Positron emission tomographic analysis of central 5-hydroxytryptamine2 receptor occupancy in healthy volunteers treated with the novel antipsychotic agent, ziprasidone

Journal of Pharmacology and Experimental Therapeutics

Volumn 279, Issue 2, 1996, Pages 939-947

  Fischman, Alan J ^a,b,c   Bonab, Ali A ^a   Babich, John W ^a   Alpert, Nathaniel M ^a   Rauch, Scott L ^a,b   Elmaleh, David R ^a   Shoup, Timothy M ^d   Williams, Stephen A ^e   Rubin, Robert H ^a,c  

^a HARVARD MEDICAL SCHOOL   (United States)

^b MASSACHUSETTS GENERAL HOSPITAL   (United States)

^c MASSACHUSETTS INSTITUTE OF TECHNOLOGY   (United States)

^d EMORY UNIVERSITY SCHOOL OF MEDICINE   (United States)

^e PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CHLORPROMAZINE; CLOZAPINE; NEUROLEPTIC AGENT; SEROTONIN 2 RECEPTOR; SETOPERONE; ZIPRASIDONE;

ADULT; ARTICLE; BINDING KINETICS; CLINICAL TRIAL; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG TRANSPORT; HUMAN; HUMAN EXPERIMENT; MALE; MATHEMATICAL COMPUTING; NORMAL HUMAN; ORAL DRUG ADMINISTRATION; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; PSYCHOSIS; RECEPTOR AFFINITY; RECEPTOR BLOCKING; RECEPTOR OCCUPANCY;

ADULT; ANTIPSYCHOTIC AGENTS; BRAIN CHEMISTRY; CEREBROVASCULAR CIRCULATION; HUMANS; MALE; PIPERAZINES; PYRIMIDINONES; RECEPTORS, SEROTONIN; SEROTONIN ANTAGONISTS; THIAZOLES; TOMOGRAPHY, EMISSION-COMPUTED;

EID: 0030441051     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (64)

1. BALDESSARINI, R. J., COLE, J. O. AND DAVIS, J. M.: Tardive dyskinesia: Summary of a task force report of the American Psychiatric Association. Am. J. Psychiatry 137: 1163-1172, 1980.
2. BARON, J. C., MARTINOT, J. L., CAMBON, H., BOULENGER, J. P., POIRIER, M. F., CAILLARD, V., BLIN, J., HURET, J. D., LOC'H, C. AND MAZIERE, B.: Striatal dopamine receptor occupancy during and following withdrawal from neuroleptic treatment: Correlative evaluation by positron emission tomography and plasma prolactin levels. Psychopharmacology (Berl.) 99: 463-472, 1989.
3. 11C-raclopride. Psychopharmacology (Berl.) 112: 308-314, 1993.
4. 2 antagonism in schizophrenia: Clinical, extrapyramidal and neuroendocrine response in a preliminary study with risperidone (R64.766). Human Psychopharmacol. 5: 225-231, 1990.
5. 18F-setoperone studied in humans using positron emission tomography. J. Neurochem. 58: 2303-2310, 1992.
6. 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: 73-82, 1988.
7. 18F-labeled setoperone. J. Neurochem. 54: 1744-1754, 1990.
8. BUCHSBAUM, M. A., WU, J. C., DELISI, L. E., HOLCOMB, H. H., HAZLETT, E., COOPER-LANGSTON, K. AND KESSLER, R.: Positron emission tomography studies of basal ganglia and somatosensory cortex: Neuroleptic drug effects. Biol. Psychiatry 22: 479-494, 1987.
9. BUNNEY, B. S. AND GRACE, A. A.: Acute and chronic haloperidol treatment: Comparison of effects on nigral dopaminergic cell activity. Life Sci. 23: 1715-1727, 1978.
10. BURT, D. R., CREESE, I. AND SNYDER, S. H.: Antischizophrenic drugs: Chronic treatment elevated dopamine binding in the brain. Science (Wash. DC) 196: 326-328, 1977.
11. CAMBON, H., BARON, J. C., BOULENGER, J. B., COC'H, C., ZARIFIAN, E. AND MAZIERE, B.: In vivo assay for neuroleptic receptor binding in the striatum. Positron tomography in humans. Br. J. Psychiatry 151: 824-830, 1987.
12. CASEY, D. E.: Clozapine: Neuroleptic-induced EPS and tardive dyskinesia. Psychopharmacology (Berl.) 99: S47-S53, 1989.
13. CEULEMANS, D. L., GELDERS, Y. G., HOPPENBROUWERS, M. L., REYNTJENS, A. J. AND JANSSEN, P. A.: Effect of serotonin antagonism in schizophrenia: A pilot study with setoperone. Psychopharmacology (Berl.) 853: 329-332, 1985.
14. CHIODO H. AND BUNNEY, B. S.: Possible mechanisms by which repeated clozapine administration differentially affects the activity of two subpopulations of midbrain dopamine neurons. J. Neurosci. 5: 2539-2544, 1985.
15. CLOW, A., THEODOROU, A., JENNER, P. AND MARSDEN, C. D.: Changes in rat striatal dopamine turnover and receptor activity during one year's neuroleptic administration. Eur. J. Pharmacol. 63: 135-144, 1980.
16. COSTALL, B., FORTUNE, D. H., NAYLOR, R. J., MARDSEN, C. D. AND PYCOCK, C.: Serotonergic involvement with neuroleptic catalepsy. Neuropharmacology 1411: 859-868, 1975.
17. CREESE, I., BURT, D. R. AND SNYDER, S. H.: Dopamine receptor binding predicts clinical and pharmacological potencies of antischizophrenic drugs. Science (Wash. DC) 192: 481-483, 1976.
18. DALAY, J. AND DENIKER, O.: Caracteristiques psycho-physiologiques des medicamementes neuroleptiques. In The Psychotropic Drugs, S. Gararrini and V. Ghetti, pp. 557-564, Elsevier Publishing Co., Amsterdam, 1957.
19. DAVIS, J. M., SCHAFFER, C. B., KILLIAN, G. A., KINARD, C. AND CHAN, C.: Important issues in the drug treatment of schizophrenia. Schizophr. Bull. 6: 70-87, 1980.
20. DELISI, L. E., HOLCOMB, H. H., COHEN, R. M., PICKAR, D., CARPENTER, W., MORIHISA, J. M., KING, A. C., KESSLER, R. AND BUCHSBAUM, M. A.: Positron emission tomography in schizophrenic patients with and without neuroleptic medication. J. Cerebr. Blood Flow Metab. 5: 201-206, 1985.
21. 11C]raclopride. Psychopharmacology (Berl.) 107: 23-29, 1992.
22. 11C-raclopride. Psychopharmacology (Berl.) 92: 278-284, 1987.
23. 2-receptor occupancy in clozapine-treated patients. J. Clin. Psychiatry 55: Suppl. B, 67-69, 1994.
24. 2 dopamine receptor occupancy in patients treated with classical neuroleptics and clozapine. Relation to extrapyramidal side effects. Arch. Gen. Psychiatry 49: 538-544, 1992.
25. 2 receptor binding in risperidone-treated schizophrenic patients. J. Clin. Psychopharmacol. 15: Suppl. 1, 19S-23S, 1995.
26. 2-dopamine receptor occupancy in schizophrenic patients treated with antipsychotic drugs. Arch. Gen. Psychiatry 45: 71-76, 1988.
27. 2-dopamine receptor occupancy during treatment with conventional and atypical neuroleptics. Psychopharmacology (Berl.) 99: S28-S31, 1989.
28. 2 dopamine receptors in neuroleptic naive schizophrenic patients. Arch. Gen. Psychiatry 47: 213-219, 1990.
29. 2 receptor blockers in the treatment of chronic schizophrenia. Clin. Neuropharmacol. 9: Suppl. 4, 325-327, 1986.
30. HOWARD, H. R., PRAKASH, C. AND SEEGER, T. F.: Ziprasidone hydrochloride. Drug Future 19: 560-563, 1994.
31. HUME, S. P., MYERS, R., BLOOMFIELD, P. M., OPACKA-JUFFRY, J., CREMER, J. E., AHIER, R. G., LUTHRA, S. K., BROOKS, D. J. AND LAMMERTSMA, A. A.: Quantitation of carbon-11 labeled raclopride in rat striatum using positron emission tomography. Synapse 12: 47-54, 1992.
32. KANE, J. M., COOPER, T. B., SACHAR, E. J., HALPERN, F. S. AND BAILINE, S.: Clozapine plasma levels and prolactin response. Psychopharmacology (Berl.) 73: 181-187, 1981.
33. KANE, J. M., HONIGFELD, G., SINGER, J. AND MELTZER, H. Y.: Clozapine for the treatment-resistant schizophrenic. A double-blind comparison with chlorpromazine. Arch. Gen. Psychiatry 45: 789-796, 1988.
34. KEBABIAN, J. W., PETZOLD, G. L. AND GREENGARD, P.: Dopamine-sensitive adenylate cyclase in caudate nucleus of rat brain, and its similarity to the "dopamine receptor." Proc. Natl. Acad. Sci. U.S.A. 69: 2145-2149, 1972.
35. 2 striatal receptors in schizophrenia. A study with positron emission tomography and 78Br bromospiperone. Br. J. Psychiatry 158: 346-350, 1991.
36. MATSUBARA, R.: A study on the pharmacological properties of atypical antipsychotic drugs: In vivo dopamine and serotonin receptor occupancy by atypical antipsychotic drugs in the rat brain. Hokkaido Igaku Zasshi 68: 570-582, 1993.
37. 2 receptor occupation by typical and atypical antipsychotic drugs in vivo. J. Pharmacol. Exp. Ther. 265: 498-508, 1993.
38. 18F-setoperone, a potential ligand for in-vivo imaging of cortical serotonin receptors. Int. J. Rad. Appl. Instrum. [B] 15: 463-168, 1988.
39. MELTZER, H. Y. AND FANG, V. S.: The effect of neuroleptics on serum prolactin in schizophrenic patients. Arch. Gen. Psychiatry 33: 279-286, 1976.
40. MELTZER, H. Y., GOODE, D. J., SCHYVE, P. M., YOUNG, M. AND FANG, V. S.: Effect of clozapine on human serum prolactin levels. Am. J. Psychiatry 136: 1550-1555, 1979.
41. 2 affinities differentiate atypical and typical antipsychotic drugs. Psychopharmacol. Bull. 25: 390-392, 1989.
42. MELTZER, H. Y.: The mechanism of action of novel antipsychotic drugs. Schizophr. Bull. 17: 263-287, 1991.
43. MINTUN, M. A., RAICHLE, M. E., KILBOURNE, M. R., WOOTON, G. F. AND WELCH, M. J.: A quantitative model for the in vivo assessment of drug binding sites with positron emission tomography. Annu. Neurol. 15: 217-227, 1984.
44. MIZULI, Y., KAJAMURA, N., IMAI, T., SUETSUGI, M., KAI, S., KANEYUKI, H. AND YAMADA, M.: Effects of mianserin on negative symptoms in schizophrenia. Int. Clin. Psychopharmacol. 5: 83-95, 1990.
45. 2 receptor occupancy in clozapine treated patients demonstrated by PET. Psychopharmacology (Berl.) 110: 365-367, 1993.
46. PEROUTKA, S. J. AND SNYDER, S. H.: Relationship of neuroleptic drug effects at brain dopamine, serotonin, adrenergic and histamine receptors to clinical potency. Am. J. Psychiatry 137: 1518-1522, 1980.
47. 18F-setoperone kinetic PET data analysis. J. Nucl. Med. 37: 95-104, 1996.
48. 1C receptors. J. Pharmacol. Exp. Ther. 260: 1361-1365, 1992.
49. ROTH, B. L., CRAIGO, S. C., CHOUDHARY, M. S., ULUER, A., MONSMA, F. J., SHEN, Y., MELTZER, H. Y. AND SIBLEY, D. R.: Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors. J. Pharmacol. Exp. Ther. 268: 1403-1410, 1994.
50. SEDVALL, G., PAULI, S., FARDE, L., KARLSSON, P., NYBERG, S. AND NORDSTROM, A. L.: Recent developments in PET scan imaging of neuroreceptors in schizophrenia. Israel J. Psychiatry Related Sci. 32: 22-29, 1995.
51. 2 antagonist activities. In Program and Abstracts of the 23rd Annual Meeting of the Society for Neuroscience, New Orleans, LA, p. 1623, 1993.
52. SEEMAN, P.: Atypical neuroleptics: role of multiple receptors, endogenous dopamine, and receptor linkage. Acta Psychiatry Scand. Suppl. 358: 14-20, 1990.
53. SEEMAN, P., LEE, T., CHAU-WONG, M. AND WONG, K.: Antipsychotic drug doses and neuroleptic/dopamine receptors. Nature (Lond.) 261: 717-719, 1976.
54. SEYMOUR, P. A., SEEGER, T. F., GUANOWSKY, V., ROBINSON, G. L., HOWARD, H. AND HEYM, J.: Behavioral pharmacology of CP-88,059: A new antipsychotic with both 5-HT2 and D2 antagonist activities. In Program and Abstracts of the 23rd Annual Meeting of the Society for Neuroscience, New Orleans, LA, p. 599, 1993.
55. STILE, G. AND HIPPIUS, H.: Kritische Stellungsnahme zum Begriff der Neuroleptika (anhand von pharmakologischen und klinischen Befunden mit Clozapin). Pharmacopsychiatry (Berl.) 4: 182-191, 1971.
56. 2 receptors. J. Pharmacol. Exp. Ther. 266: 1374-1384, 1993.
57. 2 antagonists with potential atypical antipsychotic activity: Antipsychotic profile of iloperidone (HP 873). J. Med. Chem. 38: 1119-1131, 1995.
58. SZECHTMAN, H., NAHMIAS, C., GARNETT, S., FIRNAU, G., BROWN, G. M., KAPLAN, R. D. AND CLEGHORN, J. M.: Effects of neuroleptics on altered cerebral glucose metabolism in schizophrenia. Arch. Gen. Psychiatry 45: 523-532, 1988.
59. TARSEY, D.: Neuroleptic-induced extrapyramidal reactions: Classification, description and diagnosis. Clin. Neuropharmacol. 6: 9-26, 1983.
60. VAN ROSSUM, M. J.: The significance of dopamine receptor-blockade for the mechanism of action of neuroleptic drugs. Arch. Int. Pharmacodyn. Ther. 160: 492-494, 1966.
61. VOLKOW, N. D., BRODIE, J. D., WOLF, A. P., ANGRIST, B., RUSSEL, J. AND CANCRO, R.: Brain metabolism in patients with schizophrenia before and after acute administration of neuroleptic medication. J. Neurol. Neurosurg. Psychiatry 49: 1199-1202, 1986.
62. WADDINGTON, J. L. AND O'BOYLE, K. M.: Drugs acting on brain dopamine receptors: A conceptual re-evaluation five years after the first selective D-1 antagonist. Pharmacol. Ther. 43: 1-52, 1989.
63. 2 dopamine receptors in drug-naive schizophrenics. Science (Wash. DC) 234: 1558-1563, 1986.
64. ZETTERSTOM, T., SHARP, T. AND UNGERSTEDT, U.: Effect of neuroleptic drugs on striatal dopamine release and metabolism in the awake rat studied by intracerebral dialysis. Eur. J. Pharmacol. 106: 27-37, 1984.