1997
DOI: 10.1038/sj.bjp.0701164
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The atypical antipsychotic profile of NRA0045, a novel dopamine D4 and 5‐hydroxytryptamine2A receptor antagonist, in rats

Abstract: 1 The atypical antipsychotic pro®le of (R)-(+)-2-amino-4-(4-¯uorophenyl)-5-[1-[4-(4-¯uorophenyl)-4-oxobutyl] pyrrolidin-3-yl] thiazole (NRA0045), a potent dopamine D 4 and 5-hydroxytryptamine (5-HT) 2A receptor antagonist, was examined in rats. 2 Spontaneous locomotor activity was decreased dose-dependently with i.p. administration of clozapine (ED 50 3.7 mg kg 71 ), haloperidol (ED 50 0.1 mg kg 71 ) and chlorpromazine (ED 50 0.9 mg kg 71 ), whereas inhibition of this type of behaviour induced by i.p. adminis… Show more

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Cited by 43 publications
(33 citation statements)
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“…Neural substrate of PCP-induced abnormal behavior NRA0045 and clozapine each effectively inhibited not only PCP-induced hyperlocomotion but also stereotypy and ataxia, although each drug has been reported effectively to block methamphetamine-induced hyperlocomotion, but not stereotypy (Okuyama et al 1997a(Okuyama et al , 1997b. Amphetamine-induced hyperlocomotion is closely related to the neuronal activity in the nucleus accumbens (Kelly et al 1975).…”
Section: Discussionmentioning
confidence: 98%
See 1 more Smart Citation
“…Neural substrate of PCP-induced abnormal behavior NRA0045 and clozapine each effectively inhibited not only PCP-induced hyperlocomotion but also stereotypy and ataxia, although each drug has been reported effectively to block methamphetamine-induced hyperlocomotion, but not stereotypy (Okuyama et al 1997a(Okuyama et al , 1997b. Amphetamine-induced hyperlocomotion is closely related to the neuronal activity in the nucleus accumbens (Kelly et al 1975).…”
Section: Discussionmentioning
confidence: 98%
“…A novel thiazole derivative, NRA0045, which potently blocks not only dopamine D 4 receptors but also 5-HT 2A and a 1 -adrenaline receptors, inhibits methamphetamineinduced hyperlocomotion and PCP-induced cognitive dysfunction such as the prolongation of swimming latency in the water maze task (Okuyama et al 1997a(Okuyama et al , 1997b. Although another novel thiazole derivative, NRA0160, that selectively blocks dopamine D 4 receptors, inhibits PCP-induced prolongation of swimming latency, this agent weakly attenuates methamphetamine-induced hyperlocomotion (Okuyama et al 1999).…”
Section: Introductionmentioning
confidence: 99%
“…Appendix -extended list of papers referring to drug effects on PPI Apomorphine: Mansbach et al 1988;Davis et al 1990;Keith et al 1991;Swerdlow et al 1991bSwerdlow et al , 1994Swerdlow et al , 1995Swerdlow et al , 1998bSchwarzkopf et al 1993, Swerdlow andGeyer 1993;Hoffman and Donovan 1994;Caine et al 1995;Campeau and Davis 1995;Ellenbroek et al 1995;Lipska et al 1995;Taylor et al 1995;Varty and Higgins 1995;Young et al 1995;Zhang et al 1995;Hauber and Koch 1997;Okuyama et al 1997;Druhan et al 1998;Hart et al 1998;Kretschmer and Koch 1998;Martin-Iverson 1999;Rigdon 1999;Varty and Higgins 1999 Amphetamine: Mansbach et al 1988;Swerdlow et al 1990Swerdlow et al , 1991bHijzen et al 1991;Ott and Mandel 1995;Wan et al 1995;Zhang et al 1995;Feifel and Minor 1997;Feifel et al 1997aFeifel et al , 1997bFeifel et al , 1999Curzon and Decker 1998;Druhan et al 1998;Mintz et al 1998;Zhang et al 1998 Dopamine uptake blockers: …”
mentioning
confidence: 99%
“…In addition, both compounds attenuated hyperlocomotion induced by DA agonists and significantly reversed apomorphine-induced disruption of PPI. 96,97,116,117 The findings suggest that these compounds may have potential for clinical psychotropic activity with a low risk of extrapyramidal motor effects associated with effective D 2 receptor blockade that seems to be characteristic of all typical neuroleptics. 1,17 Surprisingly, preliminary clinical trials with at least two agents with D 4 -over-D 2 selectivity have failed to indicate any evidence of antipsychotic benefits.…”
Section: Positron-emission Tomography (Pet)mentioning
confidence: 98%