Imaging the serotonin transporter during major depressive disorder and antidepressant treatment

Journal of Psychiatry and Neuroscience

Volumn 32, Issue 2, 2007, Pages 86-102

  Meyer, Jeffrey H ^a  

^a CENTRE FOR ADDICTION AND MENTAL HEALTH   (Canada)

Author keywords

Antidepressant; Depression; PET; Positron emission tomography; Serotonin; Serotonin transporter

Indexed keywords

3 AMINO 4 (2 DIMETHYLAMINOMETHYL PHENYLSULFANYL)BENZONITRILE; ALTANSERIN; AMISULPRIDE; CARBON 11; CITALOPRAM; CLOMIPRAMINE; FLUORINE 18; FLUOXETINE; FLUVOXAMINE; KETANSERIN; NITRILE; PAROXETINE; PLACEBO; SEROTONIN; SEROTONIN RECEPTOR; SEROTONIN TRANSPORTER; SEROTONIN UPTAKE INHIBITOR; SERTRALINE; SETOPERONE; TRANYLCYPROMINE; UNCLASSIFIED DRUG; VENLAFAXINE;

BINDING AFFINITY; CLINICAL FEATURE; DOSE RESPONSE; DRUG DISTRIBUTION; DRUG MECHANISM; DRUG RECEPTOR BINDING; HUMAN; MAJOR DEPRESSION; NEUROIMAGING; NONHUMAN; POSITRON EMISSION TOMOGRAPHY; RECEPTOR OCCUPANCY; REVIEW;

EID: 34247137134     PISSN: 11804882     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (191)

1. Lesch KP, Wolozin BL, Estler HC, et al. Isolation of a cDNA encoding the human brain serotonin transporter. J Neural Transm Gen Sect 1993;91:67-72.
2. Lesch KP, Wolozin BL, Murphy DL, et al. Primary structure of the human platelet serotonin uptake site: identity with the brain serotonin transporter. J Neurochem 1993;60:2319-22.
3. Blakely R, Ramamoorthy S, Qian Y, et al. Regulation of Antidepressant-Sensitive Serotonin Transporters. In: Reith M, editor. Neurotransmitter Transporters: Structure, Function, and Regulation. Totowa: Humana Press, 1997. p. 29-72.
4. Zhou FC, Tao-Cheng JH, Segu L, et al. Serotonin transporters are located on the axons beyond the synaptic junctions: anatomical and functional evidence. Brain Res 1998;805:241-54.
5. Cortes R, Soriano E, Pazos A, et al. Autoradiography of Antidepressant Binding Sites in the Human Brain: Localization Using [3H]Imipramine and [3H]Paroxetine. Neuroscience 1988;27:473-96.
6. Kish SJ, Furukawa Y, Chang LJ, et al. Regional distribution of serotonin transporter protein in postmortem human brain: is the cerebellum a SERT-free brain region? Nucl Med Biol 2005;32:123-8.
7. Laruelle M, Vanisberg MA, Maloteaux JM. Regional and subcellular localization in human brain of [3H] paroxetine binding, a marker of serotonin uptake sites. Biol Psychiatry 1988;24:299-309.
8. Blier P, De Montigny C. Electrophysiological Investigations On The Effect of Repeated Zimelidine Administration on Serotonergic Neurotransmission in the Rat. J Neurosci 1983;3:1270-8.
9. Bel N, Artigas F. Fluvoxamine preferentially increases extracellular 5-hydroxytryptamine in the raphe nuclei: an in vivo microdialysis study. Eur J Pharmacol 1992;229:101-3.
10. Bel N, Artigas F. Chronic Treatment With Fluvoxamine Increases Extracellular Serotonin in Frontal Cortex but Not in Raphe Nuclei. Synapse 1993;15:243-5.
11. Dreshfield LJ, Wong DT, Perry KW, et al. Enhancement of fluoxetine-dependent increase of extracellular serotonin (5-HT) levels by (-)-pindolol, an antagonist at 5-HT1A receptors. Neurochem Res 1996;21:557-62.
12. Moret C, Briley M. Effects of acute and repeated administration of citalopram on extracellular levels of serotonin in rat brain. Eur J Pharmacol 1996;295:189-97.
13. Bel N, Artigas F. In vivo evidence for the reversible action of the monoamine oxidase inhibitor brofaromine on 5-hydroxytryptamine release in rat brain. Naunyn Schmiedebergs Arch Pharmacol 1995;351:475-82.
14. Mathews TA, Fedele DE, Unger EL, et al. Effects of serotonin transporter inactivation on extracellular 5-HT levels, in vivo microdialysis recovery, and MDMA-induced release of serotonin and dopamine in mouse striatum. Soc Neurosci Abstr 2000;30:624.
15. Huang Y, Hwang DR, Narendran R, et al. Comparative evaluation in nonhuman primates of five PET radiotracers for imaging the serotonin transporters: [11C]McN 5652, [11C]ADAM, [11C]DASB, [11C]DAPA, and [11C]AFM. J Cereb Blood Flow Metab 2002;22: 1377-98.
16. Frankle WG, Huang Y, Hwang DR, et al. Comparative evaluation of serotonin transporter radioligands 11C-DASB and 11C-McN 5652 in healthy humans. J Nucl Med 2004;45:682-94.
17. Szabo Z, Kao P, Scheffel U, et al. Positron Emission Tomography Imaging of Serotonin Transporters in the Human Brain Using [11C](+)McN5652. Synapse 1995;20:37-43.
18. Buck A, Gucker PM, Schonbachler RD, et al. Evaluation of serotonergic transporters using PET and [11C](+)McN-5652: assessment of methods. J Cereb Blood Flow Metab 2000;20:253-62.
19. Parsey RV, Kegeles LS, Hwang DR, et al. In vivo quantification of brain serotonin transporters in humans using [11C]McN 5652. J Nucl Med 2000;41:1465-77.
20. Ginovart N, Wilson AA, Meyer JH, et al. Positron emission tomography quantification of [(11)C]-DASB binding to the human serotonin transporter: modeling strategies. J Cereb Blood Flow Metab 2001;21:1342-53.
21. Ichise M, Liow JS, Lu JQ, et al. Linearized reference tissue parametric imaging methods: application to [11C]DASB positron emission tomography studies of the serotonin transporter in human brain. J Cereb Blood Flow Metab 2003;23:1096-112.
22. Carroll FI, Kotian P, Dehghani A, et al. Cocaine and 3 beta-(4′-substituted phenyl)tropane-2 beta-carboxylic acid ester and amide analogues. New high-affinity and selective compounds for the dopamine transporter. J Med Chem 1995;38:379-88.
23. Laruelle M, Giddings SS, Zea-Ponce Y, et al. Methyl 3 beta-(4-[125I]iodophenyl)tropane-2 beta-carboxylate in vitro binding to dopamine and serotonin transporters under "physiological" conditions. J Neurochem 1994;62:978-86.
24. Shank RP, Vaught JL, Pelley KA, et al. McN-5652: a highly potent inhibitor of serotonin uptake. J Pharmacol Exp Ther 1988;247:1032-8.
25. Kung MP, Hou C, Oya S, et al. Characterization of [(123)I]IDAM as a novel single-photon emission tomography tracer for serotonin transporters. Eur J Nucl Med 1999;26:844-53.
26. Wilson AA, Ginovart N, Schmidt M, et al. Novel radiotracers for imaging the serotonin transporter by positron emission tomography: synthesis, radiosynthesis, in vitro and ex vivo evaluation of [11]C-labeled 2-(phenylthio)araalkylamines. J Med Chem 2000;43: 3103-10.
27. Wilson AA, Ginovart N, Hussey D, et al. In vitro and in vivo characterisation of [11C]-DASB: a probe for in vivo measurements of the serotonin transporter by positron emission tomography. Nucl Med Biol 2002;29:509-15.
28. Choi SR, Hou C, Oya S, et al. Selective in vitro and in vivo binding of [(125)I]ADAM to serotonin transporters in rat brain. Synapse 2000;38:403-12.
29. Oya S, Choi SR, Hou C, et al. 2-((2-((dimethylamino)methyl) phenyl)thio)-5-iodophenylamine (ADAM): an improved serotonin transporter ligand. Nucl Med Biol 2000;27:249-54.
30. Pirker W, Asenbaum S, Kasper S, et al. beta-CIT SPECT demonstrates blockade of 5HT-uptake sites by citalopram in the human brain in vivo. J Neural Transm Gen Sect 1995;100:247-56.
31. Tauscher J, Pirker W, de Zwaan M, et al. In vivo visualization of serotonin transporters in the human brain during fluoxetine treatment. Eur Neuropsychopharmacol 1999;9:177-9.
32. Kent JM, Coplan JD, Lombardo I, et al. Occupancy of brain serotonin transporters during treatment with paroxetine in patients with social phobia: a positron emission tomography study with 11C McN 5652. Psychopharmacology (Berl) 2002;164:341-8.
33. Suhara T, Takano A, Sudo Y, et al. High levels of serotonin transporter occupancy with low-dose clomipramine in comparative occupancy study with fluvoxamine using positron emission tomography. Arch Gen Psychiatry 2003;60:386-91.
34. Meyer JH, Wilson AA, Ginovart N, et al. Occupancy of serotonin transporters by paroxetine and citalopram during treatment of depression: a [(11)C]DASB PET imaging study. Am J Psychiatry 2001; 158:1843-9.
35. Meyer JH, Wilson AA, Sagrati S, et al. Serotonin transporter occupancy of five selective serotonin reuptake inhibitors at different doses: an [11C]DASB positron emission tomography study. Am J Psychiatry 2004;161:826-35.
36. Erlandsson K, Sivananthan T, Lui D, et al. Measuring SSRI occupancy of SERT using the novel tracer [123I]ADAM: a SPECT validation study. Eur J Nucl Med Mol Imaging 2005;32:1329-36.
37. Brucke T, Kornhuber J, Angelberger P, et al. SPECT imaging of dopamine and serotonin transporters with [123I]beta-CIT. Binding kinetics in the human brain. J Neural Transm Gen Sect 1993;94:137-46.
38. Kuikka JT, Bergstrom KA, Vanninen E, et al. Initial experience with single-photon emission tomography using iodine-123-labelled 2 beta-carbomethoxy-3 beta-(4-iodophenyl) tropane in human brain. Eur J Nucl Med 1993;20:783-6.
39. Ikoma Y, Suhara T, Toyama H, et al. Quantitative analysis for estimating binding potential of the brain serotonin transporter with [11 C]McN5652. J Cereb Blood Flow Metab 2002;22:490-501.
40. Houle S, Ginovart N, Hussey D, et al. Imaging the serotonin transporter with positron emission tomography: initial human studies with [11C]DAPP and [11C]DASB. Eur J Nucl Med 2000;27:1719-22.
41. Catafau AM, Perez V, Penengo MM, et al. SPECT of serotonin transporters using 1231-ADAM: optimal imaging time after bolus injection and long-term test-retest in healthy volunteers. J Nucl Med 2005;46:1301-9.
42. Frankle WG, Lombardo I, New AS, et al. Brain serotonin transporter distribution in subjects with impulsive aggressivity: a positron emission study with [11C]McN 5652. Am J Psychiatry 2005;162:915-23.
43. Praschak-Rieder N, Wilson AA, Hussey D, et al. Effects of tryptophan depletion on the serotonin transporter in healthy humans. Biol Psychiatry 2005;58:825-30.
44. Innis RB, Seibyl JP, Scanley BE, et al. Single photon emission computed tomographic imaging demonstrates loss of striatal dopamine transporters in Parkinson disease. Proc Natl Acad Sci U S A 1993;90:11965-9.
45. Ciliax BJ, Drash GW, Staley JK, et al. Immunocytochemical localization of the dopamine transporter in human brain. J Camp Neurol 1999;409:38-56.
46. Ichimiya T, Suhara T, Sudo Y, et al. Serotonin transporter binding in patients with mood disorders: a PET study with [11C](+)McN5652. Biol Psychiatry 2002;51:715-22.
47. Meyer JH, Houle S, Sagrati S, et al. Brain serotonin transporter binding potential measured with carbon 11-labeled DASB positron emission tomography: effects of major depressive episodes and severity of dysfunctional attitudes. Arch Gen Psychiatry 2004;61:1271-9.
48. Takano A, Suhara T, Ichimiya T, et al. Time course of in vivo 5-HTT transporter occupancy by fluvoxamine. J Clin Psychopharmacol 2006;26:188-91.
49. Acton PD, Choi SR, Hou C, et al. Quantification of serotonin transporters in nonhuman primates using [(123)I]ADAM and SPECT. J Nucl Med 2001;42:1556-62.
50. Chalon S, Tarkiainen J, Garreau L, et al. Pharmacological characterization of N,N-dimethyl-2-(2-amino-4-methylphenyl thio)benzylamine as a ligand of the serotonin transporter with high affinity and selectivity. J Pharmacol Exp Ther 2003;304:81-7.
51. Halldin C, Lundberg J, Sovago J, et al. [(11)C]MADAM, a new serotonin transporter radioligand characterized in the monkey brain by PET. Synapse 2005;58:173-83.
52. Lundberg J, Halldin C, Farde L. Measurement of serotonin transporter binding with PET and [(11)C]MADAM: A test-retest reproducibility study. Synapse 2006;60:256-63.
53. Lundberg J, Odano I, Olsson H, et al. Quantification of 11C-MADAM binding to the serotonin transporter in the human brain. J Nucl Med 2005;46:1505-15.
54. Kim JS, Ichise M, Sangare J, et al. PET Imaging of Serotonin Transporters with [11C]DASB: Test-Retest Reproducibility Using a Multilinear Reference Tissue Parametric Imaging Method. J Nucl Med 2006;47:208-14.
55. Ashburner J, Friston KJ. Nonlinear spatial normalization using basis functions. Hum Brain Mapp 1999;7:254-66.
56. Ashburner J, Neelin P, Collins DL, et al. Incorporating prior knowledge into image registration. Neuroimage 1997;6:344-52.
57. Rusjan P, Mamo D, Ginovart N, et al. An automated method for the extraction of regional data from PET images. Psychiatry Res 2006;147:79-89.
58. Meyer J, Wilson A, Ginovart N, Houle S. Misunderstandings about how to choose a reference region. Biol Psychiatry 2007. In press.
59. Praschak-Rieder N, Kennedy J, Wilson A, et al. Novel 5-HTTLPR allele associates with higher serotonin transporter binding in putamen: An [11C] DASB Positron Emission Tomography study. Biol Psychiatry. In press.
60. 11C]-DASB binding to the serotonin transporter in humans, in Abstracts of the 48th Annual Meeting of the Society of Nuclear Medicine. Reston: SNM; 2001. p. 62.
61. Logan J, Fowler JS, Volkow ND, et al. Distribution volume ratios without blood sampling from graphical analysis of PET data. J Cereb Blood Flow Metab 1996;16:834-40.
62. Ichise M, Meyer JH, Yonekura Y. An introduction to PET and SPECT neuroreceptor quantification models. J Nucl Med 2001;42: 755-63.
63. Kontur PJ, al-Tikriti M, Innis RB, et al. Postmortem stability of monoamines, their metabolites, and receptor binding in rat brain regions. J Neurochem 1994;62:282-90.
64. Mann J, Underwood M, Arango V. Postmortem Studies of Suicide Victims, in Biology of Schizophrenia and Affective Disorders. In: Watson SJ, editor. Biology of Schizophrenia and Affective Disease. Washington: American Psychiatric Press; 1996 p. 197-221.
65. Pare CM. Iproniazid in the treatment of depression. Proc R Soc Med 1959;52:585-7.
66. Owens MJ, Morgan WN, Plott SJ, et al. Neurotransmitter receptor and transporter binding profile of antidepressants and their metabolites. J Pharmacol Exp Ther 1997;283:1305-22.
67. Tatsumi M, Groshan K, Blakely RD, et al. Pharmacological profile of antidepressants and related compounds at human monoamine transporters. Eur J Pharmacol 1997;340:249-58.
68. Practice guideline for the treatment of patients with major depressive disorder (revision). American Psychiatric Association. Am J Psychiatry 2000;157(4 Suppl):1-45.
69. Quetsch RM, Achor RW, Litin EM, et al. Depressive reactions in hypertensive patients; a comparison of those treated with Rauwolfia and those receiving no specific antihypertensive treatment. Circulation 1959;19:366-75.
70. Delgado PL, Charney DS, Price LH, et al. Serotonin function and the mechanism of antidepressant action: reversal of antidepressant-induced remission by rapid depletion of plasma tryptophan. Arch Gen Psychiatry 1990;47:411-8.
71. Delgado PL, Price LH, Miller HL, et al. Serotonin and the neurobiology of depression. Effects of tryptophan depletion in drug-free depressed patients. Arch Gen Psychiatry 1994;51:865-74.
72. Leyton M, Young SN, Benkelfat C. Relapse of depression after rapid depletion of tryptophan [letter; comment]. Lancet 1997;349: 1840-1.
73. Smith KA, Fairburn CG, Cowen PJ. Relapse of depression after rapid depletion of tryptophan. Lancet 1997;349:915-9.
74. Benkelfat C, Ellenbogen MA, Dean P, et al. Mood-lowering effect of tryptophan depletion. Enhanced susceptibility in young men at genetic risk for major affective disorders. Arch Gen Psychiatry 1994; 51:687-97.
75. Young SN, Smith SE, Pihl RO, et al. Tryptophan depletion causes a rapid lowering of mood in normal males. Psychopharmacology (Berl) 1985;87:173-7.
76. Smith K, Clifford E, Hockney R, et al. Effect of tryptophan depletion on mood in male and female volunteers: a pilot study. Hum Psychopharmacol Clin Exp 1997;12:111-7.
77. Neumeister A, Konstantinidis A, Stastny J, et al. Association between serotonin transporter gene promoter polymorphism (5HT-TLPR) and behavioral responses to tryptophan depletion in healthy women with and without family history of depression. Arch Gen Psychiatry 2002;59:613-20.
78. Arango V, Ernsberger P, Marzuk PM, et al. Autoradiographic demonstration of increased serotonin 5-HT2 and beta-adrenergic receptor binding sites in the brain of suicide victims. Arch Gen Psychiatry 1990;47:1038-47.
79. Arango V, Underwood M, Mann J. Alterations in monoamine receptors in the brain of suicide victims. J Clin Psychopharmacol 1992; 12:8S-12S.
80. Arora RC, Meltzer HY. Serotonergic measures in the brains of suicide victims: 5-HT2 binding sites in the frontal cortex of suicide victims and control subjects. Am J Psychiatry 1989;146:730-6.
81. Hrdina PD, Vu TB. Chronic fluoxetine treatment upregulates 5-HT uptake sites and 5-HT2 receptors in rat brain: an autoradiographic study. Synapse 1993;14:324-31.
82. Mann JJ, Stanley M, McBride PA, et al. Increased serotonin2 and beta-adrenergic receptor binding in the frontal cortices of suicide victims. Arch Gen Psychiatry 1986;43:954-9.
83. Stanley M, Mann JJ. Increased serotonin-2 binding sites in frontal cortex of suicide victims. Lancet 1983;1:214-6.
84. Yates M, Leake A, Candy JM, et al. 5HT2 receptor changes in major depression. Biol Psychiatry 1990;27:489-96.
85. Stockmeier CA, Dilley GE, Shapiro LA, et al. Serotonin receptors in suicide victims with major depression. Neuropsychopharmacology 1997;16:162-73.
86. Turecki G, Briere R, Dewar K, et al. Prediction of level of serotonin 2A receptor binding by serotonin receptor 2A genetic variation in postmortem brain samples from subjects who did or did not commit suicide. Am J Psychiatry 1999;156:1456-8.
87. Pandey GN, Dwivedi Y, Rizavi HS, et al. Higher expression of serotonin 5-HT(2A) receptors in the postmortem brains of teenage suicide victims. Am J Psychiatry 2002;159:419-29.
88. Stockmeier CA. Involvement of serotonin in depression: evidence from postmortem and imaging studies of serotonin receptors and the serotonin transporter. J Psychiatr Res 2003;37:357-73.
89. Meyer JH, McMain S, Kennedy SH, et al. Dysfunctional Attitudes and 5-HT(2) Receptors During Depression and Self-Harm. Am J Psychiatry 2003;160:90-9.
90. Stockmeier CA, Shapiro LA, Dilley GE, et al. Increase in serotonin-1A autoreceptors in the midbrain of suicide victims with major depression- postmortem evidence for decreased serotonin activity. J Neurosci 1998;18:7394-401.
91. O'Regan D, Kwok RP, Yu PH, et al. A behavioural and neurochemical analysis of chronic and selective monoamine oxidase inhibition. Psychopharmacology (Berl) 1987;92:42-7.
92. Roth BL, McLean S, Zhu XZ, et al. Characterization of two [3H]ketanserin recognition sites in rat striatum. J Neurochem 1987;49:1833-8.
93. Stockmeier CA, Kellar KJ. In vivo regulation of the serotonin-2 receptor in rat brain. Life Sci 1986;38:117-27.
94. Todd KG, McManus DJ, Baker GB. Chronic administration of the antidepressants phenelzine, desipramine, clomipramine, or maprotiline decreases binding to 5-hydroxytryptamine2A receptors without affecting benzodiazepine binding sites in rat brain. Cell Mol Neurobiol 1995;15:361-70.
95. Hoyer D, Pazos A, Probst A, et al. Serotonin receptors in the human brain. II. Characterization and autoradiographic localization of 5-HT1C and 5-HT2 recognition sites. Brain Res 1986;376:97-107.
96. Marazziti D, Rossi A, Giannaccini G, et al. Distribution and characterization of [3H]mesulergine binding in human brain postmortem. Eur Neuropsychopharmacol 1999;10:21-6.
97. Schmuck K, Ullmer C, Engels P, et al. Cloning and functional characterization of the human 5-HT2B serotonin receptor. FEBS Lett 1994;342:85-90.
98. D'haenen H, Bossuyt A, Mertens J, et al. SPECT imaging of serotonin2 receptors in depression. Psychiatry Res 1992;45:227-37.
99. Biver F, Wikler D, Lotstra F, et al. Serotonin 5-HT2 receptor imaging in major depression: focal changes in orbito-insular cortex. Br J Psychiatry 1997;171:444-8.
100. Attar-Levy D, Martinot J-L, Blin J, et al. The cortical serotonin2 receptors studied with positron emission tomography and [18F]-setoperone during depressive illness and antidepressant treatment with clomipramine. Biol Psychiatry 1999;45:180-6.
101. Meyer JH, Kapur S, Houle S, et al. Prefrontal cortex 5-HT2 receptors in depression: a [18F] setoperone PET imaging study. Am J Psychiatry 1999;156:1029-34.
102. Meltzer CC, Price JC, Mathis A, et al. PET imaging of serotonin type 2A receptors in late-life neuropsychiatric disorders. Am J Psychiatry 1999;156:1871-8.
103. Yatham LN, Liddle PF, Shiah IS, et al. Brain serotonin2 receptors in major depression: a positron emission tomography study. Arch Gen Psychiatry 2000;57:850-8.
104. Messa C, Colombo C, Moresco RM, et al. 5-HT(2A) receptor binding is reduced in drug-naive and unchanged in SSRI-responder depressed patients compared to healthy controls: a PET study. Psychopharmacology (Berl) 2003;167:72-8.
105. Mintun MA, Sheline YI, Moerlein SM, et al. Decreased hippocampal 5-HT2A receptor binding in major depressive disorder: in vivo measurement with [18F]altanserin positron emission tomography. Biol Psychiatry 2004;55:217-24.
106. Blin J, Pappata S, Kiyosawa M, et al. [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 1988;147:73-82.
107. Blin J, Sette G, Fiorelli M, et al. A method for the in vivo investigation of the serotonergic 5-HT2 receptors in the human cerebral cortex using positron emission tomography and 18F-labeled setoperone. J Neurochem 1990;54:1744-54.
108. Petit-Taboue MC, Landeau B, Osmont A, et al. Estimation of neocortical serotonin-2 receptor binding potential by single-dose fluorine-18-setoperone kinetic PET data analysis. J Nucl Med 1996; 37:95-104.
109. Maziere B, Crouzel C, Venet M, et al. Synthesis, affinity and specificity of 18F- setoperone, a potential ligand for in-vivo imaging of cortical serotonin receptors. Int J Rad Appl Instrum B 1988;15:463-8.
110. Fischman AJ, Bonab AA, Babich JW, et al. Positron emission tomographic analysis of central 5-hydroxytryptamine2 receptor occupancy in healthy volunteers treated with the novel antipsychotic agent ziprasidone. J Pharmacol Exp Ther 1996;279:939-47.
111. Seeman P. Receptor tables vol. 2: Drug dissociation constants for neuroreceptors and transporters. Toronto: SZ Research; 1993.
112. De Keyser J, Clayes A, DeBacker J-P, et al. Autoradiographic localization of D1 and D2 dopamine receptors in the human brain. Neurosci Lett 1988;91:142-7.
113. Trichard C, Paillere-Martinot ML, Attar-Levy D, et al. Binding of antipsychotic drugs to cortical 5-HT2A receptors: a PET study of chlorpromazine, clozapine, and amisulpride in schizophrenic patients. Am J Psychiatry 1998;155:505-8.
114. Kapur S, Zipursky RB, Remington G, et al. 5-HT2 and D2 receptor occupancy of olanzapine in schizophrenia: a PET investigation. Am J Psychiatry 1998;155:921-8.
115. Mamo D, Kapur S, Shammi CM, et al. A PET study of dopamine D2 and serotonin 5-HT2 receptor occupancy in patients with schizophrenia treated with therapeutic doses of ziprasidone. Am J Psychiatry 2004;161:818-25.
116. Kapur S, Jones C, Da Silva J, Wilson A, et al. Reliability of [18F] setoperone in humans. Nucl Med Commun 1997;18:395-9.
117. Blin J, Crouzel C. Blood-cerebrospinal fluid and blood-brain barriers imaged by 18F- labeled metabolites of 18F-setoperone studied in humans using positron emission tomography. J Neurochem 1992; 58:2303-10.
118. Meyer JH, Cho R, Kennedy S, et al. The effects of single dose nefazodone and paroxetine upon 5-HT2A binding potential in humans using [18F]-setoperone PET. Psychopharmacology (Berl) 1999;144: 279-81.
119. Dohr KB, Rush AJ, Bernstein IH. Cognitive Biases and Depression. J Abnorm Psychol 1989;98:263-7.
120. Simons AD, Garfield SL, Murphy GE. The process of change in cognitive therapy and pharmacotherapy for depression. Changes in mood and cognition. Arch Gen Psychiatry 1984;41:45-51.
121. Cane DB, Olinger LJ, Gotlib IH, et al. Factor structure of the dysfunctional attitude scale in a student population. J Clin Psychol 1986;42:307-9.
122. Oliver JM, Baumgart EP. The dysfunctional attitude scale: psychometric properties and relation to depression in an unselected adult population. Cognit Ther Res 1985;9:161-7.
123. Weissman A. The Dysfunctional Attitude Scale: A validation study. Dissertation Abstracts International 1979; 40:1389B-1390B.
124. Bouvard M, Charles S, Guerin J, et al. [Study of Beck's hopelessness scale. Validation and factor analysis]. Encephale 1992;18:237-40.
125. Cannon B, Mulroy R, Otto MW, et al. Dysfunctional attitudes and poor problem solving skills predict hopelessness in major depression. J Affect Disord 1999;55:45-9.
126. DeRubeis RJ, Evans MD, Hollon SD, et al. How does cognitive therapy work? Cognitive change and symptom change in cognitive therapy and pharmacotherapy for depression. J Consult Clin Psychol 1990;58:862-9.
127. Norman WH, Miller W, Dow MG. Characteristics of depressed patients with elevated levels of dysfunctional cognitions. Cognit Ther Res 1988;12:39-51.
128. Beck AT, Steer RA, Kovacs M, et al. Hopelessness and eventual suicide: A 10-year prospective study of patients hospitalized with suicidal ideation. Am J Psychiatry 1985;142:559-63.
129. Beck AT, Brown G, Steer RA. Prediction of eventual suicide in psychiatric inpatients bv clinical ratings of hopelessness. J Consult Clin Psychol 1989;57:309-10.
130. Bhagwagar Z, Hinz R, Taylor M, et al. Increased 5-HT2A Receptor Binding in Euthymic Medication Free Patients Recovered from Depression: A Positron Emission Tomography Study With [11C] MDL 100,907. Am J Psychiatry 2006; 163:1580-7.
131. Boldrinin M, Underwood MD, Martini A, et al. Brainstem raphe nucleus changes in suicide victims. Psychiatr Danub 2006; 18 (Suppl 1):120.
132. Compan V, Segu L, Buhot MC, et al. Differential effects of serotonin (5-HT) lesions and synthesis blockade on neuropeptide-Y immunoreactivity and 5-HT1A, 5-HT1B/1D and 5-HT2A/2C receptor binding sites in the rat cerebral cortex. Brain Res 1998;795: 264-76.
133. McCann UD, Szabo Z, Seckin E, et al. Quantitative PET studies of the serotonin transporter in MDMA users and controls using [11C]McN5652 and [11C]DASB. Neuropsychopharmacology 2005;30: 1741-50.
134. Bernheimer H, Birkmayer W, Hornykiewicz O. [Distribution of 5-hydroxyrryptamine (serotonin) in the human brain and its behavior in patients with Parkinson's syndrome.] Klin Wochenschr 1961;39:1056-9.
135. Kish SJ. What is the evidence that Ecstasy (MDMA) can cause Parkinson's disease? Mov Disord 2003;18:1219-23.
136. Linnet K, Koed K, Wiborg O, et al. Serotonin depletion decreases serotonin transporter mRNA levels in rat brain. Brain Res 1995;697:251-3.
137. Xiao Q, Pawlyk A, Tejani-Butt SM. Reserpine modulates serotonin transporter mRNA levels in the rat brain. Life Sci 1999;64:63-8.
138. Yu A, Yang J, Pawlyk AC, et al. Acute depletion of serotonin down-regulates serotonin transporter mRNA in raphe neurons. Brain Res 1995;688:209-12.
139. Benmansour S, Cecchi M, Morilak D, et al. Effects of Chronic Anti-depressant Treatments on Serotonin Transporter Function, Density and mRNA level. J Neurosci 1999;19:10494-501.
140. Dewar KM, Grondin L, Carli M, et al. [3H]paroxetine binding and serotonin content of rat cortical areas, hippocampus, neostriatum, ventral mesencephalic tegmentum, and midbrain raphe nuclei region following p-chlorophenylalanine and p-chloroamphetamine treatment. J Neurochem 1992;58:250-7.
141. Graham D, Tahraoui L, Langer SZ. Effect of chronic treatment with selective monoamine oxidase inhibitors and specific 5-hydroxytryptamine uptake inhibitors on [3H]paroxetine binding to cerebral cortical membranes of the rat. Neuropharmacology 1987;26: 1087-92.
142. Gordon I, Weizman R, Rehavi M. Modulatory effect of agents active in the presynaptic dopaminergic system on the striatal dopamine transporter. Eur J Pharmacol 1996;298:27-30.
143. Han S, Rowell PP, Carr LA. D2 autoreceptors are not involved in the down-regulation of the striatal dopamine transporter caused by alpha-methyl-p-tyrosine. Res Commun Mol Pathol Pharmacol 1999;104:331-8.
144. Ikawa K, Watanabe A, Kaneno S, et al. Modulation of [3H]mazindol binding sites in rat striatum by dopaminergic agents. Eur J Pharmacol 1993;250:261-6.
145. Kilbourn MR, Sherman PS, Pisani T. Repeated reserpine administration reduces in vivo [18F]GBR 13119 binding to the dopamine uptake site. Eur J Pharmacol 1992;216:109-12.
146. Blier P, De Montigny C. Electrophysiological investigations on the effect of repeated zimelidine administration on serotonergic neurotransmission in the rat. J Neurosci 1983;3:1270-8.
147. Laruelle M. Imaging synaptic neurotransmission with in vivo binding competition techniques: a critical review. J Cereb Blood Flow Metab 2000;20:423-51.
148. Ginovart N, Wilson AA, Meyer JH, et al. [11C]-DASB, a tool for in vivo measurement of SSRI-induced occupancy of the serotonin transporter: PET characterization and evaluation in cats. Synapse 2003;47:123-33.
149. Lundquist P, Wilking H, Hoglund AU, et al. Potential of [11C]DASB for measuring endogenous serotonin with PET: binding studies. Nucl Med Biol 2005;32:129-36.
150. Celada P, Artigas F. Monoamine oxidase inhibitors increase preferentially extracellular 5-hydroxytryptamine in the midbrain raphe nuclei. A brain microdialysis study in the awake rat. Naunyn Schmiedebergs Arch Pharmacol 1993;347:583-90.
151. Malyszko J, Urano T, Serizawa K, et al. Serotonergic measures in blood and brain and their correlations in rats treated with tranylcypromine, a monoamine oxidase inhibitor. Jpn J Physiol 1993;43:613-26.
152. Ferrer A, Artigas F. Effects of single and chronic treatment with tranylcypromine on extracellular serotonin in rat brain. Eur J Pharmacol 1994;263:227-34.
153. Talbot PS, Frankle WG, Hwang DR, et al. Effects of reduced endogenous 5-HT on the in vivo binding of the serotonin transporter radioligand 11C-DASB in healthy humans. Synapse 2005;55:164-75.
154. Bligh-Glover W, Kolli TN, Shapiro-Kulnane L, et al. The serotonin transporter in the midbrain of suicide victims with major depression. Biol Psychiatry 2000;47:1015-24.
155. Klimek V, Roberson G, Stockmeier CA, et al. Serotonin transporter and MAO-B levels in monoamine nuclei of the human brainstem are normal in major depression. J Psychiatr Res 2003;37:387-97.
156. Perry EK, Marshall EF, Blessed G, et al. Decreased imipramine binding in the brains of patients with depressive illness. Br J Psychiatry 1983;142:188-92.
157. Crow TJ, Cross AJ, Cooper SJ, et al. Neurotransmitter receptors and monoamine metabolites in the brains of patients with Alzheimer-type dementia and depression, and suicides. Neuropharmacology 1984;23(12B):1561-9.
158. Mann JJ, Huang YY, Underwood MD, et al. A serotonin transporter gene promoter polymorphism (5-HTTLPR) and prefrontal cortical binding in major depression and suicide. Arch Gen Psychiatry 2000;57:729-38.
159. Austin MC, Whitehead RE, Edgar CL, et al. Localized decrease in serotonin transporter-immunoreactive axons in the prefrontal cortex of depressed subjects committing suicide. Neuroscience 2002; 114:807-15.
160. Hrdina PD, Foy B, Hepner A, et al. Antidepressant binding sites in brain: autoradiographic comparison of [3H]paroxetine and [3H]imipramine localization and relationship to serotonin transporter. J Pharmacol Exp Ther 1990;252:410-8.
161. Lawrence KM, De Paermentier F, Cheetham SC, et al. Brain 5-HT uptake sites, labelled with [3H]paroxetine, in antidepressant-free depressed suicides. Brain Res 1990;526:17-22.
162. Little KY, McLauglin DP, Ranc J, et al. Serotonin transporter binding sites and mRNA levels in depressed persons committing suicide. Biol Psychiatry 1997;41:1156-64.
163. Arango V, Underwood MD, Boldrini M, et al. Serotonin 1A receptors, serotonin transporter binding and serotonin transporter mRNA expression in the brainstem of depressed suicide victims. Neuropsychopharmacology 2001;25:892-903.
164. Hendricksen M, Thomas AJ, Ferrier IN, et al. Neuropathological study of the dorsal raphe nuclei in late-life depression and Alzheimer's disease with and without depression. Am J Psychiatry 2004;161:1096-102.
165. Leake A, Fairbairn AF, McKeith IG, et al. Studies on the serotonin uptake binding site in major depressive disorder and control postmortem brain: neurochemical and clinical correlates. Psychiatry Res 1991;39:155-65.
166. Malison RT, Price LH, Berman R, et al. Reduced brain serotonin transporter availability in major depression as measured by [123I]-2 beta-carbomethoxy-3 beta-(4-iodophenyl)tropane and single photon emission computed tomography. Biol Psychiatry 1998;44:1090-8.
167. Newberg AB, Amsterdam JD, Wintering N, et al. 123I-ADAM binding to serotonin transporters in patients with major depression and healthy controls: a preliminary study. J Nucl Med 2005;46:973-7.
168. Parsey RV, Hastings RS, Oquendo MA, et al. Lower serotonin transporter binding potential in the human brain during major depressive episodes. Am J Psychiatry 2006;163:52-8.
169. Herold N, Uebelhack K, Franke L, et al. Imaging of serotonin transporters and its blockade by citalopram in patients with major depression using a novel SPECT ligand [(123)I]-ADAM. J Neural Transm 2006;113:659-70.
170. Meyer JH, Houle S, Sagrati S, et al. Brain serotonin transporter binding
171. Lesch KP, Bengel D, Heils A, et al. Association of anxiety-related traits with a polymorphism in the serotonin transporter gene regulatory region. Science 1996;274:1527-31.
172. Filipenko ML, Beilina AG, Alekseyenko OV, et al. Increase in expression of brain serotonin transporter and monoamine oxidase a genes induced by repeated experience of social defeats in male mice. Biochemistry (Mosc) 2002;67:451-5.
173. Little KY, McLaughlin DP, Zhang L, et al. Cocaine, ethanol, and genotype effects on human midbrain serotonin transporter binding sites and mRNA levels. Am J Psychiatry 1998;155:207-13.
174. Heinz A, Jones DW, Mazzanti C, et al. A relationship between serotonin transporter genotype and in vivo protein expression and alcohol neurotoxicity. Biol Psychiatry 2000;47:643-9.
175. Willeit M, Stastny J, Pirker W, et al. No evidence for in vivo regulation of midbrain serotonin transporter availability by serotonin transporter promoter gene polymorphism. Biol Psychiatry 2001;50:8-12.
176. Shioe K, Ichimiya T, Suhara T, et al. No association between genotype of the promoter region of serotonin transporter gene and serotonin transporter binding in human brain measured by PET. Synapse 2003;48:184-8.
177. Parsey RV, Hastings RS, Oquendo MA, et al. Effect of a triallelic functional polymorphism of the serotonin-transporter-linked promoter region on expression of serotonin transporter in the human brain. Am J Psychiatry 2006;163:48-51.
178. Lim JE, Papp A, Pinsonneault J, et al. Allelic expression of serotonin transporter (SERT) mRNA in human pons: lack of correlation with the polymorphism SERTLPR. Mol Psychiatry 2006;11:649-62.
179. Kim DK, Lim SW, Lee S, et al. Serotonin transporter gene polymorphism and antidepressant response. Neuroreport 2000;11:215-9.
180. Zanardi R, Benedetti F, Di Bella D, et al. Efficacy of paroxetine in depression is influenced by a functional polymorphism within the promoter of the serotonin transporter gene. J Clin Psychopharmacol 2000;20:105-7.
181. Pollock BG, Ferrell RE, Mulsant BH, et al. Allelic variation in the serotonin transporter promoter affects onset of paroxetine treatment response in late-life depression. Neuropsychopharmacology 2000;23:587-90.
182. Kraft JB, Slager SL, McGrath PJ, et al. Sequence analysis of the serotonin transporter and associations with antidepressant response. Biol Psychiatry 2005;58:374-81.
183. Caspi A, Sugden K, Moffitt TE, et al. Influence of life stress on depression: moderation by a polymorphism in the 5-HTT gene. Science 2003;301:386-9.
184. Faravelli C, Ambonetti A, Pallanti S, et al. Depressive relapses and incomplete recovery from index episode. Am J Psychiatry 1986;143:888-91.
185. Georgotas A, McCue RE, Cooper TB, et al. How effective and safe is continuation therapy in elderly depressed patients? Factors affecting relapse rate. Arch Gen Psychiatry 1988;45:929-32.
186. Paykel ES, Ramana R, Cooper Z, et al. Residual symptoms after partial remission: an important outcome in depression. Psychol Med 1995;25:1171-80.
187. Paykel ES, Scott J, Teasdale JD, et al. Prevention of relapse in residual depression by cognitive therapy: a controlled trial. Arch Gen Psychiatry 1999;56:829-35.
188. Cannon DM, Ichise M, Fromm SJ, et al. Serotonin transporter binding in bipolar disorder assessed using [11C]DASB and positron emission tomography. Biol Psychiatry 2006;60:207-17.
189. Takano A, Suzuki K, Kosaka J, et al. A dose-finding study of duloxetine based on serotonin transporter occupancy. Psychopharmacology (Berl) 2006;185:395-9.
190. Parsey RV, Kent JM, Oquendo MA, et al. Acute occupancy of brain serotonin transporter by sertraline as measured by [11C]DASB and positron emission tomography. Biol Psychiatry 2006;59:821-8.
191. Fineberg NA, Gale TM. Evidence-based pharmacotherapy of obsessive-compulsive disorder. Int J Neuropsychopharmacol 2005;8:107-29.