Occupancy of agonist drugs at the 5-HT1A receptor

Neuropsychopharmacology

Volumn 29, Issue 5, 2004, Pages 847-859

  Bantick, R Alexander ^a   Rabiner, Eugenii A ^a,c   Hirani, Ella ^a   De Vries, Michiel H ^b   Hume, Susan P ^a   Grasby, Paul M ^a  

^a HAMMERSMITH HOSPITAL   (United Kingdom)

^b Solvay Pharmaceuticals Inc   (Netherlands)

^c ADDENBROOKE S HOSPITAL   (United Kingdom)

Author keywords

5 HT1 receptor agonist; 5 HT1A receptor; Cerebral cortex; Flesinoxan; Tomography, emission computed; Ziprasidone

Indexed keywords

CARBON 11; FLESINOXAN; N [2 [4 (2 METHOXYPHENYL) 1 PIPERAZINYL]ETHYL] N (2 PYRIDYL)CYCLOHEXANECARBOXAMIDE; NEUROLEPTIC AGENT; SEROTONIN 1A AGONIST; SEROTONIN 1A ANTAGONIST; SEROTONIN 1A RECEPTOR; SEROTONIN AGONIST; TRACER; ZIPRASIDONE;

ADULT; AGONIST; ANIMAL EXPERIMENT; ARTICLE; BRAIN CORTEX; DEPRESSION; DOSE RESPONSE; DRUG RECEPTOR BINDING; GENERALIZED ANXIETY DISORDER; HIPPOCAMPUS; HUMAN; MALE; NONHUMAN; NORMAL HUMAN; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; RAT; RECEPTOR AFFINITY; RECEPTOR OCCUPANCY; SCHIZOPHRENIA; SEROTONINERGIC SYSTEM; SIDE EFFECT;

ADULT; ANIMALS; HUMANS; IMAGE PROCESSING, COMPUTER-ASSISTED; MALE; MIDDLE AGED; PIPERAZINES; PYRIDINES; RADIOLIGAND ASSAY; RATS; RATS, SPRAGUE-DAWLEY; RECEPTOR, SEROTONIN, 5-HT1A; SEROTONIN AGONISTS; SEROTONIN ANTAGONISTS; THIAZOLES; TOMOGRAPHY, EMISSION-COMPUTED;

EID: 1942500219     PISSN: 0893133X     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.npp.1300390     Document Type: Article

References (90)

1. Andree B, Hedman A, Thorberg SO, Nilsson D, Halldin C, Farde L (2003). Positron emission tomographic analysis of dose-dependent NAD-299 binding to 5-hydroxytryptamine-1A receptors in the human brain. Psychopharmacology (Berl) 167: 37-45.
2. 1A receptors in the human brain confirmed with positron emission tomography. Psychopharmacology (Berl) 144: 303-305.
3. Arato M, O'Connor R, Meltzer HY (2002). A 1-year, double-blind, placebo-controlled trial of ziprasidone 40, 80 and 160 mg/day in chronic schizophrenia: the Ziprasidone Extended Use in Schizophrenia (ZEUS) study. Int Clin Psychopharmacol 17: 207-215.
4. 1A receptor in schizophrenia: a promising target for novel atypical neuroleptics? J Psychopharmacol 15: 37-46.
5. 1A receptor in schizopherinia and during clozapine treatment. J Pschycopharmacol (in press).
6. Bench CJ, Lammertsma AA, Grasby PM, Dolan RJ, Warrington SJ, Boyce M et al (1996). The time course of binding to striatal dopamine D2 receptors by the neuroleptic ziprasidone (CP-88,059-01) determined by positron emission tomography. Psychopharmacology (Berl) 124: 141-147.
7. 3H]8-OH-DPAT and demonstration of increased binding in the frontal cortex in schizophrenia. Neurochem Int 30: 565-574.
8. Chamberlain J, Offord SJ, Wolfe BB, Tyau LS, Wang HL, Frazer A (1993). Potency of 5-hydroxytryptaminela agonists to inhibit adenylyl cyclase activity is a function of affinity for the 'low-affinity' state of [3H]8-hydroxy-N,N- dipropylaminotetralin ([3H]8-OH-DPAT) binding. J Pharmacol Exp Ther 266: 618-625.
9. 3H] propylnorapomorphine to dopamine receptors in living mouse striatum: occupancy by endogenous dopamine and guanosine triphosphate-free G protein. J Cereb Blood Flow Metab 22: 596-604.
10. Daniel DG, Zimbroff DL, Potkin SG, Reeves KR, Harrigan EP, Lakshminarayanan M (1999). Ziprasidone 80 mg/day and 160 mg/day in the acute exacerbation of schizophrenia and schizoaffective disorder: a 6-week placebo-controlled trial. Ziprasidone Study Group. Neuropsychopharmacology 20: 491-505.
11. de Koning P, de Vries MH (1995). A comparison of the neuroendocrinological and temperature effects of DU 29894, flesinoxan, sulpiride and haloperidol in normal volunteers. Br J Clin Pharmacol 39: 7-14.
12. 1A receptor agonists: recent developments and controversial issues. Psychopharmacology (Berl) 121: 1-26.
13. Drevets WC, Frank E, Price JC, Kupfer DJ, Greer PJ, Mathis C (2000). Serotonin type-1A receptor imaging in depression. Nucl Med Biol 27: 499-507.
14. 1A receptors in the primate brain. Psychopharmacology (Berl) 133: 196-202.
15. Fischman AJ, Bonab AA, Babich JW, Alpert NM, Rauch SL, Elmaleh DR et al (1996). Positron emission tomographic analysis of central 5-hydroxytryptamine2 receptor occupancy in healthy volunteers treated with the novel antipsychotic agent, ziprasidone. J Pharmacol Exp Ther 279: 939-947.
16. Fletcher A, Forster EA, Bill DJ, Brown G, Cliffe IA, Hartley JE et al (1996). Electrophysiological, biochemical, neurohormonal and behavioural studies with WAY-100635, a potent, selective and silent 5-HT1A receptor antagonist. Behav Brain Res 73: 337-353.
17. Gale CK, Oakley-Browne M (2002). Generalised anxiety disorder. Clin Evid 8: 974-990.
18. Glassman AH, Bigger Jr JT (2001). Antipsychotic drugs: prolonged QTc interval, torsade de pointes, and sudden death. Am J Psychiatry 158: 1774-1782.
19. Goff DC, Posever T, Herz L, Simmons J, Kletti N, Lapierre K et al (1998). An exploratory haloperidol-controlled dose-finding study of ziprasidone in hospitalized patients with schizophrenia or schizoaffective disorder. J Clin Psychopharmacol 18: 296-304.
20. 1A receptors in rat brain membranes. Eur J Pharmacol 288: 173-186.
21. Gunasekara NS, Spencer CM, Keating GM (2002). Ziprasidone: a review of its use in schizophrenia and schizoaffective disorder. Drugs 62: 1217-1251.
22. 11C]WAY-100635 PET studies. Nucl Med Biol 27: 477-482.
23. Gunn RN, Lammertsma AA, Hume SP, Cunningham VJ (1997). Parametric imaging of ligand-receptor binding in PET using a simplified reference region model. Neuroimage 6: 279-287.
24. 11C]WAY-100635 for PET. Neuroimage 8: 426-440.
25. 1A properties of flesinoxan: in vivo electrophysiology and hypothermia study. Neuropharmacology 34: 1311-1326.
26. 1A receptors. Neurosci Lett 304: 129-132.
27. 1A receptors measured in vivo using small animal positron emission tomography with carbon-11 labeled WAY 100635. Synapse 36: 330-341.
28. Hirsch SR, Kissling W, Bauml J, Power A, O'Connor R (2002). A 28-week comparison of ziprasidone and haloperidol in outpatients with stable schizophrenia. J Clin Psychiatry 63: 516-523.
29. 1A receptors in rat brain, assessed using in vivo microdialysis and PET after fenfluramine. Synapse 41: 150-159.
30. 1A receptors in rat brain. Eur J Pharmacol 271: 515-523.
31. Hume SP, Brown DJ, Ashworth S, Hirani E, Luthra SK, Lammertsma AA (1997). In vivo saturation kinetics of two dopamine transporter probes measured using a small animal positron emission tomography scanner. J Neurosci Methods 76: 45-51.
32. Hume SP, Gunn RN, Jones T (1998). Pharmacological constraints associated with positron emission tomographic scanning of small laboratory animals. Eur J Nucl Med 25: 173-176.
33. Jeavons AP, Chandler RA, Dettmar CAR (1999). A 3D HIDAC-PET camera with sub-millimetre resolution for imaging small animals. IEEE Trans Nucl Sci 46: 468-473.
34. 1A receptor. Eur J Pharmacol 441: 137-140.
35. Keck Jr P, Buffenstein A, Ferguson J, Feighner J, Jaffe W, Harrigan EP et al (1998). Ziprasidone 40 and 120 mg/day in the acute exacerbation of schizophrenia and schizoaffective disorder: a 4-week placebo-controlled trial. Psychopharmacology (Berl) 140: 173-184.
36. 1A receptor antagonist. Brain Res 673: 217-225.
37. 11C]WAY-100635 [abstract]. Neuroimage 16: S106.
38. 11C]WAY-100635: effect of endogenous serotonin. Synapse 40: 122-129.
39. Mann JJ, Oquendo MA, Simpson N, Huang Y, Van Heertum R, Arango V et al (2002). Altered 5-HT-1A binding in major depression: an [11C]WAY100635 PET study. NeuroImage 16: S105.
40. Martinez D, Broft A, Laruelle M (2000). Pindolol augmentation of antidepressant treatment: recent contributions from brain imaging studies. Biol Psychiatry 48: 844-853.
41. 11C]WAY 100635 and positron emission tomography in humans. Neuropsychopharmacology 24: 209-229.
42. 1A receptor antagonist [abstract]. J Nucl Med 36: 162P.
43. 1A agonists as radioligands: failure of G protein-coupled receptor agonists as in vivo imaging agents. J Labelled Compd Radiopharm 40: 563-564.
44. 1A receptors with positron emission tomography. Life Sci 55: PL403-PL407.
45. 11C-carboxylation of an immobilised Grignard Reagent. J Labelled Compd Radiopharm 38: 941-953.
46. 1A receptors. J Neurochem 74: 347-357.
47. Miceli JJ, Wilner KD, Hansen RA, Johnson AC, Apseloff G, Gerber N (2000). Single- and multiple-dose pharmacokinetics of ziprasidone under non-fasting conditions in healthy male volunteers. Br J Clin Pharmacol 49: 5S-13S.
48. 1A receptors. J Pharmacol Exp Ther 295: 853-861.
49. Mongeau R, Welner SA, Quirion R, Suranyi-Cadotte BE (1992). Further evidence for differential affinity states of the serotonin1A receptor in rat hippocampus. Brain Res 590: 229-238.
50. 1A receptor examined using positron emission tomography and neuroendocrine response. Psychopharmacology (Berl).
51. 1A) receptors. Neuropsychopharmacology 18: 395-398.
52. 35S]GTPγS binding study. Eur J Pharmacol 355: 245-256.
53. 11C]WAY-100635 binding: considerations on the cerebellum. Nucl Med Biol 27: 483-486.
54. 11C]carbonyl-WAY 100635 and endogenous serotonin [abstract]. J Nucl Med 40: 29P.
55. 11C]WAY-100635 in humans: comparison of arterial and reference tissue input functions. J Cereb Blood Flow Metab 20: 1111-1133.
56. 1A) receptors in the central nervous system. Eur J Nucl Med 28: 113-129.
57. 18F]MPPF. Psychopharmacology (Berl) 155: 193-197.
58. Paxinos G, Watson C (1996). The Rat Brain in Stereotaxic Coordinates: Compact, 3rd edn. Academic Press: London.
59. Pazos A, Probst A, Palacios JM (1987). Serotonin receptors in the human brain - III. Autoradiographic mapping of serotonin-1 receptors. Neuroscience 21: 97-122.
60. 1A receptors in vivo. Prog Med Chem 38: 189-247.
61. 11C]WAY-100635. Eur J Pharmacol 301: R5-7.
62. 1A receptor agonist flesinoxan in normal volunteers. Psychopharmacology (Berl) 164: 27-32.
63. Pitsikas N (1999). Flesinoxan. Curr Opin CPNS Invest Drugs 1: 489-502.
64. 1A receptors in vivo and in vitro: implications for antidepressant therapy. Neuropsychopharmacology 23: 285-293.
65. 11C]WAY-100635. Nucl Med Biol 27: 509-513.
66. 11C]raclopride. J Psychopharmacol 16: 195-199.
67. 1A receptors in normal male volunteers: normative data and relationship to methodological, demographic, physiological, and behavioral variables. Neuroimage 15: 620-632.
68. 11C][O-methyl- 3H]-N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-py ridinyl) cyclohexanecarboxamide trihydrochloride (WAY-100635) positron emission tomography study in humans. J Pharmacol Exp Ther 301: 1144-1150.
69. Rice OV, Gatley SJ, Shen J, Huemmer CL, Rogoz R, DeJesus OT et al (2001). Effects of endogenous neurotransmitters on the in vivo binding of dopamine and 5-HT radiotracers in mice. Neuropsychopharmacology 25: 679-689.
70. 1A receptor activation contributes to ziprasidone-induced dopamine release in the rat prefrontal cortex. Biol Psychiatry 48: 229-237.
71. 11C]WAY-100635: effects of depression and antidepressant treatment. Arch Gen Psychiatry 57: 174-180.
72. Schmidt AW, Lebel LA, Howard Jr HR, Zorn SH (2001). Ziprasidone: a novel antipsychotic agent with a unique human receptor binding profile. Eur J Pharmacol 425: 197-201.
73. Seeger TF, Seymour PA, Schmidt AW, Zorn SH, Schulz DW, Lebel LA et al (1995). Ziprasidone (CP-88,059): a new antipsychotic with combined dopamine and serotonin receptor antagonist activity. J Pharmacol Exp Ther 275: 101-113.
74. 1A receptor activation by flesinoxan in humans. Body temperature and neuroendocrine responses. Neuropsychopharmacology 13: 93-104.
75. 1A receptor system: possible implications for schizophrenic negative symptomatology. Psychiatr Annals 26: 88-92.
76. 18F]-MPPF: a potential radioligand for PET studies of 5-HT1A receptors in humans. Synapse 25: 147-154.
77. 11C]WAY-100635 binding parameters with reference tissue models: effect of violations of model assumptions. Nucl Med Biol 27: 487-492.
78. Solvay Pharmaceuticals (1997). Investigational Drug Brochure: Flesinoxan.HCl capsules. Solvay Pharmaceuticals, Weesp: The Netherlands.
79. Spinks TJ, Jones T, Bailey DL, Townsend DW, Grootoonk S, Bloomfield PM et al (1992). Physical performance of a positron tomograph for brain imaging with retractable septa. Phys Med Biol 37: 1637-1655.
80. Spinks TJ, Jones T, Bloomfield PM, Bailey DL, Miller M, Hogg D et al (2000). Physical characteristics of the ECAT EXACT3D positron tomograph. Phys Med Biol 45: 2601-2618.
81. 1A receptor activation. Neuropsychopharmacology 21: 622-631.
82. Strange PG (1999). G-protein coupled receptors: conformations and states. Biochem Pharmacol 58: 1081-1088.
83. Tandon R (2000). Introduction. Ziprasidone appears to offer important therapeutic and tolerability advantages over conventional, and some novel, antipsychotics. Br J Clin Pharmacol 49(Suppl 1): 1S-3S.
84. 11C]WAY-100635. Arch Gen Psychiatry 59: 514-520.
85. 11C]WAY-100635 in conscious monkeys. Synapse 42: 242-251.
86. 18F]MPPF binding. Synapse 46: 108-115.
87. 1A receptor agonist flesinoxan via P-glycoprotein at the blood-brain barrier. Eur J Pharm Sci 14: 81-86.
88. 1A receptor agonist, and its in vivo evaluation in anaesthetised rat and in awake cat. Nucl Med Biol 30: 541-546.
89. 18F-MPPF in the rat hippocampus: kinetic beta measurements combined with microdialysis. J Neurochem 80: 278-286.
90. 18F-MPPF binding in the rat hippocampus. J Nucl Med 44: 1495-1501.