Abstract:
:The purpose of this review was to establish in vivo apparent pA2 and pKB values for antagonism of the discriminative stimulus effects of benzodiazepine ligands, and to compare these values to those obtained from other behavioral procedures. Articles were chosen from the Medline data base from January 1976 to August 1995. This literature consisted of studies with flumazenil (Ro 15-1788) as the antagonist, as well as other benzodiazepine ligands (beta-carbolines, CGS 9896, CGS 8216). The dose which occasioned 50% of the maximal response (ED50) was obtained from values estimated from the graphs presented in each article. These ED50 values were used to conduct apparent pKB and apparent pA2 analyses. Apparent pA2 values for antagonism of the discriminative stimulus effects of diazepam in rats were the following (antagonist, pA2, slope): flumazenil, 4.7, -1.5; beta-CCE, 4.0, -3.0; beta-CCtB, 5.0, -2.2. The apparent pA2 value for CGS 8216 antagonism of the discriminative stimulus effects of diazepam in rats was 5.74, -2.22 (reported in Shannon and Davis 1984). The mean apparent pA2 value for flumazenil antagonism of the discriminative stimulus effects of diazepam in rhesus monkeys was 6.55, with a mean slope of -1.42. Analysis of baboon data from Ator and Griffiths (1986) revealed apparent pKB values for flumazenil antagonism of the discriminative stimulus effects of lorazepam that were lower than the pKB values for either zopiclone or CL 218,872. Analyses of the pKB data also revealed the following: no effect of route of administration (rat, PO versus IP; baboon, PO versus IM), no effect of pretreatment time (grouped into two categories: 10-20 min and 40-70 min, in rats and non-human primates), and a species effect (pKB values for rats were reliably lower than either non-human primates or pigeons, rhesus monkeys were lower than baboons). The apparent pA2 and pKB values obtained in the present review were similar across behavioral assays, except that, in squirrel monkeys, flumazenil pKB values for antagonism of benzodiazepine-induced decreases in schedule-controlled behavior were lower than pKB values obtained from drug discrimination studies. This review provides apparent pA2 values for antagonism of the discriminative stimulus effects of benzodiazepine ligands and provides evidence from pKB analyses consistent with functional heterogeneity of benzodiazepine receptors in vivo.
journal_name
Psychopharmacology (Berl)journal_title
Psychopharmacologyauthors
Rowlett JK,Woolverton WLdoi
10.1007/s002130050103subject
Has Abstractpub_date
1996-11-01 00:00:00pages
1-16issue
1eissn
0033-3158issn
1432-2072journal_volume
128pub_type
杂志文章,meta分析abstract::The effects of 4 weeks of treatment with the selective monoamine oxidase (MAO) inhibiting antidepressant clorgyline and pargyline on the sleep of affectively disordered patients were studied. Both inhibitors resulted in near total suppression of REM sleep, a decrease in total sleep time, and an increase in the percent...
journal_title:Psychopharmacology
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1007/BF00432251
更新日期:1982-01-01 00:00:00
abstract::Two experiments were carried out on pigeons to assess the effects of acute ethanol (ETOH) administration on a delayed pair comparison procedure. ETOH disrupted performance at the two higher doses (1.0 and 2.0 g/kg, given orally). When the initial (zero delay) performance levels of treated and untreated birds were equa...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00434411
更新日期:1980-01-01 00:00:00
abstract::We examined the effects on sucrose consumption of a dopamine (DA) D2/D3 antagonist (raclopride, 0-0.3 mg/kg), a serotonin 5-HT2/2c antagonist (ritanserin, 0-0.4 mg/kg), and raclopride (0.15 mg/kg) combined with ritanserin (0-0.4 mg/kg). Three different concentrations of sucrose solution (0.7%, 7.0% and 34%) were teste...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF02246286
更新日期:1996-01-01 00:00:00
abstract::Intracerebroventricular injections of gamma-aminobutyric acid (GABA) and of the GABA-transaminase inhibitor, ethanolamine-O-sulphate (EOS), decreased the food intake of freely-fed (GABA and EOS) and food-deprived rats (EOS). The effect, still evident 24 h after treatment, was not decreased by the GABA receptor-blocker...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00432135
更新日期:1980-01-01 00:00:00
abstract::In an attempt to define the nature of the involvement of delta 9-tetrahydrocannabinol (THC) with central cholinergic neurotransmission, the effects of THC on direct cholinergic stimulation of the rat brain were investigated. THC, in doses of 3 mg/kg and 6 mg/kg, administered intraperitoneally (i.p.), potentiated the e...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00426661
更新日期:1979-02-28 00:00:00
abstract::Aniamls were administered increasing doses of morphine for 16 days. During withdrawal they were challenged with an apomorphine ester or lergotrile. These dopamine agonists produced quantitatively different effects on behaviour. The results suggest that chronic morphine administration leads to dopamine supersensitivity...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00433570
更新日期:1979-05-15 00:00:00
abstract::Neuroleptic-free schizophrenic patients received caerulein, a potent analogue of cholecystokinin octapeptide, in a fixed- and rising-dose schedule. In addition, neuroleptic-treated patients received a single dose of the peptide with a 4-week follow-up. No significant change in mental status was observed after any of t...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00180843
更新日期:1986-01-01 00:00:00
abstract::First, it was confirmed that systemic injection of the neurotoxin 6-hydroxydopamine HBr (30 mg/kg IP) depleted noradrenaline levels in rat heart, but not centrally. Losses averaged 90% of control 1 day after injection, and 50% at 42 days. The same drug and dose was then administered to 50% of a group of rats which had...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00431782
更新日期:1985-01-01 00:00:00
abstract:RATIONALE:Reduction of body temperature is used as predictor of psychotropic drug action. The cutaneous circulation functions as a heat-loss component of temperature regulation. Clozapine and olanzapine reverse hyperthermia and sympathetically-mediated cutaneous vasoconstriction induced by MDMA (3,4-methylenedioxymetha...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-004-1850-6
更新日期:2004-10-01 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::The effect of 15 min/day of immobilization (IM) stress on oral self-administration (SA) of morphine (0.5 mg/ml) or fentanyl (25 micrograms/ml) and withdrawal was examined in rats. In addition, the role of conditioning factors in these effects was assessed. For each drug, four groups of subjects were exposed for 50 day...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF02253539
更新日期:1993-01-01 00:00:00
abstract:RATIONALE:Studies have shown that social drinkers are poor estimators of alcohol-induced impairment. Underestimates of blood alcohol concentration and other indices of intoxication are associated with decisions to perform risky behaviors, such as operating a motor vehicle. It is possible that self-evaluations of impair...
journal_title:Psychopharmacology
pub_type: 临床试验,杂志文章
doi:10.1007/s00213-004-1964-x
更新日期:2005-02-01 00:00:00
abstract::Each morning eight adults with caffeine versus placebo discrimination histories ingested letter-coded capsules containing 100 mg caffeine or placebo and then engaged in a relaxation or vigilance activity. Subjects were first exposed to caffeine and placebo once each with each activity. Then each day for 10 days subjec...
journal_title:Psychopharmacology
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1007/BF02249332
更新日期:1994-04-01 00:00:00
abstract::Adult hooded rats exposed to a repeated maternal separation procedure during the neonatal period showed a blunted expression of locomotor hyperactivity conditioned to the presentation of the daily food ration. We have demonstrated that the expression of food-conditioned anticipatory hyperactivity is sensitive to the r...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF02246414
更新日期:1996-07-01 00:00:00
abstract:RATIONALE:N-methyl-D-aspartate (NMDA) receptors play crucial roles in learning and memory, but the role of each NMDA receptor subtype in a specific cognitive process is unclear. Non-selective blockers of NMDA receptor are used to model the cognitive impairment in schizophrenia and Alzheimer's disease. Counter-intuitive...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-015-4008-9
更新日期:2015-11-01 00:00:00
abstract::When injected IP, the M1 muscarinic receptor antagonist pirenzepine dose-dependently induced a deficit in passive avoidance learning in rats. This activity was optimal at 75 mg/kg injected 1 h before the acquisition session. The deficit induced by pirenzepine was antagonized by oxotremorine (0.03-0.3 mg/kg SC) and phy...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00444707
更新日期:1989-01-01 00:00:00
abstract:RATIONALE:The cAMP-dependent protein kinase A (PKA) signaling transduction pathway has been shown to play an important role in the modulation of several ethanol-induced behaviors. Different studies have demonstrated intracellular calcium (Ca(2+))-dependent activation of the PKA cascade after ethanol administration. Thu...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-014-3610-6
更新日期:2014-12-01 00:00:00
abstract:RATIONALE:Prepulse inhibition (PPI) and locomotor activity have been used to investigate the effects of antipsychotic and stimulant drugs and their underlying dopaminergic mechanisms. Whereas D2-like agonists consistently decreased PPI and increased locomotion in rats in previous studies, we recently reported that thes...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-006-0511-3
更新日期:2007-04-01 00:00:00
abstract::Serotonin(5-HT)-stimulated intracellular calcium(Ca) mobilization was measured in the platelets of depressed patients to assess 5-HT2 receptor function. The 5-HT-induced Ca response was significantly higher in unmedicated patients with bipolar depression and melancholic major depression than in those with non-melancho...
journal_title:Psychopharmacology
pub_type: 临床试验,杂志文章
doi:10.1007/BF02245204
更新日期:1994-01-01 00:00:00
abstract:RATIONALE:Cannabinoid CB1 receptors are expressed in the prefrontal cortex, but their role in mediating executive functions such as behavioral flexibility is unclear. OBJECTIVE:The present study examined the effect of pharmacological activation or blockade of the cannabinoid CB1 receptors on behavioral flexibility usi...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-006-0421-4
更新日期:2006-08-01 00:00:00
abstract:RATIONALE:Neuromedin-U (NmU) is an agonist at NMU1R and NMU2R. The brain distribution of NmU and its receptors, in particular NMU2R, suggests widespread central roles for NmU. In agreement, centrally administered NmU affects feeding behaviour, energy expenditure and pituitary output. Further central nervous system (CNS...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-004-1918-3
更新日期:2004-12-01 00:00:00
abstract::Herrnstein's matching equation was used to analyze drug effects on performance in random interval reinforcement schedules. Pimozide caused effects compatible with both motor and motivational impairments, in a 5-component multiple schedule, a 3-schedule 3-day cycle (ALT-3), and a 2-schedule 2-day cycle (ALT-2). However...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF02244238
更新日期:1990-01-01 00:00:00
abstract::Benzodiazepines and other compounds which act at benzodiazepine binding sites have been shown previously to attenuate the acquisition of conditioned fear in rodents when administered before the acquisition session, an effect which may parallel the disruption of human memory produced by anxiolytics and sedatives. Such ...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00181243
更新日期:1986-01-01 00:00:00
abstract:RATIONALE:An important goal of addiction research is to discover neurobiological markers that could predict the severity of addiction and help to determine appropriate treatment. Brain-derived neurotrophic factor (BDNF) and thiobarbituric acid reactive substances (TBARS) are being related to cerebral plasticity and imp...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-014-3542-1
更新日期:2014-10-01 00:00:00
abstract:BACKGROUND:Abnormalities of membrane phospholipid metabolism have been described in Alzheimer's disease (AD). We investigated, with the aid of (31)P magnetic resonance spectroscopy, the in vivo intracerebral availability of phosphomonoesters (PME) and phosphodiesters (PDE) in patients with AD. METHODS:Eighteen outpati...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-005-2168-8
更新日期:2005-07-01 00:00:00
abstract:RATIONALE:Typical neuroleptic medications are still administered to as many as 40% of patients receiving antipsychotic treatment in the US. Intermittent administration or interruption of long-term neuroleptic medication for schizophrenia may increase the incidence of human tardive dyskinesias, and similarly may produce...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s002130000572
更新日期:2001-01-01 00:00:00
abstract:RATIONALE:The metabotropic glutamate (mGlu5) receptor subtype 5 antagonist MPEP attenuates self-administration of numerous drugs of abuse. OBJECTIVES:The purpose of the present study was to explore whether MPEP-induced decreases in nicotine and cocaine self-administration reflect attenuation of the reinforcing and inc...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-004-2070-9
更新日期:2005-04-01 00:00:00
abstract:RATIONALE:The majority of volumetric magnetic resonance imaging (MRI) studies of the hippocampus in patients with bipolar disorder (BD) show no differences in hippocampal volume between patients and healthy controls. Significant variability, however, exists in the medication status of patients included in these studies...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-007-0906-9
更新日期:2007-12-01 00:00:00
abstract:RATIONALE:Therapeutic efficacy of antidepressant drugs appears to be related to their ability in producing neuroadaptive changes that restore normal brain function. Activity-regulated cytoskeletal associated protein (Arc) is an effector immediate early gene that plays a fundamental role in activity-dependent neural pla...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-008-1276-7
更新日期:2008-12-01 00:00:00
abstract::The aim of the present study was to investigate the locomotor stimulant effects of the atypical antipsychotic agent, olanzapine, in mice depleted of their dopamine by reserpine and alpha-methyl-DL-p-tyrosine pretreatment. Olanzapine (0.5, 1 and 2 mg/kg) dose-dependently increased locomotor activity, which was complete...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s002130050877
更新日期:1999-02-01 00:00:00