Development of 123I-labelled NNC 13-8241 as a radioligand for SPECT visualization of benzodiazepine receptor binding

Nuclear Medicine and Biology

Volumn 23, Issue 3, 1996, Pages 201-209

  Foged, Christian ^a,b   Halldin, Christer ^a   Hiltunen, Jukka ^c   Braestrup, Claus ^b,d   Thomsen, Christian ^b   Hansen, Holger C ^b   Suhara, Tetsuya ^a   Pauli, Stefan ^a   Swahn, Carl Gunnar ^a   Karlsson, Per ^a   Larsson, Stig ^a   Farde, Lars ^a  

^a KAROLINSKA UNIVERSITY HOSPITAL   (Sweden)

^b NOVO NORDISK A S   (Denmark)

^c MAP Medical Technologies Oy   (Finland)

^d BAYER PHARMA AG   (Germany)

Author keywords

123I,NNC 13 8241; Benzodiazepine; Radioligand; SPECT

Indexed keywords

4 AMINOBUTYRIC ACID A RECEPTOR; BENZODIAZEPINE DERIVATIVE; DIAGNOSTIC AGENT; NNC 13 8241; NNC 13-8241; RADIOACTIVE IODINE; IODINE 123; UNCLASSIFIED DRUG;

ANIMAL; ARTICLE; BRAIN CORTEX; COMPUTER ASSISTED EMISSION TOMOGRAPHY; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; ISOTOPE LABELING; MACACA; MALE; METABOLISM; METHODOLOGY; RADIOASSAY; RAT; SCINTISCANNING; TISSUE DISTRIBUTION; WISTAR RAT; ANIMAL EXPERIMENT; CONTROLLED STUDY; DRUG SYNTHESIS; MONKEY; SINGLE PHOTON EMISSION COMPUTER TOMOGRAPHY;

ANIMALS; BENZODIAZEPINES; CEREBRAL CORTEX; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; IODINE RADIOISOTOPES; ISOTOPE LABELING; MACACA FASCICULARIS; MALE; RADIOLIGAND ASSAY; RATS; RATS, WISTAR; RECEPTORS, GABA-A; TISSUE DISTRIBUTION; TOMOGRAPHY, EMISSION-COMPUTED;

EID: 0029665290     PISSN: 09698051     EISSN: None     Source Type: Journal    
DOI: 10.1016/0969-8051(95)02041-1     Document Type: Article

References (29)

1. Beer H. F., Blauenstein P. A., Hasler P. H., Delaloye B., Riccabona G., Banger I., Hunkeler W., Bonetti E. P., Pieri L., Richards J. G. and Schuhiger P. A. (1990) In vitro and in vivo evaluation of iodine-123-Ro 16-0154: A new imaging agent for SPECT investigations of henzodiazepine receptors. J. Nucl. Med. 31, 1007.
2. Carmann H. and Hunkeler W. (1990) Radioaktiv markierte benzodiazepin derivate. European Patent 0 353 754 A2.
3. Dauth J., Höll K. and Deisenhammer E. (1989) In: Proceedings of the 6th Böttstein colloquim on the use of iomazenil and other brain receptor tracers for SPECT, Roche, Basel, 33-40.
4. Gardner C. R., Tully W. R. and Hedgecock C. J. R. (1993) The rapidly expanding range of neuronal benzodiazepine receptor ligands. Prog. Neurobiol 40, 4-6.
5. 11C]cotinine. Preparation, metabolite studies and in vivo distribution in human brain using PET. Nucl Med. Biol. 19, 871-880.
6. 11C-labelling of its main metabolite Ro 15-3890 for PET studies of BZ receptors. Appl Radiat. Isot. 39, 993-997.
7. Hanson R. N., Tonneson G. L., McLaughlin W. H., Bloomer W. D. and Seitz D. E. (1981) Electrophilic radio iodo destannylation as a new radio iodination method. J. Labelled Comp. Radiopharm. 18, 128-129.
8. Hantraye P., Kaijima M., Prenant C., Giubert B., Sastre J., Crouzel M., Naquet R., Comar D. and Mazière M. (1984) Central type benzodiazepine binding sites: a positron emission tomography study in the baboon's brain. Neurosci. Lett. 48, 115-120.
9. 123I]Ro 16-0154. Eur. J. Pharmacol. 193, 249-252.
10. 125I-Ro 16-0154: Potential probe for SPECT brain imaging. Life Sci. 47, 1535-1546.
11. Kyburz E. (1989) Serendipity in drug discovery. The case of BZR ligands. II Farmaco 44, 345-382.
12. Larsson S. A. (1980) Gamma camera emission tomography. Development and properties of a multi-sectional emission computed tomography system. Acta Radiol. (suppl.) 363, 1-75.
13. Larsson S. A., Bergstrand H., Berg J., Flygare O., Schnell P. O., Andersson N. and Lagergren C. (1984) A special cut-off gamma camera for high resolution SPECT of the head. J. Nucl. Med. 25, 1023-1030.
14. Lassen N. A. (1992) Neuroreceptor quantification in vivo by the steady-state-principle using constant infusion for bolus injection of radioactive tracers. J. Cereb. Blood Flow. Metab. 12, 709.
15. 11C]Ro 15.1788): a specific radioligand for the in vivo study of central BZ receptor by positron emission tomography. Appl. Radiat. Isot. 35, 973-976.
16. McPherson G. A. (1987) KINETIC, EBDA, LlGAND, LOWRY: A collection of radioligand binding analysis programs. Elsvier-BIOSOFT, Cambridge, UK.
17. Müller L., Halldin C., Foged C., Karlsson P., Hall H., Swahn C-G., Suzdak P.D., Hohlweg R., Nielsen E. B. and Farde L. (1994) Preparation of a potential positron emission tomographic radioligand for the dopamine transporter. Eur. J. Nucl. Med. 21, 131-137.
18. 11C-labelled Ro 15-1788 binding to BZ receptors in the human brain by positron emission tomography. J. Psychiatr. Res. 19, 609-622.
19. 11C]Ro 15-1788 binding to the human neocortex using positron emission tomography. Human Psychopharmacology 4, 21-31.
20. 11C]Ro 15-3890; PET study in healthy volunteers. Human Psycopharmacology 4, 215-220.
21. Pike V. W., Halldin C., Crouzel C., Barré L., Nutt D. J., Osman S., Shah F., Turton D. R. and Waters S. L. (1993) Radioligands for PET studies of central BZ receptors and peripheral BZ binding sites - current status. Nucl. Med. Biol. 20, 503-525.
22. 11C]Ro 15-1788, a BZ antagonist, studied in human brain in vivo by positron tomography. Eur. J. Pharmacol. 110, 247-251.
23. Seevers R. H. and Counsell R. E. (1992) Radioiodination techniques for small organic molecules. Chem. Rev. 82, 575-590.
24. Seitz D. E., Tonneson G. L., Hellman S., Hanson R. N, and Adelstein J. S. (1980) Iododestannylation-Position-specific synthesis of iodotamoxifen. J. Organomet. Chem. 186, C33.
25. 11C-labelled dopamine antagonists, raclopride, SCH 23390 and N-methylspiroperidol. Human Psychopharmacology 7, 97-103.
26. 11C]raclopride. J. Labelled Compd. Radiopharm. 32, 284-285.
27. 11C]SCH 23390. Identification of two radiolabelled metabolites with HPLC. Human Psychopharmacology 9, 25-31.
28. Swahn C-G., Persson A. and Pauli S. (1989) Metabolism of the BZ antagonist carbon-11 Ro 15-1788 after intravenous administration in man. Human Psychopharmacology 4, 297-301.
29. 125I-iodotamozifen. Int. J. Appl. Radiat. Isot. 32, 171-173.