Abstract:
RATIONALE:Clozapine is a unique antipsychotic with very low propensity to cause motor side effects. In contrast to most other antipsychotics that block more than 70% of dopamine D(2) receptors at therapeutic doses, clozapine occupies less than 70%. Furthermore, even at maximum occupancy, 70% is not exceeded. Several mechanisms have been proposed as explanations for this low D(2) receptor occupancy, but clear evidence is limited. OBJECTIVES:In patient studies the data are limited by the dose-range that can be safely used; therefore, the aims of this study were to examine the maximum occupancy of dopamine D(2) receptors with up to 5.0 mg/kg of bolus injection of clozapine to non-human primates and to measure the time course of occupancy. METHODS:PET examination with [(11)C]raclopride was performed to measure the dopamine D(2) receptor occupancy in the striatum of two monkeys after the bolus injection of 0.2-5.0 mg/kg clozapine. [(11)C]raclopride was injected sequentially to follow the time course of occupancy up to 7 h after the clozapine injection. RESULTS:Dopamine D(2) receptor occupancy reached up to 83% after 5.0 mg/kg clozapine injection. Occupancy decreased with a half-life of 7.22 h after 5.0 mg/kg clozapine and 5.25 h after 1.0 and 2.0 mg/kg clozapine. CONCLUSIONS:Clozapine could occupy a high proportion of dopamine D(2) receptors. The time course of occupancy was relatively fast, with a half-life of several hours.
journal_name
Psychopharmacology (Berl)journal_title
Psychopharmacologyauthors
Suhara T,Okauchi T,Sudo Y,Takano A,Kawabe K,Maeda J,Kapur Sdoi
10.1007/s00213-001-0967-0subject
Has Abstractpub_date
2002-02-01 00:00:00pages
107-12issue
1eissn
0033-3158issn
1432-2072journal_volume
160pub_type
杂志文章abstract:RATIONALE:C-reactive protein (CRP), an acute phase protein that is released in response to inflammatory stimuli, is implicated in Alzheimer's disease (AD). However, the role of CRP in memory deficits associated with AD remains unclear. OBJECTIVE:Experiments were carried out to determine whether CRP impaired memory and...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-009-1499-2
更新日期:2009-07-01 00:00:00
abstract:RATIONALE:We test methods to advance (shift earlier) circadian rhythms without producing misalignment between rhythms and sleep. We previously tested (1) a gradually advancing sleep/dark schedule plus morning bright light and afternoon/evening melatonin and (2) the same sleep schedule with only morning bright light. No...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-012-2869-8
更新日期:2013-02-01 00:00:00
abstract::Maternal pup searching behaviour of lactating house mice treated with apomorphine, haloperidol or saline was examined on a running board with a central depression as a nest. Pup searching was elicited by artificial ultrasonic stimuli: a female moved out from the nest either towards a 50 kHz tone (key stimulus) which i...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00174523
更新日期:1988-01-01 00:00:00
abstract::Abnormal beta-adrenergic receptor (betaAR) density in the brains of suicide victims has been reported, although results of studies are inconsistent. Ethanol modifies betaAR-mediated signal transduction. Moreover abnormal betaAR function has been implicated in alcoholism. BetaAR antagonists, which were used as ligands ...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s002130051029
更新日期:1999-07-01 00:00:00
abstract::Amphetamine stimulates locomotor activity, in large part by activating central dopaminergic systems. Serotonin shares on overlapping distribution with dopamine and has been shown to modulate dopaminergic function and dopamine-mediated behaviors. The present study examined whether increasing serotonergic function, via ...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s002130050852
更新日期:1999-02-01 00:00:00
abstract:BACKGROUND:Delivering nicotine in the way smokers seek is likely to be the key factor in e-cigarette (EC) success in replacing cigarettes. We examined to what degree different types of EC mimic nicotine intake from cigarettes. METHODS:Twelve participants ('dual users' of EC and cigarettes) used their own brand cigaret...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-016-4512-6
更新日期:2017-03-01 00:00:00
abstract:RATIONALE:Reelin, a large extracellular matrix glycoprotein, is down-regulated in the brain of schizophrenic patients and of heterozygous reeler mice (rl/+). The behavioral phenotype of rl/- mice, however, matches only partially the schizophrenia hallmarks. OBJECTIVES:We recently reported (Marrone et al., Eur J Neuros...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-009-1483-x
更新日期:2009-06-01 00:00:00
abstract::The behavioural effects of increasing doses of apomorphine and haloperidol were observed in a group of six marmosets. Behaviour was classified quantitatively into categories: Locomotion, inactivity, checking (small head movements), social interaction and purposeful activities. Statistical analysis revealed that apomor...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00431987
更新日期:1979-01-01 00:00:00
abstract::In the rat, the antimuscarinics atropine and scopolamine failed to block the reduction in pentobarbital-induced sleep time produced by either thyrotropin-releasing hormone (TRH) or MK-771 (a TRH analog). Previous reports have indicated that the marked analeptic effect produced by TRH is antagonized by such agents. It ...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00431749
更新日期:1981-01-01 00:00:00
abstract:RATIONALE:(+/-)-3,4-methylenedioxymethamphet-amine (MDMA; 'ecstasy'), a commonly used recreational drug, has typically been found to be related to poor cognitive function in humans. However, cannabis consumption may not have been adequately controlled for in these studies. OBJECTIVE:The present study was designed to f...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s002130000591
更新日期:2001-01-01 00:00:00
abstract::The behavioral effects of repeated methylphenidate (MPH) treatment were assessed in the adult rat. Protein kinase A (PKA) and adenylyl cyclase (basal and DA-stimulated) activity in the dorsal striatum (i.e., caudate-putamen) were measured to determine whether MPH-induced alterations in these enzymes correlate with the...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s002130050536
更新日期:1998-03-01 00:00:00
abstract::The purpose of this study was to compare the subchronic, low-dose effects of clozapine with those of olanzapine in a learned behavioral task previously shown to distinguish between clozapine and haloperidol with acute and subchronic treatment regimes. Rats were trained to use a single forelimb to press a force-recordi...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s002130050363
更新日期:1997-08-01 00:00:00
abstract:OBJECTIVES:To investigate the relationship between benzodiazepine and risk of developing pneumonia in patients with schizophrenia, whose benzodiazepine dosage and usage frequency was higher than that of the general population. METHODS:We conducted a nested case-control study to assess the association between benzodiaz...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-018-5039-9
更新日期:2018-11-01 00:00:00
abstract:RATIONALE:A sensitized dopamine system may be linked to the genesis of psychotic symptoms in schizophrenia. Following withdrawal from amphetamine exposures, psychotic-like traits have been robustly demonstrated, but the presence of cognitive/mnemonic deficits remains uncertain. METHODS:Adult male Lewis and Fischer rat...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-009-1514-7
更新日期:2009-11-01 00:00:00
abstract::The behavioral effects of the benzodiazepine (BZP)-receptor partial inverse agonists, beta-CCE and FG 7142, are reviewed and the claim that these compounds possess "anxiogenic" properties is examined. Results obtained from human studies and global observations in animals, as well as those from experiments on aggressio...
journal_title:Psychopharmacology
pub_type: 杂志文章,评审
doi:10.1007/BF00212837
更新日期:1988-01-01 00:00:00
abstract:RATIONALE:We have shown that differences in the level of neural activation to stimuli associated with smoking vs. natural rewards, a biomarker related to reward sensitivity, predict treatment outcome. OBJECTIVES:This paper examined whether this biomarker moderates the impact of bupropion or varenicline on smoking cess...
journal_title:Psychopharmacology
pub_type: 杂志文章,随机对照试验
doi:10.1007/s00213-017-4580-2
更新日期:2017-06-01 00:00:00
abstract::Offensive and defensive components of aggressive behavior were determined in resident and intruder mice. Withdrawal aggression was measured after the removal of a subcutaneous morphine pellet or after precipitation by naloxone in naive mice and after removal of a morphine pellet in mice with prior fighting experience....
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00174059
更新日期:1986-01-01 00:00:00
abstract::The benzodiazepine diazepam and the benzodiazepine antagonist Ro 15-1788 were tested alone or in combination for their influence on scopolamine-induced locomotor stimulation in mice. The benzodiazepine antagonist had no effect by itself, but prevented the enhancement of scopolamine-induced locomotor stimulation produc...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00464583
更新日期:1982-01-01 00:00:00
abstract:RATIONALE:Nitric oxide (NO) is a messenger synthesized in both the neuronal and glial populations by nitric oxide synthase type 1 (NOS1). Nicotine regulates NO production in a sex-dependent manner, both molecules being involved in motor function. OBJECTIVE:The present study evaluates sex differences in motor coordinat...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-013-3284-5
更新日期:2014-02-01 00:00:00
abstract::Rats were chronically administered either haloperidol (HAL) or fluphenazine (FLU) via depot injections for 8 months, given these same drugs in their drinking water for the next 2 months, and then withdrawn from the drugs. Throughout the experiment the animals were tested repeatedly in an enclosed tube using a computer...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00174701
更新日期:1988-01-01 00:00:00
abstract:RATIONALE:Repeated treatment with morphine has been shown to sensitize rats to its stimulant effects on motor activity and mesolimbic dopamine (DA) transmission. OBJECTIVES:The aim of this study is to investigate if morphine sensitization is associated to changes in the behavioral reactions to appetitive and aversive ...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-011-2220-9
更新日期:2011-08-01 00:00:00
abstract:RATIONALE:In an animal model for vulnerability to drug abuse, rats that are more reactive to a novel environment (high responders, HRs) are more sensitive to behavioral effects of psychostimulants than are less reactive rats (low responders, LRs). In a companion article, we reported that HRs and LRs differ in sensitivi...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-004-1921-8
更新日期:2004-12-01 00:00:00
abstract::Mood disorders, despite the widespread availability of monoamine-based antidepressant treatments, are associated with persistently high rates of disability, together with elevated rates of mortality due to suicide, cardiovascular disease, and other causes. The development of more effective treatments has been hindered...
journal_title:Psychopharmacology
pub_type: 杂志文章,评审
doi:10.1007/s00213-016-4214-0
更新日期:2016-05-01 00:00:00
abstract::Metergoline given IP reduced the response to noxious stimulation in the mouse formalin test. Tolerance to this effect developed after a chronic treatment schedule consisting of ten daily injections of 5 mg/kg. Twenty four hours after the last injection a test dose of metergoline (2.5 mg/kg) reduced the licking time in...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF02439580
更新日期:1987-01-01 00:00:00
abstract:RATIONALE:The ability of nicotine to induce dependence (result in a withdrawal syndrome) is typically thought to require long-term, daily smoking. Emerging evidence suggests that symptoms of nicotine withdrawal may occur following only a few cigarettes. Whether acute exposure to nicotine can induce dependence in animal...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-012-2814-x
更新日期:2013-01-01 00:00:00
abstract:RATIONALE:Current medications for attention-deficit/hyperactivity disorder (ADHD) include some single isomer compounds [dextroamphetamine (D: -amphetamine, dexedrine) and dexmethylphenidate (Focalin)] and some racemic compounds [methylphenidate and mixed-salts amphetamine (Adderall)]. Adderall, which contains approxima...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-004-2012-6
更新日期:2005-03-01 00:00:00
abstract::The peripheral BDZ receptor ligand Ro 5-4864 was administered to rabbits in doses ranging from 0.2 to 7 mg/kg IV. Changes in electrocortical activity appeared within 1 min after administration, characterized by trains of slow waves in the posterior sensorimotor and optic cortices (0.6-2 mg/kg) and by grand mal seizure...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00180835
更新日期:1986-01-01 00:00:00
abstract:RATIONALE:Clinical observations have shown that pain sensitivity is altered in some schizophrenic patients. OBJECTIVES:To study alterations in pain sensitivity, the ketamine model in schizophrenia research was employed. MATERIALS AND METHODS:Rats were subchronically injected with the dissociative anaesthetic ketamine...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-006-0557-2
更新日期:2006-12-01 00:00:00
abstract:RATIONALE:The beneficial effects of psychostimulant drugs in the treatment of psychiatric disorders occur because they increase the extracellular dopamine concentration by inhibiting re-uptake of extracellular dopamine at dopamine transporters. However, the psychological effects at low dopamine transporter occupancy ha...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-016-4464-x
更新日期:2017-02-01 00:00:00
abstract::The effects of pindolol on the prolactin (PRL) and growth hormone (GH) responses to intravenous tryptophan (LTP) were studied in eight healthy male volunteers. Pindolol pretreatment (40 mg over 48 h) markedly attenuated the GH response to LTP and modestly, but significantly, reduced the LTP-induced increase in plasma ...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF02244090
更新日期:1991-01-01 00:00:00