Ex vivo assessment of binding site occupancy of monoamine reuptake inhibitors: Methodology and biological significance

Neuropharmacology

Volumn 55, Issue 1, 2008, Pages 63-70

  Lengyel, Kelly ^a   Pieschl, Rick ^a   Strong, Todd ^a   Molski, Thaddeus ^a   Mattson, Gail ^a   Lodge, Nicholas J ^a   Li, Yu Wen ^a  

^a BRISTOL MYERS SQUIBB   (United States)

Author keywords

Dopamine; Ex vivo; Monoamine transporter; Norepinephrine; Occupancy; Radioligand binding; Reuptake inhibitor; Serotonin

Indexed keywords

1 [2 (BENZHYDRYLOXY)ETHYL] 4 (3 PHENYLPROPYL)PIPERAZINE; 3BETA (4 IODOPHENYL) 2BETA TROPANECARBOXYLIC ACID METHYL ESTER; AMFEBUTAMONE; CITALOPRAM; DOPAMINE TRANSPORTER; DOV 216303; DOV 21947; DULOXETINE; FLUOXETINE; INDATRALINE; IODINE 125; MONOAMINE; NISOXETINE; NOMIFENSINE; NORADRENALIN TRANSPORTER; NORADRENALIN UPTAKE INHIBITOR; RADIOLIGAND; REBOXETINE; SEROTONIN NORADRENALIN REUPTAKE INHIBITOR; SEROTONIN TRANSPORTER; SEROTONIN UPTAKE INHIBITOR; TRITIUM; VENLAFAXINE; WIN 35426;

ACCURACY; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; AUTORADIOGRAPHY; BINDING AFFINITY; BINDING ASSAY; BINDING SITE; BRAIN HOMOGENATE; CONTROLLED STUDY; CORRELATION ANALYSIS; DISSOCIATION; EX VIVO STUDY; HIGH THROUGHPUT SCREENING; IN VITRO STUDY; LIGAND BINDING; MALE; NEUROIMAGING; NONHUMAN; PRIORITY JOURNAL; RAT; TEMPERATURE;

ANIMALS; AUTORADIOGRAPHY; BINDING SITES; BRAIN; BRAIN MAPPING; DOSE-RESPONSE RELATIONSHIP, DRUG; MALE; MEMBRANE TRANSPORT PROTEINS; NEUROTRANSMITTER UPTAKE INHIBITORS; PROTEIN BINDING; RADIOISOTOPES; RATS; RATS, SPRAGUE-DAWLEY; TIME FACTORS; TISSUE DISTRIBUTION;

EID: 45649085042     PISSN: 00283908     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.neuropharm.2008.04.014     Document Type: Article

References (39)

1. Basso A.M., Gallagher K.B., Bratcher N.A., Brioni J.D., Moreland R.B., Hsieh G.C., Drescher K., Fox G.B., Decker M.W., and Rueter L.E. Antidepressant-like effect of D (2/3) receptor, but not D(4) receptor-activation in the rat forced swim test. Neuropsychopharmacology 30 (2005) 1257-1268
2. 3H]desmethylimipramine binding sites in rat brain by quantitative autoradiography. J. Neurosci. 3 (1983) 1069-1076
3. Bymaster F.P., Dreshfield-Ahmad L.J., Threlkeld P.G., Shaw J.L., Thompson L., Nelson D.L., Hemrick-Luecke S.K., and Wong D.T. Comparative affinity of duloxetine and venlafaxine for serotonin and norepinephrine transporters in vitro and in vivo, human serotonin receptor subtypes, and other neuronal receptors. Neuropsychopharmacology 25 (2001) 871-880
4. Bymaster F.P., Katner J.S., Nelson D.L., Hemrick-Luecke S.K., Threlkeld P.G., Heiligenstein J.H., Morin S.M., Gehlert D.R., and Perry K.W. Atomoxetine increases extracellular levels of norepinephrine and dopamine in prefrontal cortex of rat: a potential mechanism for efficacy in attention deficit/hyperactivity disorder. Neuropsychopharmacology 27 (2002) 699-711
5. 50) of an enzymatic reaction. Biochem. Pharmacol. 22 (1973) 3099-3108
6. D'Amato R.J., Largent B.L., Snowman A.M., and Snyder S.H. Selective labeling of serotonin uptake sites in rat brain by [3H]citalopram contrasted to labeling of multiple sites by [3H]imipramine. J. Pharmacol. Exp. Ther. 242 (1987) 364-371
7. Duffy R.A., Varty G.B., Morgan C.A., and Lachowicz J.E. Correlation of neurokinin (NK) 1 receptor occupancy in gerbil striatum with behavioral effects of NK1 antagonists. J. Pharmacol. Exp. Ther. 301 (2002) 536-542
8. Gorka Z., Earley B., and Leonard B.E. Effect of bilateral olfactory bulbectomy in the rat, alone or in combination with antidepressants, on the learned immobility model of depression. Neuropsychobiology 13 (1985) 26-30
9. Hayes P.E., and Kristoff C.A. Adverse reactions to five new antidepressants. Clin. Pharm. 5 (1986) 471-480
10. Hirano K., Kimura R., Sugimoto Y., Yamada J., Uchida S., Kato Y., Hashimoto H., and Yamada S. Relationship between brain serotonin transporter binding, plasma concentration and behavioural effect of selective serotonin reuptake inhibitors. Br. J. Pharmacol. 144 (2005) 695-702
11. Kametani H., Nomura S., and Shimizu J. The reversal effect of antidepressants on the escape deficit induced by inescapable shock in rats. Psychopharmacology (Berl.) 80 (1983) 206-208
12. Kapur S., Barlow K., VanderSpek S.C., Javanmard M., and Nobrega J.N. Drug-induced receptor occupancy: substantial differences in measurements made in vivo vs ex vivo. Psychopharmacology (Berl.) 157 (2001) 168-171
13. Kent J.M., Coplan J.D., Lombardo I., Hwang D.R., Huang Y., Mawlawi O., Van Heertum R.L., Slifstein M., Abi-Dargham A., Gorman J.M., and Laruelle M. 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.) 164 (2002) 341-348
14. Koch S., Hemrick-Luecke S.K., Thompson L.K., Evans D.C., Threlkeld P.G., Nelson D.L., Perry J.W., and Bymaster F.P. Comparison of effects of dual transporter inhibitors on monoamine transporters and extracellular levels in rats. Neuropharmacology 45 (2003) 935-944
15. Langlois X., Riele P., Wintmolders C., Leysen J.E., and Jurzak M. Use of the beta-imager for rapid ex vivo autoradiography exemplified with central nervous system penetrating neurokinin 3 antagonists. J. Pharmacol. Exp. Ther. 299 (2001) 712-717
16. Larsen A.K., Brennum L.T., Egebjerg J., Sanchez C., Halldin C., and Andersen P.H. Selectivity of (3)H-MADAM binding to 5-hydroxytryptamine transporters in vitro and in vivo in mice; correlation with behavioural effects. Br. J. Pharmacol. 141 (2004) 1015-1023
17. Lavretsky H., Kim M.D., Kumar A., and Reynolds C.F. Combined treatment with methylphenidate and citalopram for accelerated response in the elderly: an open trial. J. Clin. Psychiatry 64 (2003) 1410-1414
18. Lavretsky H., and Nguyen L.H. Innovations: geriatric psychiatry: diagnosis and treatment of neuropsychiatric symptoms in Alzheimer's disease. Psychiatr. Serv. 57 (2006) 617-619
19. Learned-Coughlin S.M., Bergstrom M., Savitcheva I., Ascher J., Schmith V.D., and Langstrom B. In vivo activity of bupropion at the human dopamine transporter as measured by positron emission tomography. Biol. Psychiatry 54 (2003) 800-805
20. Li J., Fish R.L., Cook S.M., Tattersall F.D., and Atack J.R. Comparison of in vivo and ex vivo [3H]flumazenil binding assays to determine occupancy at the benzodiazepine binding site of rat brain GABAA receptors. Neuropharmacology 51 (2006) 168-172
21. Li S.X., Perry K.W., and Wong D.T. Influence of fluoxetine on the ability of bupropion to modulate extracellular dopamine and norepinephrine concentrations in three mesocorticolimbic areas of rats. Neuropharmacology 42 (2002) 181-190
22. Little K.Y., Carroll F.I., and Cassin B.J. Characterization and localization of [125I]RTI-121 binding sites in human striatum and medial temporal lobe. J. Pharmacol. Exp. Ther. 274 (1995) 1473-1483
23. Masand P.S., Anand V.S., and Tanquary J.F. Psychostimulant augmentation of second generation antidepressants: a case series. Depress. Anxiety 7 (1998) 89-91
24. Meyer J.H., Goulding V.S., Wilson A.A., Hussey D., Christensen B.K., and Houle S. Bupropion occupancy of the dopamine transporter is low during clinical treatment. Psychopharmacology (Berl.) 163 (2002) 102-105
25. Meyer J.H., Wilson A.A., Sagrati S., Hussey D., Carella A., Potter W.Z., Ginovart N., Spencer E.P., Cheok A., and Houle S. Serotonin transporter occupancy of five selective serotonin reuptake inhibitors at different doses: an [11C]DASB positron emission tomography study. Am. J. Psychiatry 161 (2004) 826-835
26. Millan M.J., Gobert A., Lejeune F., Newman-Tancredi A., Rivet J.M., Auclair A., and Peglion J.L. S33005, a novel ligand at both serotonin and norepinephrine transporters: I. Receptor binding, electrophysiological, and neurochemical profile in comparison with venlafaxine, reboxetine, citalopram, and clomipramine. J. Pharmacol. Exp. Ther. 298 (2001) 565-580
27. Nelson J.C., and Charney D.S. The symptoms of major depressive illness. Am. J. Psychiatry 138 (1981) 1-13
28. Papakostas G.I., Worthington III J.J., Iosifescu D.V., Kinrys G., Burns A.M., Fisher L.B., Homberger C.H., Mischoulon D., and Fava M. The combination of duloxetine and bupropion for treatment-resistant major depressive disorder. Depress. Anxiety 23 (2006) 178-181
29. Parsey R.V., Kent J.M., Oquendo M.A., Richards M.C., Pratap M., Cooper T.B., Arango V., and Mann J.J. Acute occupancy of brain serotonin transporter by sertraline as measured by [11C]DASB and positron emission tomography. Biol. Psychiatry 59 (2006) 821-828
30. Reneric J.P., and Lucki I. Antidepressant behavioral effects by dual inhibition of monoamine reuptake in the rat forced swimming test. Psychopharmacology (Berl.) 136 (1998) 190-197
31. Skolnick P., Popik P., Janowsky A., Beer B., and Lippa A.S. Antidepressant-like actions of DOV 21,947: a "triple" reuptake inhibitor. Eur. J. Pharmacol. 461 (2003) 99-104
32. Skolnick P., Popik P., Janowsky A., Beer B., and Lippa A.S. Broad spectrum" antidepressants: is more better for the treatment of depression?. Life Sci. 73 (2003) 3175-3179 Review
33. Skolnick P., Krieter P., Tizzano J., Basile A., Popik P., Czobor P., and Lippa A. Preclinical and clinical pharmacology of DOV 216,303, a "triple" reuptake inhibitor. CNS Drug Rev. 2 (2006) 123-134
34. Statnick M.A., Tinsley F.C., Eastwood B.J., Suter T.M., Mitch C.H., and Heiman M.L. Peptides that regulate food intake: antagonism of opioid receptors reduces body fat in obese rats by decreasing food intake and stimulating lipid utilization. Am. J. Physiol. Regul. Integr. Comp. Physiol. 284 (2003) R1399-R1408
35. Suhara T., Takano A., Sudo Y., Ichimiya T., Inoue M., Yasuno F., Ikoma Y., and Okubo Y. High levels of serotonin transporter occupancy with low-dose clomipramine in comparative occupancy study with fluvoxamine using positron emission tomography. Arch. Gen. Psychiatry 60 (2003) 386-391
36. Szabo Z., Argyelan M., Kanyo B., Pavics L., and Janka Z. Change of dopamine transporter activity (DAT) during the action of bupropion (in depression). Neuropsychopharmacol. Hung. 6 (2004) 79-81
37. Takano A., Suzuki K., Kosaka J., Ota M., Nozaki S., Ikoma Y., Tanada S., and Suhara T. A dose-finding study of duloxetine based on serotonin transporter occupancy. Psychopharmacology (Berl.) 185 (2006) 395-399
38. Talbot P.S., and Laruelle M. The role of in vivo molecular imaging with PET and SPECT in the elucidation of psychiatric drug action and new drug development. Eur. Neuropsychopharmacol. 12 (2002) 503-511
39. Volkow N.D., Volkow G.J., Wang J.S., Fowler S.J., Gatley J., and LoganDing Y.S. Dopamine transporter occupancies in the human brain induced by therapeutic doses of oral methylphenidate. Am. J. Psychiatry 155 (1998) 1325-1331