Abstract:
:Ro 15-4513, a partial inverse agonist at the benzodiazepine (BZ) receptor site was labelled with 11C and used for in vitro autoradiography on human post mortem brain sections and for positron emission tomography (PET) on Cynomolgus monkeys. The total radiochemical yield of [11C]Ro 15-4513 was 30-40% with an overall synthesis time of 40 min. The specific radioactivity was about 1000 Ci/mmol at end of synthesis. In vitro autoradiography showed that [11C]Ro 15-4513 bound specifically predominantly in the neocortex of the human brain. Specific binding was also demonstrated in the basal ganglia and the cerebellar cortex. Flumazenil (Ro 15-1788) and clonazepam inhibited the binding in cerebral regions, but a significant proportion in the cerebellum was not inhibited by these agents. This proportion may represent alpha 6-containing BZ receptors. PET examination of [11C]Ro 15-4513 binding in Cynomolgus monkeys demonstrated high uptake of radioactivity in neocortex. The uptake of radioactivity was markedly displaced by high doses of Ro 15-4513 or clonazepam. [11C]Ro 15-4513 should be a useful ligand to examine BZ receptor characteristics in the living human brain by PET.
journal_name
Psychopharmacology (Berl)journal_title
Psychopharmacologyauthors
Halldin C,Farde L,Litton JE,Hall H,Sedvall Gdoi
10.1007/BF02245279subject
Has Abstractpub_date
1992-01-01 00:00:00pages
16-22issue
1-2eissn
0033-3158issn
1432-2072journal_volume
108pub_type
杂志文章abstract:RATIONALE:Relapse to smoking is often precipitated by stress, yet little is known about the effects of nicotine withdrawal on responses to acute stress, or whether nicotine replacement reverses withdrawal-induced changes in stress response. OBJECTIVES:The aim of the present study is to use an effective social stressor...
journal_title:Psychopharmacology
pub_type: 杂志文章,随机对照试验
doi:10.1007/s00213-010-2150-y
更新日期:2011-11-01 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:RATIONALE:Dopamine (DA) and glutamate (Glu) interactions in the mesocorticolimbic pathway may regulate motivation and reward and contribute to schizophrenia and drug abuse. We have recently demonstrated synergistic effects of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA)/kainate receptor blockade and ...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-005-0039-y
更新日期:2005-10-01 00:00:00
abstract:RATIONALE:Neuropeptide Y (NPY) is implicated in the pathophysiology of affective illness. Multiple receptor subtypes (Y1R, Y2R, and Y5R) have been suggested to contribute to NPY's effects on rodent anxiety and depression-related behaviors. OBJECTIVES:To further elucidate the role of Y1R in (1) NPY's anxiolytic-like ef...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-007-0945-2
更新日期:2008-01-01 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::Naloxone HCl (10 micrograms/0.5 ml) was injected in the locus coeruleus (LC) of morphine-dependent rats and the behavioural manifestations of morphine withdrawal and the cortical levels of 3-methoxy-4-hydroxyphenylethyleneglycol sulfate (MHPG-SO4) were measured 30 min later. Naloxone precipitated a withdrawal syndrome...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00187263
更新日期:1987-01-01 00:00:00
abstract:BACKGROUND:Although ethanol is frequently used in combination with other psychoactive drugs, the behavioral and pharmacological reasons for this form of polydrug abuse have not been well described. MATERIALS AND METHODS:Rhesus monkeys with indwelling intravenous catheters produced intravenous injections of ethanol (50...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-007-0809-9
更新日期:2007-09-01 00:00:00
abstract:RATIONALE:Available neurochemical probes that lower brain dopamine (DA) levels in man are limited by their tolerability and efficacy. For instance, the acute lowering of brain tyrosine is well tolerated, but only modestly lowers brain DA levels. Modification of tyrosine depletion to robustly lower DA levels would provi...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-013-2977-0
更新日期:2013-05-01 00:00:00
abstract:RATIONALE:Research on the effects of nicotine abstinence and nicotine replacement has not provided consistent information about the impact of replacement therapies on tobacco withdrawal and craving. OBJECTIVE:. This study investigated craving and withdrawal symptoms over a 72-h period of abstinence from cigarettes. M...
journal_title:Psychopharmacology
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1007/s00213-002-1176-1
更新日期:2002-11-01 00:00:00
abstract::The concurrent influence of dopaminergic, sigma and muscarinic neurotransmitter systems in mediating cocaine-induced lethality is predicted by previous receptor binding results from our laboratories. The present results demonstrate that pharmacological manipulations of these predicted neurotransmitter systems alter th...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s002130050198
更新日期:1997-02-01 00:00:00
abstract::5-Hydroxytryptamine1A (5-HT1A) receptors have been shown to be suppressed by corticosteroid hormones in a variety of animal experimental paradigms. It has been suggested that this effect may be central to the pathophysiology of severe clinical depressive illness, a condition in which 5-HT1A receptor function is reduce...
journal_title:Psychopharmacology
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1007/s002130050711
更新日期:1998-10-01 00:00:00
abstract::A prospective study of response to treatment with nortriptyline was carried out in a group of 14 inpatients with mixed symptoms of depression and dementia. Platelet membrane fluidity, as reflected by the fluorescence anisotropy of DPH labeled membranes, was determined for all 14 drug-free subjects prior to treatment b...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00174688
更新日期:1988-01-01 00:00:00
abstract::In a phase II study the antidepressive effect of citalopram, a selective and potent serotonin reuptake inhibitor, was examined in 20 endogenously and three non-endogenously depressed hospitalized patients. Four endogenously depressed patients dropped out due to deterioration early in the treatment period. The remainin...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00464566
更新日期:1982-01-01 00:00:00
abstract::The present studies were undertaken to investigate the neuroactive steroidal modulation of feeding behavior and possible involvement of gamma-aminobutyric acid type-A (GABA-A) and mitochondrial diazepam binding inhibitor (DBI) receptors (MDR) in food-deprived male mice. Allopregnanolone (0.5-2 mg/kg), a neurosteroid, ...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s002130050635
更新日期:1998-06-01 00:00:00
abstract::A theory of acute tolerance to alcohol is proposed that includes two assumptions: 1) acute tolerance is a linear process with time, and 2) the slope of the line is a measure of the magnitude of the acute tolerance effect. Evidence that supports the validity of the theory is presented both from studies in which blood a...
journal_title:Psychopharmacology
pub_type: 杂志文章,评审
doi:10.1007/BF02245438
更新日期:1994-02-01 00:00:00
abstract::Several studies have demonstrated a paradoxical form of antinociception induced by the repeated administration of opioid antagonists accompanied by exposure to a painful stimulus. The underlying mechanism of this naloxone-induced antinociception (NIA) is still unknown, but the results of several studies suggest that i...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF02245234
更新日期:1994-01-01 00:00:00
abstract::Augmentation with low-dose fluvoxamine (50-100 mg/day) to antipsychotic treatment may improve the negative symptoms in schizophrenic patients, but involves a risk of drug-drug interaction. We studied the effects of fluvoxamine on plasma concentrations of haloperidol and reduced haloperidol, and their clinical symptoms...
journal_title:Psychopharmacology
pub_type: 临床试验,杂志文章
doi:10.1007/s00213-003-1567-y
更新日期:2004-01-01 00:00:00
abstract:RATIONALE:Electronic cigarettes (ECs) are becoming popular alternatives for smokers, but there has been limited study of their abuse liability. OBJECTIVES:The objective of this study was to evaluate the abuse liability of three Vuse Solo ECs, ranging from 14 to 36 mg in nicotine content, relative to high- and low-abus...
journal_title:Psychopharmacology
pub_type: 杂志文章,随机对照试验
doi:10.1007/s00213-017-4665-y
更新日期:2017-09-01 00:00:00
abstract::The thymoleptics potentiate and modify the behavioral effects of apomorphine (probably the most specific dopaminergic agonist) as well as those of Dopa. The effect of the thymoleptics is not abolished by emptying of amine stores, and this together with other evidence suggests that these drugs facilitate the access of ...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00427282
更新日期:1976-09-17 00:00:00
abstract:RATIONALE:Preclinical evidence suggests that non-cannabinoid neurotransmitter systems are involved in the behavioral and physiological effects of cannabinoids, but relatively little research has been conducted in humans. OBJECTIVES:The aims of this study were to assess whether oral Delta(9)-tetrahydrocannabinol (Delta...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-008-1393-3
更新日期:2009-04-01 00:00:00
abstract:RATIONALE:Carbon monoxide synthetized by inducible heme oxygenase (HO-1) exerts potent anti-inflammatory and antinociceptive effects during acute and neuropathic pain, but its role in the modulation of chronic inflammatory pain and the possible involvement of nitric oxide in this action remain unknown. OBJECTIVES AND ...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-013-3302-7
更新日期:2014-03-01 00:00:00
abstract::Ethologic analysis has been used to study the behavioural effects following injection of delta-aminolaevulinic acid (ALA) in mice. After a dose level of 1.6 mmol ALA/kg, male and female mice showed periods of immobility and scanned less frequently than saline-injected controls. Exploration of the cage was significantl...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00426726
更新日期:1979-03-22 00:00:00
abstract:RATIONALE:Brain waves reflect collective behavior of neurons and provide insight into distributed network processing. Frontal and hippocampal theta oscillations (4-7 Hz) were linked to cognitive tasks and animal studies have suggested an involvement of glutamatergic neurotransmission in integrative frontal-hippocampal ...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-006-0397-0
更新日期:2006-07-01 00:00:00
abstract::Because of the increasing demand for refined techniques to record drug-induced motoric changes, we designed and evaluated a computer monitoring system with continuous measurement of different parameters of rat motor activity. This system is particularly useful for chronic drug studies because it can characterize patte...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00432113
更新日期:1983-01-01 00:00:00
abstract::We have previously obtained evidence that the mesoamygdaloid dopamine projection modulates the acquisition of a conditioned response (CR) elicited by presentation of a conditioned stimulus (CS) predicting the availability of a natural (sucrose) reward. This property was found to be dependent upon D3, but not D1 or D2,...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s002130050771
更新日期:1998-12-01 00:00:00
abstract:RATIONALE:Repeated social stress experiences engender "behavioral sensitization" and may also increase the potential for abuse of psychomotor stimulants, particularly cocaine use during "binges." OBJECTIVE:Experimental protocols were designed to induce behavioral sensitization through exposures to social-defeat stress...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s002130100858
更新日期:2001-12-01 00:00:00
abstract::Chronic administration of the pre-synaptic alpha-adrenoreceptor agonist clonidine decreases the concentration of the extra-neuronal metabolite of noradrenaline normetanephrine in the amygdaloid cortex and increases it in the mid-brain. Conversely, blockade of these pre-synaptic receptors by yohimbine increases the nor...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00427519
更新日期:1979-09-01 00:00:00
abstract::We have previously demonstrated that depletion of forebrain norepinephrine (NE) led to an attenuation of neophobia in a novel environment, as defined by a greater preference for novel food over familiar food. To study further the role of forebrain NE in neophobia we chronically infused noradrenergic receptor ligands o...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF02253601
更新日期:1992-01-01 00:00:00
abstract::Measurements of the amplitude and latency of the P3b component of the event-related potential (ERP), simple reaction time (SRT) and four psychomotor tests (VAS, DSST, DSp and CFF) were made on 12 male subjects (aged 19-24 years) 1.0-1.5 and 4.0-4.5 h after single oral doses of triprolidine (7.5 mg), terfenadine (60 mg...
journal_title:Psychopharmacology
pub_type: 临床试验,杂志文章
doi:10.1007/BF00451699
更新日期:1989-01-01 00:00:00
abstract:RATIONALE:Several halogenated analogs of benztropine (BZT) have previously been characterized as potent DA uptake inhibitors with behavioral profiles that indicate diminished psychomotor stimulant effects relative to cocaine. In a previous study using a fixed-ratio 10 schedule, two chloro-analogs (3'-Cl-BZT and 4'-Cl-B...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s002130000616
更新日期:2001-04-01 00:00:00