Labeling and evaluation of N-[11C]methylated quinoline-2-carboxamides as potential radioligands for visualization of peripheral benzodiazepine receptors

Journal of Medicinal Chemistry

Volumn 44, Issue 4, 2001, Pages 579-585

  Matarrese, M ^a   Moresco, R M ^a   Cappelli, A ^b   Anzini, M ^c   Vomero, S ^b   Simonelli, P ^a   Verza, E ^a   Magni, F ^a   Sudati, F ^a   Soloviev, D ^a   Todde, S ^a   Carpinelli, A ^a   Kienle, M G ^a   Fazio, F ^a  

^a UNIVERSITY OF MILANO BICOCCA   (Italy)

^b UNIVERSITY OF SIENA   (Italy)

^c UNIVERSITY MAGNA GRAECIA OF CATANZARO   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

3 METHYL 4 (2 FLUOROPHENYL) N (1 METHYLPROPYL)QUINOLINE 2 CARBOXAMIDE; 3 METHYL 4 PHENYL N (PHENYLMETHYL)QUINOLINE 2 CARBOXAMIDE; 3 METHYL N (1 METHYLPROPYL) 4 PHENYLQUINOLINE 2 CARBOXAMIDE; AMIDE; BENZODIAZEPINE RECEPTOR; CARBON 11; METHYL IODIDE; N SEC BUTYL 1 (2 CHLOROPHENYL) N METHYL 3 ISOQUINOLINECARBOXAMIDE; N SEC BUTYL 1 (2 FLUORO 5 NITROPHENYL) N METHYL 3 ISOQUINOLINECARBOXAMIDE; N,N DIMETHYLFORMAMIDE; POTASSIUM HYDROXIDE; QUINOLINE DERIVATIVE; RADIOLIGAND; TETRABUTYLAMMONIUM; TRIFLUOROMETHANESULFONIC ACID; UNCLASSIFIED DRUG;

ADRENAL GLAND; ANIMAL EXPERIMENT; ARTICLE; BRAIN; CONTROLLED STUDY; DRUG STRUCTURE; HEART; ISOTOPE LABELING; KIDNEY; LUNG; MALE; METHYLATION; NONHUMAN; POSITRON EMISSION TOMOGRAPHY; RADIOISOTOPE DISTRIBUTION; RAT; SPLEEN; SYNTHESIS;

AMIDES; ANIMALS; CARBON RADIOISOTOPES; ISOTOPE LABELING; LIGANDS; MALE; METHYLATION; QUINOLINES; RADIOPHARMACEUTICALS; RATS; RECEPTORS, GABA-A; TISSUE DISTRIBUTION; TOMOGRAPHY, EMISSION-COMPUTED;

EID: 0035865790     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm001004h     Document Type: Article

References (38)

1. 3H]diazepam binding
2. Benzodiazepine receptor: Demonstration in the central nervous system
3. A receptor structure and function
4. Limitations of the benzodiazepine receptor nomenclature: A proposal for a pharmacological classification as omega receptor subtypes
5. Peripheral types benzodiazepine receptors
6. Enigma of the peripheral benzodiazepine receptor
7. 3H]PK 11195 and autoradiographic localization
8. Peripheral-type benzodiazepine receptors in endocrine organs: Autoradiographic localization in rat pituitary, adrenal, and testis
9. Peripheral-type benzodiazepine receptors: Autoradiographic localization in whole-body sections of neonatal rats
10. 3H]PK 11195, an isoquinoline carboxamide derivative: Kinetic studies and autoradiographic localisation
11. The peripheral-type benzodiazepine receptor. Localization to the mitochondrial outer membrane
12. Peripheral benzodiazepine binding sites in Alzheimer's disease frontal and temporal cortex
13. Imaging of human brain lesions with an omega3 site radioligand
14. PK 11195 binding to the peripheral benzodiazepine receptor as a marker of microglia activation in multiple sclerosis and experimental autoimmune encephalomyelitis
15. 3]Ro5-4864 benzodiazepine binding in the kainate lesioned striatum and Huntington's diseased basal ganglia
16. 11C](R)-PK 11195 positron emission tomography imaging of activated microglia in vivo in Rasmussen's encephalitis
17. 11C]methyl, N-(methyl-1-propyl), chloro-2-pheny])-1 isoquinoline carboxamide-3 (PK-11195): A new ligand for peripheral benzodiazepine receptors
18. Radioligands for PET studies of central benzodiazepine receptors and PK (peripheral benzodiazepine) binding sites-current status
19. PET imaging of human gliomas with ligands for the peripheral benzodiazepine binding site
20. PET study of carbon-11-PK 11195 binding to peripheral type benzodiazepine sites in glioblastoma: A case report
21. PET imaging of cerebral infarcts using a ligand for the peripheral benzodiazepine binding site
22. Peripheral-type benzodiazepine receptors in the living heart characterized by positron emission tomography
23. 18F]PK 14105 as an alternative radioligand for peripheral type benzodiazepine binding sites
24. Mapping the peripheral benzodiazepine receptor binding site by conformationally restrained derivatives of 1-(2-chlorophenyl)-N-methylpropyl)-3-isoquinolinecarboxamide (PK 11195)
25. 11C]PK 11195 and comparison of their behaviours as radioligands for PK binding sites in rats
26. 11C]PK 11195 to omega3 sites in baboons: Positron Emission Tomography study
27. 3H]PK 14105
28. 3) in heart
29. Synthesis of a hih specific activity 125I-labeled analogue of PK 11195, potential agent for SPECT imaging of the peripheral benzodiazepine binding site
30. Mitochondrial benzodiazepine receptor ligands as indicator of damage in the CNS: Their application in Positron Emission Tomography
31. PET of peripheral benzodiazepine binding sites in the microgliosis of Alzheimer's disease
32. 123I]iodo-PK11195: A possible single-photon emission tomography tracer for visualization of inflammation
33. Chirality of bioactive agents in protein binding storage and transport process
34. Chiral aspects of drug metabolism
35. Synthesis and evaluation of 11C-PK 11195 for in vivo study of peripheral-type benzodiazepine receptors using positron emission tomography
36. 11C]methyl-L-methionine
37. 11C]methyl triflate