Synthesis of a 11C-labelled nitrated 1,4-dihydroquinoxaline-2,3- dione, the NMDA glycine receptor antagonist ACEA 1021 (Licostinel)

Journal of Labelled Compounds and Radiopharmaceuticals

Volumn 41, Issue 4, 1998, Pages 345-353

  Thorell, Jan Olov ^a   Stone Elander, Sharon ^a   Duelfer, Tim ^b   Cai, Sui Xiong ^c   Jones, Lawrence ^b   Pfefferkorn, Heidi ^b   Ciszewska, Grazyna ^b  

^a KAROLINSKA UNIVERSITY HOSPITAL   (Sweden)

^b NOVARTIS PHARMA AG   (Switzerland)

^c Department of Pharmacokinetics and Drug Metabolism   (United States)

Author keywords

1,4 dihydroquinoxaline 2,3 dione; ACEA 1021; Carbon 11; Glycine site; NMDA; PET

Indexed keywords

AMINES; BINDING SITES; CARBON; CYCLIZATION; LIQUID CHROMATOGRAPHY; NITRATION; NITRIC ACID; OXALIC ACID; SYNTHESIS (CHEMICAL);

1,4-DIHYDROQUINOXALINE-2,3-DIONE; ACEA 1021; CARBON-11; GLYCINE RECEPTOR; GLYCINE SITE; IN-VIVO; NMDA; NMDA RECEPTOR; PHENYLENEDIAMINES; RECEPTOR ANTAGONISTS;

AMINO ACIDS;

1,4 DIHYDROQUINOXALINE 2,3 DIONE; 6,7 DICHLORO 1,4 DIHYDROQUINOXALINE 2,3 DIONE; 6,7 DICHLORO 5 NITRO 2,3 QUINOXALINEDIONE; CARBON 11; GLYCINE RECEPTOR ANTAGONIST; N METHYL DEXTRO ASPARTIC ACID RECEPTOR BLOCKING AGENT; NITRIC ACID; QUINOXALINE DERIVATIVE; SULFURIC ACID; UNCLASSIFIED DRUG;

ARTICLE; CYCLIZATION; DRUG STRUCTURE; DRUG SYNTHESIS;

EID: 0031967910     PISSN: 03624803     EISSN: None     Source Type: Journal    
DOI: 10.1002/(SICI)1099-1344(199804)41:4<345::AID-JLCR87>3.0.CO;2-S     Document Type: Article

References (18)

1. The NMDA receptor. Eds: J.C. Watkins and G.L. Collingridge. Oxford University Press, Oxford (1989)
2. Leeson P.D. and Iversen L.L. - J. Med. Chem. 37: 4053 (1994)
3. Honore T., Davies S.N., Drejer J., Fletcher E.J., Jacobsen P., Lodge D. and Nielsen F.E. - Science 241: 701 (1988)
4. Kessler M., Baudry M. and Lynch G.- Brain Res. 489: 377 (1989)
5. Woodward R.M., Huettner J.E., Guastella J., Keana J.F.W. and Weber E. - Mol. Pharmacol. 47: 568 (1995)
6. Keana J.F.W., Kher S.M., Cai S.X., Dinsmore C.M., Glenn A.G., Guastella J., Huang J.C., Ilyin V., Lü Y., Mouser P.L., Woodward R.M. and Weber E.- J. Med. Chem. 38: 4367 (1995)
7. Woodward R.M, Huettner J.E., Guastella J. and Weber E.- Soc. Neurosci. Abstr. 19 (Part 1): 296.14. (1993)
8. Warner D.S., Martin H., Ludwig P., McAllister A., Keana J.F.W. and Weber E. - J. Cerebr. Blood Flow Metabol. 15: 188 (1995)
9. McFarlane C., Warner D.S., Nader A. and Dexter F. - Anesthesiology 82: 963 (1995)
10. Martin H., Warner D.S. and Todd M.M. - Neurosci. Lett. 180: 285 (1994)
11. Matsumoto R.R., Nguyen D. and Truong D.D. - Eur. J. Pharmacol. 275: 117 (1995)
12. Thorell J.-O., Stone-Elander S., Ingvar M., Duelfer T., Jones L., Pfefferkorn H., Ciszewska G., Cai S.X. - Proceedings, XIIth Int. Symp. Radiopharm. Chem., Uppsala, Sweden (1997)
13. Thorell J-O., Stone-Elander S. and Elander N. - J. Label. Compds. Radiopharm. 33: 995 (1993).
14. Thorell J.-O., Stone-Elander S., Ingvar M. and Eriksson L. - J. Label. Compds. Radiopharm. 36: 251 (1995)
15. Nyhammer T. and Grivas S. - Acta Chem. Scand. B40: 583 (1986)
16. Tian W. and Grivas S. - J. Heterocyclic Chem. 22: 1305 (1992)
17. Cai S.X., Kher S.M., Zhou Z-L, Ilyin V., Espitia S.A., Tran M., Hawkinson J.E., Woodward R.M., Weber E. and Keana J.F.W. J. Med. Chem. 40: 730 (1997)
18. Stone-Elander S., Elander N., Thorell J-O., Solås G. and Svennebrink J. J. Label. Compds Radiopharm. 34: 949 (1994)