagonist: radioiodinated IQNP. J Nucl Med 1993;34:197.Google Scholar
  48. 48.
    Kuhl DE, Koeppe RA, Fessler JA et al. In vivo mapping of cholinergic neurons in the human brain using SPET and (-)-5-I-123-iodobenzovesamicol (IBVM). J Nucl Med 1993;34:25.Google Scholar
  49. 49.
    Brücke T, Roth J, Podreka I, et al. Striatal dopamine D2-receptor blockade by typical and atypical neuroleptics. Lancet 1992;339:497.PubMedCrossRefGoogle Scholar
  50. 50.
    Grünwald F, Danos P, Kasper S, et al. IBZM SPET in psychiatric diseases. In: Höfer R, Bergmann H, and Sinzinger H, editors. Radioactive Isotopes in Clinical Medicine and Research. Stuttgart: Schattauer Verlag, 1993: 122–5.Google Scholar
  51. 51.
    Pilowsky LS, Costa DC, Ell PJ, et al. D2 receptor abnormalities in schizophrenia: A I-123 IBZM single photon emission tomography (SPET) study of drug naive schizophrenic patients. J Cerebr Blood Flow Metabol 1993;13:512.Google Scholar
  52. 52.
    Costa DC, George MS, Ell PJ, Verhoeff NPLG, Robertson MM.. D2 dopamine receptor studies in patients with Gilles de la Tourette syndrome. Eur J Nucl Med 1991;18:561.CrossRefGoogle Scholar
  53. 53.
    Marienhagen J, Schrell U, Ordnung D, et al. Darstellung von Dopamin D2-Rezeptoren in Makroprolaktinomen mit J-123 IBZM-SPET. Nucl Med 1992;31:A81.Google Scholar

Copyright information

© Springer Science+Business Media Dordrecht 1995

Authors and Affiliations

There are no affiliations available

Personalised recommendations