Nuklearmedizin 1992; 31(01): 29-31
DOI: 10.1055/s-0038-1629596
Originalarbeiten
Schattauer GmbH

Ergebnisse von Verdrängungsuntersuchungen an Benzodiazepin-Rezeptoren (123J-Jomazenil und Flumazenil)

Results of Displacement Studies of Benzodiazepine Receptors (123I-Jomazenil and Flumazenil)
K. Buchali
1   Aus der Nuklearmedizinischen Klinik der Charité, Humboldt-Universität Berlin, FRG
› Author Affiliations
Further Information

Publication History

Eingegangen: 09 October 1991

in revidierter Form: 14 November 1991

Publication Date:
05 February 2018 (online)

Zusammenfassung

Bei 14 Patienten mit hepatischer Enzephalopathie wurden SPECT-Unter- suchungen mit 123J-Jomazenil durchgeführt. Der spontane Abfall der Aktivitätskonzentration im Gehirn innerhalb 80 min betrug zwischen 10 und 20%, im Nasenbereich 35%. Nach Injektion von 0,1 bis 0,5 mg Flumazenil wurden innerhalb 20 min bzw. bei Zweitinjektion 29 bis 38% ausgeschwemmt. Eine vergleichbare Ausschwemmung erfolgte in der weißen Substanz und im Nasenbereich. Die Anwendung bekannter Modelle der Rezeptorkinetik war dadurch nicht möglich.

Summary

SPECT studies with 123I-Jomazenil were performed in 14 patients with hepatic encephalopathy. The activity concentration in the brain decreases spontaneously by 10 to 20% within 80 min, in the nasal tissue by 35%. After an i.v. injection of 0.1 to 0.5 mg Flumazenil a decrease of 29 to 38% is observed within 20 min, with a comparable decrease in white matter and nasal tissue. The application of well-known models of receptor kinetics is therefore impossible.

 
  • LITERATUR

  • 1 Baraldi M, Zandi P, Zeneroli ML. Hepatic encephalopathy: neurochemical mechanisms and new treatments. In: GABA and benzodiazepine receptor subtypes. Biggio G, Costa E. eds. New York: Raven Press; 1990
  • 2 Basile AS, Ostrowski NL, Gammal SH, Jones EA, Skolnick P. The involvement of the benzodiazepine receptor in hepatic encephalopathy: evidence for the presence of a benzodiazepine receptor ligand. In: GABA and benzodiazepine receptor subtypes. Biggio G, Costa E. eds. New York: Raven Press; 1990
  • 3 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 SPECT investigations of benzodiazepine receptors. J Nucl Med 1990; 31: 1007-10.
  • 4 Eckelman WC, Reba RC, Gibson RE. et al. Receptor binding radiotracers: a class of potential radiopharmaceuticals. J Nucl Med 1979; 20: 350-7.
  • 5 Farde L, Hall H, Ehrin E, Sedvall G. Quantitative analysis of D2 dopamine receptor binding in the living human brain by PET. Science 1986; 231: 258-61.
  • 6 Grimm G, Ferenci P, Katzenschlager R. et al. Improvement of hepatic encephalopathy treated with flumazenil. Lancet 1988; ii: 1392-4.
  • 7 Hantraye P, Kaijima M, Prenant C. et al. Central type benzodiazepine binding sites: a positron emission tomographic study in the baboon’s brain. Neurosci Lett 1984; 48: 115-20.
  • 8 Hoell K, Deisenhammer E, Dauth J. et al. SPECT mapping of human brain benzodiazepine receptors. J Nucl Med 1988; 29: 759.
  • 9 Huang SC, Barrio JR, Phelps ME. Neuroreceptor assay with positron emission tomography: equilibrium versus dynamic approaches. J Cerebr Blood Flow Metab 1986; 06: 515-21.
  • 10 Owen F, Poulter M, Waddington JL, Marshal RD, Crow TJ. [3H] RO 5-4864 and [3H] flunitrazepam binding in kainate-lesioned rat striatum and in temporal cortex of brains from patients with senile dementia of the Alzheimer type. Brain Res 1983; 278: 373-5.
  • 11 Richards JG, Möhler H. Benzodiazepine receptors. Neuropharmacol 1984; 23: 233-42.
  • 12 Samson Y, Hantraye P, Baron JC. et al. Kinetics and displacement of [11C] RO 151788, a benzodiazepine antagonist, studied in human brain in vivo by positron tomography. Eur J Pharmacol 1985; 110: 247-51.
  • 13 Sherwin A, Matthew E, Blain M, Guévremont D. Benzodiazepine receptor binding is not altered in human epileptogenic cortical foci. Neurology 1986; 36: 1380-2.
  • 14 Shinoteh H, Yamasaki T, Inone O. et al. Visualization of specific binding sites of benzodiazepine in human brain. J Nucl Med 1986; 27: 1593-9.
  • 15 Verhoeff NPLG, van Royen EA, Overweg J, Limburg M. A kinetic analysis of the binding of 1-123 iomazenil to central benzodiazepine receptors in healthy volunteers. Eur J Nucl Med 1991; 18: 537.
  • 16 Wong DF, Gjedde A, Wagner HN. Quantification of neuroreceptors in the living human brain. I. Irreversible binding of ligands. J Cerebr Blood flow Metab 1986; 06: 137-46.
  • 17 Koeppe RA, Holthoff VA, Frey KA, Kilbourn MR, Kuhl DE. Compartmental analysis of [11C]flumazenil kinetics for the estimation of ligand transport rate and receptor distribution using positron emission tomography. J Cerebr Blood Flow Metab 1991; 11: 34-44.