In vivo evaluation in mice and metabolism in blood of human volunteers of [123I]iodo-PK11195: A possible single-photon emission tomography tracer for visualization of inflammation

European Journal of Nuclear Medicine

Volumn 26, Issue 3, 1999, Pages 194-200

  Dumont, Filip ^a,d   De Vos, Filip ^a   Versijpt, Jan ^b,c   Jansen, Hugo ML ^b   Korf, Jakob ^c   Dierckx, Rudi A ^b   Slegers, Guido ^a  

^a GHENT UNIVERSITY   (Belgium)

^b GHENT UNIVERSITY HOSPITAL   (Belgium)

^c UNIVERSITY MEDICAL CENTER GRONINGEN   (Netherlands)

^d Faculty of Pharmaceutical Sciences   (Belgium)

Author keywords

123I iodo PK11195; Human volunteers; In vivo evaluation; Inflammation; Mice

Indexed keywords

BENZODIAZEPINE RECEPTOR BLOCKING AGENT; IODINE 123; N SEC BUTYL 1 (2 CHLOROPHENYL) N METHYL 3 ISOQUINOLINECARBOXAMIDE; RADIOPHARMACEUTICAL AGENT;

ADULT; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BRAIN; DRUG DISTRIBUTION; DRUG EXCRETION; DRUG METABOLISM; DRUG UPTAKE; FEMALE; HEART; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN EXPERIMENT; INTRAVENOUS DRUG ADMINISTRATION; KIDNEY; LUNG; MALE; MOUSE; NONHUMAN; PHOTON EMISSION TOMOGRAPHY;

ADULT; ANIMALS; ANTINEOPLASTIC AGENTS; FEMALE; HUMANS; INFLAMMATION; IODINE RADIOISOTOPES; ISOQUINOLINES; MALE; MICE; RADIOPHARMACEUTICALS; TISSUE DISTRIBUTION; TOMOGRAPHY, EMISSION-COMPUTED, SINGLE-PHOTON;

EID: 0033030334     PISSN: 03406997     EISSN: None     Source Type: Journal    
DOI: 10.1007/s002590050376     Document Type: Article

References (38)

1. 3H]diazepam binding. Proc Natl Acad Sci USA 1977; 74: 3805-3809.
2. 2. Mohler H, Okada GJ. Benzodiazepine receptors: demonstration in the central nervous system. Science 1977; 198: 849-851.
3. 3. Basile AS, Skolnick P. Subcellular localization of "peripheral-type" binding sites for benzodiazepines in rat brain. J Neurochem 1986; 46: 305-308.
4. 3H]PK11195: anatomical and subcellular distribution. Brain Res Bull 1987; 18: 49-61.
5. 5. Gehlert DR, Yammura HI, Wamsley JK. Autoradiographic location of "peripheral-type" benzodiazepine receptors in the rat brain, heart and kidney. Naunyn-Schmiedebergs Arch Pharmacol 1985; 328: 454-460.
6. 6. Anholt RR, De Souza EB, Oster-Granite ML, Snyder SH. Peripheral-type benzodiazepine receptors: autoradiographic localization in whole-body sections of neonatal rats. J Pharmacol Exp Ther 1985; 233: 517-526.
7. 3H]PK11195 and autoradiographic localization. Arch Int Pharmacodyn Ther 1983; 266: 38-43.
8. 8. De Souza EB, Anholt RR, Murphy KM, Snyder SH, Kuhar MJ. Peripheral-type benzodiazepine receptors in endocrine organs: autoradiographic localization in rat pituitary, adrenal and testis. Endocrinology 1985; 116: 567-573.
9. 9. Richards JG, Mohler H. Benzodiazepine receptors. Neuropharmacology 1984; 23: 233-242.
10. 3H-PK11195, an isoquinoline carboxamide derivative: kinetic studies and autoradiographic localization. J Neurochem 1983; 41: 1744-1750.
11. 11. Syapin PJ, Skolnick P. Characterization of benzodiazepine binding sites in cultured cells of neural origin. J Neurochem 1979; 32: 1047-1051.
12. 12. McCarthy KD, Harden TK. Identification of two benzodiazepine binding sites on cells cultured from rat cerebral cortex. J Pharmacol Exp Ther 1981; 261: 183-191.
13. 13. Bender AS, Hertz L. Flunitrazepam binding to intact and homogenized astrocytes and neurons in primary cells. J Neurochem 1984; 43: 1319-1327.
14. 3H-diazepam binding sites on cultured murine glia and neurons. Brain Res 1984; 316: 1-6.
15. 15. Olson JM, Junk L, Young AB, Penny JB, Mancini WR. Isoquinoline and peripheral-type benzodiazepine binding in gliomas: implications for diagnostic imaging. Cancer Res 1988; 48: 5837-5841.
16. 16. Black KL, Ikezaki K, Santori EM, Backer DP, Vinters HV. Specific high-affinity binding of peripheral benzodiazepine receptor ligands to brain tumors in rat and man. Cancer 1990; 65: 93-97.
17. 17. Itzhak Y, Baker L, Norenberg M. Characterization of the peripheral-type benzodiazepine receptors in cultured astrocytes: evidence for multiplicity. Glia 1993; 9: 211-218.
18. 18. Ruff MR, Pert CG, Weber RJ. Benzodiazepine receptor-mediated chemotaxis of human monocytes. Science 1985; 1281-1283.
19. 19. Zavala F, Lenfant M. Benzodiazepines and PK11195 exert immunomodulating activities by binding on a specific recepetor on macrophages. Ann N Y Acad Sci 1987; 496: 240-249.
20. 20. Fares F, Bar-Ami S, Haj-Yehia Y, Gavish M. Hormonal regulation of peripheral benzodiazepine receptors in femal rat adrenal gland and kidneys. J Recept Res 1989; 9: 143-157.
21. 21. Saano V, Rago L, Raty M. Peripheral benzodiazepine receptors. Pharmacol Ther 1989; 41: 503-514.
22. 22. Verna A, Snyder SH. Peripheral type benzodiazepine receptors. Annu Rev Pharmacol Toxicol 1989; 29: 307-317.
23. 23. Gavish M, Bar-Ami S, Weizman R. The endocrine system and mitochondrial benzodiazepine receptors. Mol Cell Endocrinol 1992; 88: 1-13.
24. 3 site radioligand. Ann Neurol 1988; 24: 708-712.
25. 25. Ramsay SC, Weiler C, Myers R, Cremer JE, Luthra SK, Lammertsma AA, Frackowiak RSJ. Monitoring by PET of macrophage accumulation in brain after ischaemic stroke. Lancet 1992; 339: 1054-1055.
26. 3HRo5-4864 benzodiazepine binding in the kainate lesioned striatum and Huntington's diseased basal ganglia. Brain Res 1982; 248: 396-401.
27. 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: 373-375.
28. 28. McGeer EG, Singh EA, McGeer PH. Peripheral-type benzodiazepine receptor in Alzheimer's disease. Alzheimer Dis Assoc Disord 1988; 2: 331-336.
29. 3 (peripheral type benzodiazepine) radioligand. In: Abstracts of the fifth international conference on AIDS, p 458.
30. 3H]PK11195 to cerebral cortex and peripheral tissues of various species: species differences and heterogeneity in peripheral benzodiazepine binding sites. J Neurochem 1987; 49: 1407-1414.
31. 31. Awad M, Gavish M. Heterogeneity between rat and calf peripheral-type benzodiazepine binding sites: differential sensitivity to Triton X-100. J Recept Res 1989; 9: 369-384.
32. 32. Awad M, Gavish M. Solubilization of peripheral-type benzodiazepine binding sites from cat cerebral cortex. J Neurochem 1989; 52: 1880-1885.
33. 33. Awad M, Gavish M. Species differences and heterogeneity of solubilized peripheral-type benzodiazepine binding sites. Biochem Pharmacol 1989; 38: 3843-3849.
34. 3H]Ro5-4864 in trout and mouse brain membranes. J Neurochem 1989; 53: 494-502.
35. 35. Junck L, Olson JMM, Ciliax BS, Koeppe RA, Watkins GL, Jewett DM, McKeever PE, Wieland DM, Kilbourn MR, Starosta-Rubinstein S, Manoni WR, Kuhl DE, Greenberg HS, Young AB. PET imaging of human gliomas with ligands for the peripheral binding site. Ann Neurol 1989; 26: 752-758.
36. 11C]PK11195 PET-imaging of microglia activation in multiple sclerosis. Neurology 1997; A313.
37. 125I-labeled analog of PK11195, potential agent for SPET imaging of the peripheral benzodiazepine binding site. Nucl Med Biol 1989; 16: 423-429.
38. 3) in heart. Nucl Med Biol 1996; 23: 23-28.