5-HT2A receptor antagonism potentiates haloperidol-induced dopamine release in rat medial prefrontal cortex and inhibits that in the nucleus accumbens in a dose-dependent manner
Liégeois, Jean-François; Ichikawa, J.; Meltzer, H. Y.
[en] Combined serotonin (5-HT)(2A) and dopamine (DA) D-2 blockade has been shown to contribute to the ability of atypical antipsychotic drugs (APDs) to increase DA release in rat medial prefrontal cortex (mPFC). We provide additional support for this hypothesis by examining the effect of the selective 5-HT2A antagonist M100907 plus haloperidol, a potent D, antagonist APD, on DA release in the mPFC and nucleus accumbens (NAC). Haloperidol (0.01-1.0 mg/kg) produced an inverted U-shaped increase in DA release in the mPFC, with a significant increase only at 0.1 mg/kg. Haloperidol (0.1 and 1.0 mg/kg) significantly increased DA release in the NAC. M100907 (0.1 mg/kg) by itself had no effect on DA release in either region. This dose of M100907 potentiated the ability of low (0.01-0.1 mg/kg), but not high dose (0.3-1.0 mg/kg) haloperidol to increase mPFC DA release, whereas it abolished the effect of both 0.1 and 1.0 mg/ka haloperidol on NAC DA release. These results suggest that the relatively higher ratio of 5-HT2A to D-2 antagonism may contribute to the potentiation of haloperidol-induced mPFC DA release, whereas 5-HT2A antagonism can diminish haloperidol-induced NAC DA release, even when combined with extensive D, antagonism, which may not be synergistic with 5-HT2A antagonism in the mPFC. (C) 2002 Elsevier Science B.V. All rights reserved.
Disciplines :
Neurosciences & behavior
Author, co-author :
Liégeois, Jean-François ; Université de Liège - ULiège > Département de pharmacie > Chimie pharmaceutique
Ichikawa, J.
Meltzer, H. Y.
Language :
English
Title :
5-HT2A receptor antagonism potentiates haloperidol-induced dopamine release in rat medial prefrontal cortex and inhibits that in the nucleus accumbens in a dose-dependent manner
Abi-dargham A., Gil R., Krystal J., Baldwin R.M., Seibyl J.P., Bowers M., Van Dyck C.H., Charney D.S., Innis R.B., Laruelle M. (1998) Increased striatal dopamine transmission in schizophrenia: Confiramation in a second cohort. Am. J. Psychiatry 155:761-767.
Abi-Dargham A., Rodenhiser J., Printz D., Zea-Ponce Y., Gil R., Kegeles L.S., Weiss R., Cooper T.B., Mann J.J., Van Heertum R.L., Gorman J.M., Laruelle M. (2000) Increased baseline occupancy of D2 receptors by dopamine in schizophrenia. Pro. Natl. Acad. Sci. USA 97:8104-8109.
Altar C.A., Wasley A.M., Neale F., Stone G.A. (1986) Typical and atypical antipsychotic occupancy of D2 and S2 receptors: An autoradiographic analysis in rat brain. Brain Res. Bull. 16:517-525.
Andersson J.L., Nomikos G.G., Marcus M., Hertel P., Mathe J.M., Svensson T.H. (1995) Ritanserin potentiates the stimulatory effects of raclopride on neuronal activity and dopamine release selectivity in the mesolimbic dopaminergic system. Naunyn-Schmiedeberg's Arch. Pharmacol. 352:374-385.
Arnt J., Skarsfeldt T. (1998) Do novel antipsychotics have similar pharmacological characteristics? A review of the evidence. Neuropsychopharmacology 18:63-101.
Bonaccorso S., Meltzer H.Y., Li Z., Dai J., Alboszta A., Kuroki T., Ichikawa J. SR46349-B, a 5-HT2A/2C receptor antagonist, potentiates haloperidol induced dopamine release in the medial prefrontal cortex and nucleus accumbens. Neuropharmacology, in press; . http:/www.acnp.org.citations/Npp022502247
Busatto G.F., Pilowsky L.S., Costa D.C., Ell P.J., Verhoeff N.P., Kerwin R.W. (1995) Dopamine D2 receptor blockade in vivo with the novel antipsychotics risperidone and remoxipride - An 123I-IBZM single photon emission tomography (SPET) study. Psychopharmacology 117:55-61.
Carboni E., Rolando M.T.P., Silvagni A., Di Chiara G. (2000) Increase of dialysate dopamine in the bed nucleus of stria terminalis by clozapine and related neuroleptics. Neuropsychopharmacology 22:140-147.
Carpenter W.T., Zito J.M., Vitrai J., Volavka J. (1998) Hypothesis testing: Is clozapine's superior efficacy dependent on moderate D2 receptor occupancy?. Biol. Psychiat. 43:79-83.
Davis K.L., Kahn R.S., Grant K., Davidson M. (1991) Dopamine in schizophrenia: A review and reconceptualization. Am. J. Psychiat. 148:1474-1486.
De Deurwaerdère P., Spampinato U. (1999) Role of serotonin2A and serotonin2B/2C receptor subtypes in the control of accumbal and striatal dopamine release elicited in vivo by dorsal raphe nucleus electrical stimulation. J. Neurochem. 73:1033-1042.
Di Giovanni G., Di Mascio M., Di Matteo V., Esposito E. (1998) Effects of acute and repeated administration of amisulpride, a dopamine D2/D3 receptor antagonist, on the electrical activity of midbrain dopaminergic neurons. J. Pharmacol. Exp. Ther. 287:51-57.
Di Matteo V., Di Giovanni G., Di Masci M., Esposito E. (1999) SB 242084, a selective serotonin2C receptor antagonist, increases dopaminergic transmission in the mesolimbic system. Neuropharmacology 38:1195-1205.
Drew K.L., O'Connor W.T., Kehr J., Ungerstedt U. (1990) Regional specific effects of clozapine and haloperidol on GABA and dopamine release in rat basal ganglia. Eur. J. Pharmacol. 187:385-397.
Farde L., Wiesel F.A., Halldin C., Sedvall G. (1988) Central D2-dopamine receptor occupancy in schizophrenic patients treated with antipsychotic drugs. Arch. Gen. Psychiat. 45:71-76.
Farde L., Nordström A.-L., Wiesel F.-A., Pauli S., Halldin C., Sedvall G. (1992) PET-analysis of central D1-and D2-dopamine receptor occupancy in patients treated with classical neuroleptics and clozapine-relation to extrapyramidal side effects. Arch. Gen. Psychiat. 49:538-544.
Gobert A., Millan M.J. (1999) Serotonin (5-HT)2A receptor activation enhances dialysate levels of dopamine and noradrenaline, but not 5-HT, in the frontal cortex of freely-moving rats. Neuropharmacology 38:315-317.
Gobert A., Rivet J.-M., Lejeune F., Newman-Tancredi A., Adhumeau-Auclair A., Nicolas J.-P., Cistarelli L., Melon C., Millan M.J. (2000) Serotonin2C receptors tonically suppress the activity of mesocortical dopaminergic and adrenergic, but not serotonergic, pathways: A combined dialysis and electrophysiological analysis in the rat. Synapse 36:205-221.
Hertel P., Fagerquist M.V., Svensson T.H. (1999) Enhanced cortical dopamine output and antipsychotic-like effects of raclopride by α2 adrenoceptor blockade. Science 286:105-107.
Ichikawa J., Meltzer H.Y. (1995) DOI, a 5-HT2C/2A receptor agonist, potentiates amphetamine-induced dopamine release in rat striatum. Brain Res. 698:204-208.
Ichikawa J., Meltzer H.Y. (1999) R-(+)-8-OH-DPAT, a serotonin1A receptor agonist, potentiated S-(-) sulpiride-induced dopamine release in rat medial prefrontal cortex and nucleus accumbens but not striatum. J. Pharmacol. Exp. Ther. 291:1227-1232.
Ichikawa J., Meltzer H.Y. (1999) Relationship between dopaminergic and serotonergic neuronal activity in the frontal cortex and the action of typical and atypical antipsychotic drugs. Eur. Arch. Psychiat. Clin. Neurosci. 249(SUPPL. 4).
Ichikawa J., Meltzer H.Y. (2000) The effect of serotonin1A receptors on antipsychotic drug-induced dopamine release in rat striatum and nucleus accumbens. Brain Res. 858:252-263.
Ichikawa J., Ishii H., Bonaccorso S., Fowler W.L., O'Laughlin I.A., Meltzer H.Y. (2001) 5-HT2A and D2 receptor blockade increases cortical DA release via 5-HT1A receptor activation: A possible mechanism of atypical antipsychotic-induced cortical dopamine release. J. Neurochem. 76:1521-1531.
Johnson E.A., Tsai C.E., Shahan Y.H., Azzaro A.J. (1993) Serotonin 5-HT1A receptors mediate inhibition of tyrosine hydroxylation in rat striatum. J. Pharmacol. Exp. Ther. 266:133-141.
Johnson E.A., Fox J.L., Azzaro A.J. (1996) The anxiolytic serotonin 5-HT1A receptor agonists buspirone, ipsapirone and gepirone are inhibitors of tyrosine hydroxylation in rat striatum. Behav. Brain Res. 73:331-335.
Kapur S., Remington G., Zipursky R.B., Wilson A.A., Houle S. (1995) The D2 dopamine receptor occupancy of risperidone and its relationship to extrapyramidal symptoms: A PET study. Life Sci. 57.
Kapur S. (1996) 5-HT2 antagonism and EPS benefits: Is there a causal connection?. Psychopharmacology 124:35-39.
Kapur S., Remington G. (1996) Serotonin-dopamine interaction and its relevance to schizophrenia. Am. J. Psychiat. 153:466-476.
Kapur S., Barsoum S.C., Seeman P. (2000) Dopamine D2 receptor blockade by haloperidol 3H-raclopride reveals much higher occupancy than EEDQ. Neuropsychopharmacology 23:595-598.
Kapur S., Zipursky R., Jones C., Shammi C.S., Remington G., Seeman P. (2000) A positron emission tomography study of quetiapine in schizophrenia: A preliminary finding of an antipsychotic effect with only transiently high dopamine D2 receptor occupancy. Arch. Gen. Psychiat. 57:553-559.
Kapur S., Seeman P. (2001) Does fast dissociation from the dopamine D2 receptor explain the action of atypical antipsychotics?: A new hypothesis. Am. J. Psychiat. 158:360-369.
Knable M.B., Weinberger D.R. (1997) Dopamine, the prefrontal cortex and schizophrenia. J. Psychopharmacol. 11:123-131.
Kuroki T., Meltzer H.Y., Ichikawa J. (1999) Effects of antipsychotic drugs on extracellular dopamine levels in rat medial prefrontal cortex and nucleus accumbens. J. Pharmacol. Exp. Ther. 288:774-781.
Kuroki T., Dai J., Meltzer H.Y., Ichikawa J. (2000) R-(+)-8-OH-DPAT, a selective 5-HT1A receptor agonist, attenuated amphetamine-induced dopamine synthesis in rat striatum, but not nucleus accumbens or medial prefrontal cortex. Brain Res. 872:204-207.
Laruelle M., Abi-Dargham A., Gil R., Kegeles L., Innis R. (1999) Increased dopamine transmission in schizophrenia: Relationship to illness phases. Biol. Psychiat. 46:56-72.
Lucas G., Spampinato U. (2000) Role of striatal serotonin2A and serotonin2C receptor subtypes in the control of in vivo dopamine outflow in the rat striatum. J. Neurochem. 74:693-701.
Lucas G., De Deurwaerdère P., Caccia S., Spampinato U. (2000) The effect of serotonergic agents on haloperidol-induced striatal dopamine release in vivo: Opposite role of 5-HT2A and 5-HT2C receptor subtypes and significance of the haloperidol dose used. Neuropharmacology 39:1053-1063.
Marcus M.M., Nomikos G.G., Svensson T.H. (1996) Differential actions of typical and atypical antipsychotic drugs on dopamine release in the core and shell of the nucleus accumbens. Eur. Neuropsychopharmacol. 6:29-38.
Matsubara S., Matsubara R., Kusumi I., Koyama T., Yamashita I. (1993) Dopamine D1, D2 and serotonin2 receptor occupancy by typical and atypical antipsychotic drugs in vivo. J. Pharmacol. Exp. Ther. 265:498-508.
Meltzer H.Y., Stahl S.M. (1976) The dopamine hypothesis of schizophrenia: A review. Schizophr. Bull. 2:19-76.
Meltzer H.Y., Matsubara S., Lee J.-C. (1989) Classification of typical and atypical antipsychotic drugs on the basis of D-1, D-2, and serotonin2 pKi values. J. Pharmacol. Exp. Ther. 251:238-246.
Meltzer H.Y. (1999) The role of serotonin in antipsychotic drug action. Neuropsychopharmacology 21.
Meltzer H.Y. (1999) Dopamine2 receptor occupancy and the action of clozapine: Does it make a difference to add a neuroleptic?. Biol. Psychiat. 46:144-149.
Meltzer H.Y., McGurk S.R. (1999) The effect of clozapine, risperidone and olanzapine on cognitive function in schizophrenia. Schizophr. Bull. 25:233-255.
Meltzer H.Y. (2000) An atypical compound by any other name is still atypical. Psychopharmacology 148:16-19.
Moghaddam B., Bunney B.S. (1990) Acute effects of typical and atypical antipsychotic drugs on the release of dopamine from prefrontal cortex, nucleus accumbens, and striatum of the rat: An in vivo microdialysis study. J. Neurochem. 54:1755-1760.
Nyberg S., Eriksson B., Oxenstierna G., Halldin C., Farde L. (1999) Suggested minimal effective dose of risperidone based on PET-measured D2 and 5-HT2A receptor occupancy in schizophrenic patients. Am. J. Psychiat. 156:869-875.
Oshiro Y., Sato S., Kurahashi N., Tanaka T., Kikuchi T., Tottori K., Uwahodo Y., Nishi T. (1998) Novel antipsychotic agents with dopamine autoreceptor agonist properties: Synthesis and pharmacology of 7-[4-(4-phenyl-1-piperazinyl)butoxy]-3,4-dihydro-2(1H)-quinolinone derivatives. J. Med. Chem. 41:658-667.
Paxinos G., Watson C. The Rat Brain in Stereotaxic Coordinates, New York: Academic Press; 1986.
Pehek E.A., McFarlane H.G., Maguschak K., Price B., Pluto C.P. (2001) M100,907, a selective 5-HT2A antagonist, attenuates dopamine release in the rat medial prefrontal cortex. Brain Res. 888:51-59.
Raedler T.J., Knable M.B., Lafargue T., Urbina R.A., Egan M.F., Pickar D., Weinberger D.R. (1999) In vivo determination of striatal dopamine D2 receptor occupancy in patients treated with olanzapine. Psychiatry Res. 90:81-90.
Rasmussen K., Aghajanian G.K. (1988) Potency of antipsychotics in reversing the effects of a hallucinogenic drug on locus coeruleus neurons correlates with 5-HT2 binding affinity. Neuropsychopharmacology 1:101-107.
Roth B.L., Ciaranello R.D., Meltzer H.Y. (1992) Binding of typical and atypical antipsychotic agents to transiently expressed 5-HT1C receptors. J. Pharmacol. Exp. Ther. 260:1361-1365.
Schotte A., Janssen P.F.M., Gommeren W., Luyten W.H.M.L., Van Gompel P., Lesage A.S., De Loore K., Leysen J.E. (1996) Risperidone compared with new and reference antipsychotic drugs: In vitro and in vivo receptor binding. Psychopharmacology 124:57-73.
Seeman P., Tallerico T. (1999) Rapid release of antipsychotic drugs from dopamine D2 receptors: An explanation for low receptor occupancy and early clinical relapse upon withdrawal of clozapine or quetiapine. Am. J. Psychiat. 156:876-884.
Spampinato U., DeDeurwaerdère P., Caccia S., Lucas G. (1998) Opposite role of central 5-HT2A and 5-HT2C receptors subtypes in the control of haloperidol-induced release of dopamine in the rat striatum. Soc. Neurosci. Abstr. 24:484.
Stockmeier C.A., DiCarlo J.J., Zhang Y., Thompson P., Meltzer H.Y. (1993) Characterization of typical and atypical antipsychotic drugs based on in vivo occupancy of serotonin2 and dopamine2 receptors. J. Pharmacol. Exp. Ther. 266:1374-1384.
Sumiyoshi T., Kido H., Sakamoto H., Urasaki K., Suzuki K., Yamaguchi N., Mori H., Shiba K., Yokogawa K. (1994) In vivo dopamine-D2 and serotonin-5-HT2 receptor binding study of risperidone and haloperidol. Pharmacol. Biochem. Behav. 47:553-557.
Tsukada H., Nishiyama S., Kakiuchi T., Ohba H., Sato K., Harada N. (1999) Is synaptic dopamine concentration the exclusive factor which alters the in vivo binding of [11C]raclopride?: PET studies combined with microdialysis in conscious monkeys. Brain Res. 841:160-169.
Wadenberg M.L., Salmi P., Jimenez P., Svensson T., Ahlenius S. (1996) Enhancement of antipsychotic-like properties of the dopamine D2 receptor antagonist, raclopride, by the additional treatment with the 5-HT2 receptor blocking agent, ritanserin, in the rat. Eur. Neuropsychopharmacol. 6:305-310.
Wadenberg M.L., Hicks P.B., Richter J.T., Young K.A. (1998) Enhancement of antipsychotic-like properties of raclopride in rats using the selective serotonin2a receptor antagonist MDL 100,907. Biol. Psychiat. 44:508-515.
Westerink B.H.C., Kawahara Y., De Boer P., Geels C., De Vries J.B., Wikström H.V., Van Kalkeren A., Van Vliet B., Kruse C.G., Long S.K. (2001) Antipsychotic drugs classified by their effects on the release of dopamine and noradrenaline in the prefrontal cortex and striatum. Eur. J. Pharmacol. 412:127-138.
Yamada S., Takaki T., Yokoo H., Tanaka M. (1995) Inhibitory effect of haloperidol on evoked dopamine release from striatal slices of the rat. Jpn. J. Psychopharmacol. 15:43-52.
Yamada S., Takaki T., Yokoo H., Tanaka M. (1995) Differential effects of dopamine antagonists on evoked dopamine release from slices of striatum and nucleus accumbens in rats. J. Pharm. Pharmacol. 47:259-262.