Preclinical evaluation of [123I]R93274 as a SPECT radiotracer for imaging 5-HT(2A) receptors

European Journal of Pharmacology

Volumn 321, Issue 3, 1997, Pages 285-293

  Abi Dargham, Anissa ^a,b   Zea Ponce, Yolanda ^a   Terriere, Dirk ^c   Al Tikriti, Mohamed ^a   Baldwin, Ronald M ^a   Hoffer, Paul ^a   Charney, Dennis ^a   Leysen, Josée E ^d   Laruelle, Marc ^a   Mertens, John ^c   Innis, Robert B ^a  

^a YALE UNIVERSITY SCHOOL OF MEDICINE   (United States)

^b New York State Psychiatric Institute ^*  (United States)

^c VRIJE UNIVERSITEIT BRUSSEL   (Belgium)

^d JANSSEN RESEARCH FOUNDATION   (Belgium)

Author keywords

5 HT(2A) receptor; 123I R93274; SPECT (single photon emission computerized tomography)

Indexed keywords

IODINE 123; KETANSERIN; R 93274; RACLOPRIDE; SEROTONIN 2A RECEPTOR; TRACER; UNCLASSIFIED DRUG; BENZAMIDE DERIVATIVE; DIAGNOSTIC AGENT; DOPAMINE RECEPTOR BLOCKING AGENT; N ((3 P FLUOROPHENYL 1 PROPYL) 4 METHYL 4 PIPERIDINYL) 4 AMINO 5 IODO 2 METHOXYBENZAMIDE; N-((3-P-FLUOROPHENYL-1-PROPYL)-4-METHYL-4-PIPERIDINYL)-4-AMINO-5-IODO-2-METHOXYBENZAMIDE; PIPERIDINE DERIVATIVE; RADIOACTIVE IODINE; SALICYLAMIDE DERIVATIVE; SEROTONIN ANTAGONIST; SEROTONIN RECEPTOR;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BABOON; BINDING AFFINITY; BRAIN; BRAIN REGION; CONTROLLED STUDY; DRUG UPTAKE; FEMALE; INTRAVENOUS DRUG ADMINISTRATION; ISOTOPE LABELING; NONHUMAN; PRIORITY JOURNAL; QUANTITATIVE ASSAY; RECEPTOR DENSITY; SINGLE PHOTON EMISSION COMPUTER TOMOGRAPHY; ANIMAL; BLOOD; METABOLISM; PAPIO; SCINTISCANNING;

ANIMALS; BENZAMIDES; BRAIN; DOPAMINE ANTAGONISTS; FEMALE; IODINE RADIOISOTOPES; KETANSERIN; PAPIO; PIPERIDINES; RACLOPRIDE; RECEPTOR, SEROTONIN, 5-HT2A; RECEPTORS, SEROTONIN; SALICYLAMIDES; SEROTONIN ANTAGONISTS; TOMOGRAPHY, EMISSION-COMPUTED, SINGLE-PHOTON;

EID: 0030610290     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0014-2999(96)00906-5     Document Type: Article

References (49)

1. Aghajanian, G.K., 1994, Serotonin and the action of LSD in the brain, Psychiatr. Ann. 24, 137.
2. 2 binding sites in the frontal cortex of suicide victims and control subjects, Am. J. Psychiatry 146, 730.
3. 2) receptor binding in frontal cortex of schizophrenic patients, J. Neural Transm. 85, 19.
4. 123I]β-CIT) in nonhuman primates: pharmacokinetics, biodistribution and SPECT imaging coregistered with MRI, Nucl. Med. Biol. 20, 597.
5. Bennett, J.P., S.J. Enna, D.B. Bylund, J.C. Gillin, R.J. Wyatt and S.H. Snyder, 1979, Neurotransmitter receptors in frontal cortex of schizophrenics, Arch. Gen. Psychiatry 36, 927.
6. 2 antagonist, J. Label. Compd. Radiopharm. 20, 73.
7. 18F]Setoperone: a new high-affinity ligand for positron emission tomography study of the serotonin-2 receptors in baboon brain in vivo, Eur. J. Pharmacol. 147, 73.
8. 18F-labeled setoperone, J. Neurochem. 54, 1744.
9. 18F]setoperone, Brain 116, 497.
10. 18F]cyclofoxy and positron emission tomography, J. Cereb. Blood Flow Metab. 13, 24.
11. 2 receptor binding sites in depressed suicide victims, Brain Res. 443, 272.
12. Crow, T.J., A.J. Cross, S.J. Cooper, J.F.W. Deakin, I.N. Ferrier, J.A. Johnson, M.H. Joseph, F. Owen, M. Poulter, R. Lofthouse, J.A.N. Corsellis, D.R. Chambers, G. Blessed, E.K. Perry and E.H. Perry, 1984, Neurotransmitter receptors and monoamine metabolites in the patients with Alzheimer-type dementia and depression, and suicides, Neuropharmacology 23, 1561.
13. Gandelman, M.S., R.M. Baldwin, S.S. Zoghbi, Y. Zea-Ponce and R.B. Innis, 1994, Evaluation of ultrafiltration for the free fraction determination of single photon emission computerized tomography (SPECT) radiotracers: β-CIT, IBF and iomazenil, J. Pharm. Sci. 83, 1014.
14. 3H]ketanserin binding in the human brain post-mortem: effect of suicide, Brain Res. 507, 208.
15. 2 recognition sites, Brain Res. 376, 97.
16. Joyce, J.N., A. Shane, N. Lexow, A. Winokur, M.F. Casanova and J.E. Kleinman, 1993, Serotonin uptake sites and serotonin receptors are altered in the limbic system of schizophrenics, Neuropsychopharmacology 8, 315.
17. Laruelle, M., A. Abi-Dargham, M.F. Casanova, R. Toti, D.R. Weinberger and J.E. Kleinman, 1993, Selective abnormalities of prefrontal serotonergic receptors in schizophrenia: a postmortem study, Arch. Gen. Psychiatry 50, 810.
18. 123I]iodobenzofuran and single photon emission computerized tomography, Eur. J. Pharmacol. 263, 39.
19. 123I]iomazenil binding to benzodiazepine receptors in nonhuman primates. I. Kinetic modeling of single bolus experiments, J. Cereb. Blood Flow Metab. 14, 439.
20. 2 receptors in healthy subjects, J. Nucl. Med. 35, 743.
21. 123I]β-CIT in vivo binding to dopamine transporters in healthy subjects, J. Cereb. Blood Flow Metab. 14, 982.
22. Lemaire, C., R. Cantineau, M. Guillaume, A. Plenevaux and L. Christiaens, 1991, Fluorine-18-altanserin: a radioligand for the study of serotonin receptors with PET: radiolabeling and in vivo biologic behavior in rats, J. Nucl. Med. 32, 2266.
23. Levenberg, K., 1944, A method for the solution of certain problems in least squares, Q. Appl. Math. 2, 164.
24. 3H]Ketanserin (R 41 468), a selective H-ligand for serotonin-2 receptor binding sites: binding properties, brain distribution and functional role, Mol. Pharmacol. 21, 301.
25. Leysen, J.E., P.M.F. Janssen, A.A.H.P. Megens and A. Schotte, 1994, Risperidone: a novel antipsychotic with balanced serotonin-dopamine antagonism, receptor occupancy profile, and pharmacologic activity, J. Clin. Psychiatry 55 (Suppl.), 5.
26. 11C-methyl]-(-)-cocaine PET studies in human subjects, J. Cereb. Blood Flow Metab. 10, 740.
27. 2 receptors in suicide victims: violence of death, depression and effects of antidepressant treatment, Brain Res. 642, 281.
28. 2 receptors in human brain, J. Neurochem. 43, 1068.
29. 2 and beta receptor in the frontal cortices of suicide victims, Arch. Gen. Psychiatry 43, 954.
30. 2 serotonin receptors after stroke: lateralized changes and relationship to depression, Am. J. Psychiatry 145, 937.
31. McKeith, I.G., E.F. Marshall, I.N. Ferrier, M.M. Armstrong, W.N. Kennedy, R.H. Perry, E.K. Perry and D. Eccleston, 1987, 5-HT receptor binding in post-mortem brains from patients with affective disorder, J. Affect. Disord. 13, 67.
32. Meltzer, H., 1989, Clinical studies on the mechanism of action of clozapine: the dopamine-serotonin hypothesis of schizophrenia, Psychopharmacology 99, S18.
33. 2-receptors, a promising tracer for gamma-emission tomography, J. Label. Compd. Radiopharm. 34, 795.
34. Mintun, M.A., M.E. Raichle, M.R. Kilbourn, G.F. Wooten and M.J. Welch, 1984, A quantitative model for the in vivo assessment of drug binding sites with positron emission tomography, Ann. Neurol. 15, 217.
35. 2 receptors in chronic schizophrenics, Biol. Psychiatry 21, 1407.
36. 18F]fluoroethylketanserin and PET, Neurosci. Lett. 123, 23.
37. 2 dopamine receptor occupancy in the living human brain. A PET study with risperidone, Psychopharmacology 110, 265.
38. 2 receptor binding abnormalities in patients with Alzheimer's disease: comparisons with Parkinson's disease, Neurosci. Lett. 51, 353.
39. 2 receptors in senile dementia of the Alzheimer type, Neurosci. Lett. 44, 47.
40. Riche, D., P. Hantraye, B. Guibert, R. Naquet, C. Loch'h and M. Mazière, 1988, Anatomical atlas of the baboon's brain in the orbitomeatal plane used in experimental positron emission tomography, Brain Res. Bull. 20, 283.
41. 18F]altanserin: results in young normal controls, J. Cereb. Blood Flow Metab. 15, 787.
42. 123I]IPCIT as single-photon emission tomography radiotracers for the dopamine transporter in nonhuman primates, Eur. J. Nucl. Med. 22, 4.
43. 2-receptors in human brain, Brain Res. 276, 231.
44. Snyder, W.S., M.I. Cook, L.R. Karhausen, E.S. Nasset, G.P. Howells and I.H. Tipton, 1984, Central nervous system, in: Report of the Task Group on Reference Man (Pergamon Press, New York, NY) p. 281.
45. Stanley, M. and J.J. Mann, 1983, Increased serotonin-2 binding sites in frontal cortex of suicide victims, Lancet 2, 214.
46. Whitaker, P.M., T.J. Crow and I.N. Ferrier, 1981, Tritiated LSD binding in frontal cortex in schizophrenia, Arch. Gen. Psychiatry 38, 278.
47. Wong, D.F., H.N. Wagner, R.F. Dannals, J.M. Links, J.J. Frost, H.T. Ravert, A.A. Wilson, A.E. Rosenbaum, A. Gjedde, K.H. Douglass, J.D. Petronis, M.F. Folstein, J.K.T. Toung, H.D. Burns and M.J. Kuhar, 1984, Effects of age on dopamine and serotonin receptors measured by positron emission tomography in the living brain, Science 226, 1393.
48. 11C]-methyl)-2-Br-LSD, Synapse 1, 393.
49. 2 receptors changes in major depression, Biol. Psychiatry 27, 489.