Effects of olanzapine and betahistine co-treatment on serotonin transporter, 5-HT2A and dopamine D2 receptor binding density

Progress in Neuro-Psychopharmacology and Biological Psychiatry

Volumn 47, Issue , 2013, Pages 62-68

  Lian, Jiamei ^a   Huang, Xu Feng ^a,b   Pai, Nagesh ^a   Deng, Chao ^a,b  

^a UNIVERSITY OF WOLLONGONG   (Australia)

^b SCHIZOPHRENIA RESEARCH INSTITUTE   (Australia)

Author keywords

5 HT transporter; 5 HT2A receptor; Betahistine; Dopamine D2 receptor; Olanzapine; Receptor binding

Indexed keywords

BETAHISTINE; DOPAMINE 2 RECEPTOR; KETANSERIN; OLANZAPINE; PAROXETINE; RACLOPRIDE; SEROTONIN 2A RECEPTOR; SEROTONIN TRANSPORTER;

ANIMAL TISSUE; ARTICLE; AUTORADIOGRAPHY; BRAIN REGION; CINGULATE GYRUS; DRUG BINDING SITE; DRUG EFFICACY; DRUG RECEPTOR BINDING; FEMALE; NONHUMAN; NUCLEUS ACCUMBENS; PREFRONTAL CORTEX; RAT; SPRAGUE DAWLEY RAT; SUBSTANTIA NIGRA; VENTRAL TEGMENTUM;

5-HT; 5-HT TRANSPORTER; 5-HT(2A) RECEPTOR; 5-HT(2A)R; 5-HTT; ANALYSIS OF VARIANCE; ANOVA; BETAHISTINE; CAUDATE PUTAMEN; CG; CINGULATE CORTEX; CPU; D(2)R; DOPAMINE D(2) RECEPTOR; EPS; EXTRAPYRAMIDAL SYMPTOMS; FGAS; FIRST GENERATION ANTIPSYCHOTIC DRUGS; H(1)R; H(3)R; HISTAMINE H(1) RECEPTOR; HISTAMINE H(3) RECEPTOR; M(1) RECEPTOR; M(1)R; NACC; NACS; NUCLEUS ACCUMBENS, CORE; NUCLEUS ACCUMBENS, SHELL; OLANZAPINE; PFC; PREFRONTAL CORTEX; RECEPTOR BINDING; ROOM TEMPERATURE; RT; SECOND GENERATION ANTIPSYCHOTIC DRUGS; SEROTONIN; SEROTONIN (2A) RECEPTOR; SEROTONIN TRANSPORTER; SGAS; SN; SUBSTANTIA NIGRA; VENTRAL TEGMENTAL AREA; VTA; Α(1-2) RECEPTOR; Α(1-2)R;

ANIMALS; ANTIPSYCHOTIC AGENTS; AUTORADIOGRAPHY; BENZODIAZEPINES; BETAHISTINE; BRAIN; BRAIN MAPPING; DRUG COMBINATIONS; FEMALE; PROTEIN BINDING; RATS; RATS, SPRAGUE-DAWLEY; RECEPTOR, SEROTONIN, 5-HT2A; RECEPTORS, DOPAMINE D2; SEROTONIN PLASMA MEMBRANE TRANSPORT PROTEINS;

EID: 84883744693     PISSN: 02785846     EISSN: 18784216     Source Type: Journal    
DOI: 10.1016/j.pnpbp.2013.08.005     Document Type: Article

References (70)

1. Allison D., Mentore J., Heo M., Chandler L., Cappelleri J., Infante M., et al. Antipsychotic-induced weight gain: a comprehensive research synthesis. Am J Psychiatry 1999, 156:1686-1696.
2. Aravagiri M., Teper Y., Marder S.R. Pharmacokinetics and tissue distribution of olanzapine in rats. Biopharm Drug Dispos 1999, 20:369-377.
3. Bortolozzi A., Masana M., Diaz-Mataix L., Cortes R., Scorza M.C., Gingrich J.A., et al. Dopamine release induced by atypical antipsychotics in prefrontal cortex requires 5-HT(1A) receptors but not 5-HT(2A) receptors. Int J Neuropsychopharmacol 2010, 13:1299-1314.
4. Bozina N., Medved V., Kuzman M.R., Sain I., Sertic J. Association study of olanzapine-induced weight gain and therapeutic response with SERT gene polymorphisms in female schizophrenic patients. J Psychopharmacol 2007, 21:728-734.
5. Center for Drug Evaluation and Research FDA Estimating the safe starting dose in clinical trials for therapeutics in adult healthy volunteers 2005, U.S. FDA Center for Drug Evaluation and Research.
6. Choi S., DiSilvio B., Unangst J., Fernstrom J.D. Effect of chronic infusion of olanzapine and clozapine on food intake and body weight gain in male and female rats. Life Sci 2007, 81:1024-1030.
7. Cohen B.M., Cherkerzian S., Ma J., Ye N., Wager C., Lange N. Cells in midline thalamus, central amygdala, and nucleus accumbens responding specifically to antipsychotic drugs. Psychopharmacology 2003, 167:403-410.
8. Correll C.U., Lencz T., Malhotra A.K. Antipsychotic drugs and obesity. Trends Mol Med 2011, 17:97-107.
9. 2 receptors in the dorsal vagal complex of rats. Prog Neuropsychopharmacol Biol Psychiatry 2007, 31:915-920.
10. 3 receptors in food intake: a mechanism for atypical antipsychotic-induced weight gain?. Prog Neuropsychopharmacol Biol Psychiatry 2010, 34:1-4.
11. Deng C., Lian J., Pai N., Huang X.F. Reducing olanzapine-induced weight gain side-effect by betahistine: a study in the rat model. J Psychopharmacol 2012, 26:1271-1279.
12. du Bois T.M., Deng C., Bell W., Huang X.F. Fatty acids differentially affect serotonin receptor and transporter binding in the rat brain. Neuroscience 2006, 139:1397-1403.
13. du Bois T.M., Hsu C.-W., Li Y., Tan Y.Y., Deng C., Huang X.-F. Altered dopamine receptor and dopamine transporter binding and tyrosine hydroxylase mRNA expression following perinatal NMDA receptor blockade. Neurochem Res 2008, 33:1224-1231.
14. Gebhardt S., Haberhausen M., Heinzel-Gutenbrunner M., Gebhardt N., Remschmidt H., Krieg J.-C., et al. Antipsychotic-induced body weight gain: predictors and a systematic categorization of the long-term weight course. J Psychiatr Res 2009, 43:620-626.
15. Goudie A.J., Smith J., Halford J. Characterization of olanzapine-induced weight gain in rats. J Psychopharmacol 2002, 16:291-296.
16. 1 receptor expression. Psychoneuroendocrinology 2008, 33:569-580.
17. Han M., Newell K., Zavitsanou K., Deng C., Huang X.-F. Effects of antipsychotic medication on muscarinic M1 receptor mRNA expression in the rat brain. J Neurosci Res 2008, 86:457-464.
18. Han M., Huang X.F., Deng C. Aripiprazole differentially affects mesolimbic and nigrostriatal dopaminergic transmission: implications for long-term drug efficacy and low extrapyramidal side-effects. Int J Neuropsychopharmacol 2009, 12:941-952.
19. Han M., Huang X.F., du Bois T.M., Deng C. The effects of antipsychotic drugs administration on 5-HT1A receptor expression in the limbic system of the rat brain. Neuroscience 2009, 164:1754-1763.
20. He M., Deng C., Huang X.-F. The role of hypothalamic H1 receptor antagonism in antipsychotic-induced weight gain. CNS Drugs 2013, 27:423-434. 10.1007/s40263-013-0062-1.
21. Horacek J., Bubenikova-Valesova V., Kopecek M., Palenicek T., Dockery C., Mohr P., et al. Mechanism of action of atypical antipsychotic drugs and the neurobiology of schizophrenia. CNS Drugs 2006, 20:389-409.
22. 2C receptor mRNA expression in the rat brain. Behav Brain Res 2006, 171:355-362.
23. Huang X.-F., Zavitsanou K., Huang X., Yu Y., Wang H., Chen F., et al. Dopamine transporter and D2 receptor binding densities in mice prone or resistant to chronic high fat diet-induced obesity. Behav Brain Res 2006, 175:415-419.
24. Ichikawa J., Ishii H., Bonaccorso S., Fowler W.L., O'Laughlin I.A., Meltzer H.Y. 5-HT(2A) and D(2) receptor blockade increases cortical DA release via 5-HT(1A) receptor activation: a possible mechanism of atypical antipsychotic-induced cortical dopamine release. J Neurochem 2001, 76:1521-1531.
25. Kang K., Huang X.F., Wang Q., Deng C. Decreased density of serotonin 2A receptors in the superior temporal gyrus in schizophrenia-a postmortem study. Prog Neuropsychopharmacol Biol Psychiatry 2009, 33:867-871.
26. 2 receptors. Prog Neuropsychopharmacol Biol Psychiatry 2003, 27:1081-1090.
27. Kapur S., Zipursky R.B., Remington G. Clinical and theoretical implications of 5-HT2 and D2 receptor occupancy of clozapine, risperidone, and olanzapine in schizophrenia. Am J Psychiatry 1999, 156:286-293.
28. Kesby J.P., O'Loan J.C., Alexander S., Deng C., Huang X.F., McGrath J.J., et al. Developmental vitamin D deficiency alters MK-801-induced behaviours in adult offspring. Psychopharmacology 2012, 220:455-463.
29. 1 receptor-linked activation of hypothalamic AMP-kinase. Proc Natl Acad Sci 2007, 104:3456-3459.
30. Kuroki T., Nagao N., Nakahara T. Neuropharmacology of second-generation antipsychotic drugs: a validity of the serotonin-dopamine hypothesis. Progress in brain research 2008, vol. 172:199-212. Elsevier. V.D.M. Giuseppe Di Giovann, E. Ennio (Eds.).
31. Kusumi I., Takahashi Y., Suzuki K., Kameda K., Koyama T. Differential effects of subchronic treatments with atypical antipsychotic drugs on dopamine D2 and serotonin 5-HT2A receptors in the rat brain. J Neural Transm 2000, 107:295-302.
32. Lambert T. Managing the metabolic adverse effects of antipsychotic drugs in patients with psychosis. Aust Prescr 2011, 34:97-99.
33. Li X.M., Perry K.W., Wong D.T., Bymaster F.P. Olanzapine increases in vivo dopamine and norepinephrine release in rat prefrontal cortex, nucleus accumbens and striatum. Psychopharmacology 1998, 136:153-161.
34. Marcus M.M., Nomikos G.G., Svensson T.H. Effects of atypical antipsychotic drugs on dopamine output in the shell and core of the nucleus accumbens: role of 5-HT(2A) and alpha(1)-adrenoceptor antagonism. Eur Neuropsychopharmacol 2000, 10:245-253.
35. Mata-Pastor I., Arranz-Calderon M.J., Beperet-Urmeneta M., Perez-Nievas F., Sham P., Kerwin R. Influence of serotonergic transmission on response to olanzapine. Actas Esp Psiquiatr 2002, 30:265-271.
36. Matsumoto M., Hidaka K., Tada S., Tasaki Y., Yamaguchi T. Low levels of mRNA for dopamine D4 receptor in human cerebral cortex and striatum. J Neurochem 1996, 66:915-919.
37. Meltzer H.Y., Massey B.W. The role of serotonin receptors in the action of atypical antipsychotic drugs. Curr Opin Pharmacol 2011, 11:59-67.
38. Meltzer H.Y., Li Z., Kaneda Y., Ichikawa J. Serotonin receptors: their key role in drugs to treat schizophrenia. Prog Neuropsychopharmacol Biol Psychiatry 2003, 27:1159-1172.
39. Millan M.J., Marin P., Bockaert J., Mannoury la Cour C. Signaling at G-protein-coupled serotonin receptors: recent advances and future research directions. Trends Pharmacol Sci 2008, 29:454-464.
40. Nasrallah Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry 2008, 13:27-35.
41. Paxinos G., Watson C. The rat brain in stereotaxic coordinates 2007, Academic Press.
42. 3 antagonist, on olanzapine-induced weight gain in first-episode schizophrenia patients. Int Clin Psychopharmacol 2005, 20:101-103.
43. Poyurovsky M., Fuchs C., Pashinian A., Levi A., Weizman R., Weizman A. Reducing antipsychotic-induced weight gain in schizophrenia: a double-blind placebo-controlled study of reboxetine-betahistine combination. Psychopharmacology 2013, 226:615-622.
44. Reagan-Shaw S., Nihal M., Ahmad N. Dose translation from animal to human studies revisited. FASEB J 2008, 22:659-661.
45. Remington G., Mann S., McCormick P., Nobrega J.N., Hahn M., Natesan S. Modeling chronic olanzapine exposure using osmotic minipumps: pharmacological limitations. Pharmacol Biochem Behav 2011, 100:86-89.
46. Richelson E., Souder T. Binding of antipsychotic drugs to human brain receptors: focus on newer generation compounds. Life Sci 2000, 68:29-39.
47. Scarr E., Pavey G., Copolov D., Dean B. Hippocampal 5-hydroxytryptamine receptors: abnormalities in postmortem brain from schizophrenic subjects. Schizophr Res 2004, 71:383-392.
48. Seeman M.V. Secondary effects of antipsychotics: women at greater risk than men. Schizophr Bull 2009, 35:937-948.
49. Seeman P. All roads to schizophrenia lead to dopamine supersensitivity and elevated dopamine D2(high) receptors. CNS Neurosci Ther 2011, 17:118-132.
50. Seeman P., Schwarz J., Chen J.-F., Szechtman H., Perreault M., McKnight G.S., et al. Psychosis pathways converge via D2high dopamine receptors. Synapse 2006, 60:319-346.
51. Stahl S. Describing an atypical antipsychotic: receptor binding and its role in pathophysiology. Prim Care Companion J Clin Psychiatry 2003, 5:9-13.
52. Stahl S., Meyer J., Mignon L. Which comes first: atypical antipsychotic treatment or cardiometabolic risk?. Acta Psychiatr Scand 2009, 119:171-179.
53. Steward L.J., Kennedy M.D., Morris B.J., Pratt J.A. The atypical antipsychotic drug clozapine enhances chronic PCP-induced regulation of prefrontal cortex 5-HT2A receptors. Neuropharmacology 2004, 47:527-537.
54. Strange P. Antipsychotic drug action: antagonism, inverse agonism or partial agonism. Trends Pharmacol Sci 2008, 29:314-321.
55. Szelag A., Trocha M., Merwid-Lad A. Betahistine inhibits food intake in rats. Pol J Pharmacol 2001, 53:701-707.
56. Tarazi F.I., Florijn W.J., Creese I. Differential regulation of dopamine receptors after chronic typical and atypical antipsychotic drug treatment. Neuroscience 1997, 78:985-996.
57. Tarazi F.I., Zhang K., Baldessarini R.J. Long-term effects of olanzapine, risperidone, and quetiapine on dopamine receptor types in regions of rat brain: implications for antipsychotic drug treatment. J Pharmacol Exp Ther 2001, 297:711-717.
58. Tarazi F.I., Zhang K., Baldessarini R.J. Long-term effects of olanzapine, risperidone, and quetiapine on serotonin 1A, 2A and 2C receptors in rat forebrain regions. Psychopharmacology 2002, 161:263-270.
59. Tauscher J., Jones C., Remington G., Zipursky R.B., Kapur S. Significant dissociation of brain and plasma kinetics with antipsychotics. Mol Psychiatry 2002, 7:317-321.
60. Treuer T., Pendlebury J., Lockman H., Bushe C., Karagianis J., Raskin J., et al. Weight gain risk factor assessment checklist: overview and recommendation for use. Neuroendocrinol Lett 2011, 32:199-205.
61. Uchida S., Kato Y., Hirano K., Kagawa Y., Yamada S. Brain neurotransmitter receptor-binding characteristics in rats after oral administration of haloperidol, risperidone and olanzapine. Life Sci 2007, 80:1635-1640.
62. Van Oekelen D., Luyten W.H., Leysen J.E. 5-HT2A and 5-HT2C receptors and their atypical regulation properties. Life Sci 2003, 72:2429-2449.
63. Vazquez-Bourgon J., Arranz M.J., Mata I., Pelayo-Teran J.M., Perez-Iglesias R., Medina-Gonzalez L., et al. Serotonin transporter polymorphisms and early response to antipsychotic treatment in first episode of psychosis. Psychiatry Res 2010, 175:189-194.
64. Volk D. Prefrontal cortical circuits in schizophrenia. Curr Top Behav Neurosci 2010, 4:485-508.
65. Volkow N.D., Wang G.J., Baler R.D. Reward, dopamine and the control of food intake: implications for obesity. Trends Cogn Sci 2011, 15:37-46.
66. Weston-Green K., Huang X.-F., Deng C. Sensitivity of the female rat to olanzapine-induced weight gain-far from the clinic?. Schizophr Res 2010, 116:299-300.
67. Weston-Green K., Huang X.-F., Deng C. Olanzapine treatment and metabolic dysfunction: a dose response study in female Sprague Dawley rats. Behav Brain Res 2011, 217:337-346.
68. Weston-Green K., Huang X.-F., Lian J., Deng C. Effects of olanzapine on muscarinic M3 receptor binding density in the brain relates to weight gain, plasma insulin and metabolic hormone levels. Eur Neuropsychopharmacol 2012, 22:364-373.
69. Xiberas X., Martinot J.L., Artiges E., Loc'H C., Maziere B., Paillere-martinot M.L. Extrastriatal and striatal D(2) dopamine receptor blockade with haloperidol or new antipsychotic drugs in patients with schizophrenia. Br J Psychiatry 2001, 179:503-508.
70. Yadav P.N., Kroeze W.K., Farrell M.S., Roth B.L. Antagonist functional selectivity: 5-HT2A serotonin receptor antagonists differentially regulate 5-HT2A receptor protein level in vivo. J Pharmacol Exp Ther 2011, 339:99-105.