Human studies on the benzodiazepine receptor antagonist beta-carboline ZK 93 426: antagonism of lormetazepam's psychotropic effects.

Abstract:

:The effects of lormetazepam (0.03 mg/kg IV) a benzodiazepine (BZ) derivative in combination with ZK 93 426 (0.04 mg/kg IV) a beta-carboline, benzodiazepine receptor antagonist were evaluated in humans. Independently, the effects of ZK 93 426 on its own were investigated. A psychometric test battery to evaluate sedation (visual analog scales (VAS), anxiolysis (state-trait-anxiety inventory scale (STAIG X1) and cognitive functions [logical reasoning test (LR), letter detection test (LD)] was applied before and several hours after initiation of treatment. Multiple sleep latency test (MSLT), which measures day time sleepiness, was also applied. Vigilosomnograms analysed from standard EEG recordings were evaluated shortly before and for 1 h after treatment. Treatment started with an intravenous injection of either lormetazepam (LMZ) or placebo (PLA), which was followed 30 min later by administration of either ZK 93 426 or placebo; thus four treatment groups were created (PLA + PLA, LMZ + PLA, LMZ + ZK 93 426 and PLA + ZK 93 426). ZK 93 426 antagonized the sedative and hypnotic effect of LMZ as estimated by MSLT and vigilosomnograms, respectively. Impairment of cognitive functions (LR and LD) induced by LMZ was also antagonized by ZK 93 426. ZK 93 426 had no effect on the changes in the time estimation seen in the LMZ group. Furthermore, ZK 93 426 on its own increased vigilance (alertness) as measured by the vigilosomnogram. A competitive antagonism at the benzodiazepine binding site between ZK 93 426 and LMZ is suggested by their combination effects; the intrinsic activity of ZK 93 426 seems to be due to its weak partial inverse agonist component.

journal_title

Psychopharmacology

authors

Duka T,Goerke D,Dorow R,Höller L,Fichte K

doi

10.1007/BF00172956

subject

Has Abstract

pub_date

1988-01-01 00:00:00

pages

463-71

issue

4

eissn

0033-3158

issn

1432-2072

journal_volume

95

pub_type

临床试验,杂志文章
  • Basolateral amygdala inactivation abolishes conditioned stimulus- and heroin-induced reinstatement of extinguished heroin-seeking behavior in rats.

    abstract:RATIONALE:Drug-paired stimuli elicit drug craving and relapse in addicts and drug-seeking behavior in rats. The functional integrity of the basolateral amygdala (BLA) is necessary for reinstatement of cocaine-seeking behavior elicited by cocaine-conditioned stimuli, but not by cocaine itself. It is unclear, however, wh...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/s00213-001-0997-7

    authors: Fuchs RA,See RE

    更新日期:2002-04-01 00:00:00

  • Effects of 2-bromoterguride, a dopamine D2 receptor partial agonist, on cognitive dysfunction and social aversion in rats.

    abstract:RATIONALE:2-Bromoterguride, a dopamine D2 receptor partial agonist with antagonist properties at serotonin 5-HT2A receptors and α2C-adrenoceptors, meets the prerequisites of a putative atypical antipsychotic drug (APD). We recently showed that 2-bromoterguride is effective in tests of positive symptoms of schizophrenia...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/s00213-017-4747-x

    authors: Tarland E,Franke RT,Fink H,Pertz HH,Brosda J

    更新日期:2018-01-01 00:00:00

  • Quantitative analysis of the effects of some "atypical" and "conventional" antipsychotics on progressive ratio schedule performance.

    abstract:RATIONALE:Performance on progressive ratio schedules has been proposed as a means of assessing the effects of drugs on the value or "efficacy" of reinforcers. A mathematical model affords a basis for quantifying the effects of drugs on progressive ratio schedule performance. According to this model, the relation betwee...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/s00213-004-2049-6

    authors: Zhang Z,Rickard JF,Asgari K,Body S,Bradshaw CM,Szabadi E

    更新日期:2005-05-01 00:00:00

  • 5-HT2C receptors are involved in the discriminative stimulus effects of citalopram in rats.

    abstract::Rats were trained on a fixed ratio 10, food-reinforced schedule to recognize a discriminative stimulus (DS) elicited by the selective serotonin (5-HT) reuptake inhibitor (SSRI), citalopram (2.5 mg/kg, IP). The preferential, high efficacy agonist at 5-HT2C receptors, Ro60-0175, dose-dependently generalized to citalopra...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/s002130050910

    authors: Millan MJ,Girardon S,Dekeyne A

    更新日期:1999-03-01 00:00:00

  • The mGluR5 antagonist MPEP selectively inhibits the onset and maintenance of ethanol self-administration in C57BL/6J mice.

    abstract:RATIONALE:Many of the biochemical, physiological, and behavioral effects of ethanol are known to be mediated by ionotropic glutamate receptors. Emerging evidence implicates metabotropic glutamate receptors (mGluRs) in the biobehavioral effects of ethanol and other drugs of abuse, but there is little information regardi...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/s00213-005-0217-y

    authors: Hodge CW,Miles MF,Sharko AC,Stevenson RA,Hillmann JR,Lepoutre V,Besheer J,Schroeder JP

    更新日期:2006-01-01 00:00:00

  • Characteristics of oral movements in rats during and after chronic haloperidol and fluphenazine administration.

    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

    authors: See RE,Levin ED,Ellison GD

    更新日期:1988-01-01 00:00:00

  • Simulated public speaking as a model of clinical anxiety.

    abstract::Normal male volunteers took single acute doses of either diazepam or placebo under double-blind conditions in three simulated public speaking experiments. Measures of palmar sweating and subjective anxiety showed that anticipation of speaking in public increased anxiety relative to baseline and prestress conditions, a...

    journal_title:Psychopharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1007/BF00436092

    authors: McNair DM,Frankenthaler LM,Czerlinsky T,White TW,Sasson S,Fisher S

    更新日期:1982-01-01 00:00:00

  • Pharmacological specificity of enhanced sensitivity to naltrexone in rats.

    abstract::Rats treated weekly with cumulative doses (1-100 mg/kg, IP) of naltrexone develop an enhanced sensitivity to the operant response-rate decreasing effect of naltrexone. In the present experiment the pharmacological specificity of that enhanced sensitivity was determined by testing a variety of drugs for cross-sensitivi...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/BF02246951

    authors: Schindler CW,Goldberg SR,Katz JL

    更新日期:1993-01-01 00:00:00

  • Oxidative stress and BDNF as possible markers for the severity of crack cocaine use in early withdrawal.

    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

    authors: Sordi AO,Pechansky F,Kessler FH,Kapczinski F,Pfaffenseller B,Gubert C,de Aguiar BW,de Magalhães Narvaez JC,Ornell F,von Diemen L

    更新日期:2014-10-01 00:00:00

  • Cocaine self-administration in rats with histories of cocaine exposure and discrimination.

    abstract:RATIONALE:Interrelationships between the discriminative stimulus and reinforcing properties of psychoactive drugs and the way in which they may interact to control drug intake are unclear. Studies have shown that drug history can influence the expression of drug-produced behavioral effects. OBJECTIVE:The present study...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/s00213-006-0364-9

    authors: Childs E,Shoaib M,Stolerman IP

    更新日期:2006-06-01 00:00:00

  • Lithium ions inhibit function of low- but not high-affinity muscarinic receptors of murine neuroblastoma cells (clone N1E-115).

    abstract::Murine neuroblastoma cells (clone N1E-115) possess both high- and low-affinity muscarinic receptors. The low-affinity muscarinic receptor, when stimulated, initiates the formation of cyclic GMP by activating the enzyme guanylate cyclase; whereas stimulation of the high-affinity receptor inhibits prostaglanding E1-medi...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00427901

    authors: Kanba S,Pfenning M,Richelson E

    更新日期:1985-01-01 00:00:00

  • Delta 9-tetrahydrocannabinol sensitization of the rat brain to direct cholinergic stimulation.

    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

    authors: Duncan GE,Dagirmanjian R

    更新日期:1979-02-28 00:00:00

  • Effects of combined escitalopram and aripiprazole in rats: role of the 5-HT1a receptor.

    abstract:RATIONALE:Pre-clinical and clinical studies have suggested that the antidepressant efficacy of escitalopram (ESC) can be augmented by co-administration of aripiprazole (ARI). OBJECTIVE:To establish if the effects of ESC + ARI can be altered by modulating the 5-HT1a receptor. METHODS:Sprague-Dawley male rats received ...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/s00213-019-05225-z

    authors: Lapointe T,Hudson R,Daniels S,Melanson B,Zhou Y,Leri F

    更新日期:2019-07-01 00:00:00

  • Caffeine enhances the stimulant effect of methamphetamine, but may not affect induction of methamphetamine sensitization of ambulation in mice.

    abstract::Methamphetamine (MAP: 1 and 2 mg/kg SC) and caffeine (CAF: 1, 3, 10 and 30 mg/kg SC) dose-dependently increased ambulation in mice. Repeated administration (5 times at 3 to 4-day intervals) of MAP, but not CAF, induced sensitization to its effect. Furthermore, the mice repeatedly receiving CAF showed no significant ch...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/BF02245053

    authors: Kuribara H

    更新日期:1994-10-01 00:00:00

  • IBZM SPECT imaging of striatal dopamine-2 receptors in psychotic patients treated with the novel antipsychotic substance quetiapine in comparison to clozapine and haloperidol.

    abstract::We investigated the striatal dopamine-2 (D2) receptor occupancy caused by different antipsychotic substances in 18 psychotic patients (16 with schizophrenic and two with schizoaffective disorder according to DSM-IV) with single photon emission computed tomography (SPECT) using 123I-iodobenzamide (IBZM) as tracer subst...

    journal_title:Psychopharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1007/s002130050409

    authors: Küfferle B,Tauscher J,Asenbaum S,Vesely C,Podreka I,Brücke T,Kasper S

    更新日期:1997-10-01 00:00:00

  • Extrasynaptic GABAA receptor activation reverses recognition memory deficits in an animal model of schizophrenia.

    abstract:RATIONALE:Schizophrenia is a complex psychiatric disorder comprised of three main classes of symptoms: positive, negative and cognitive symptoms. Currently, no approved treatment exists for the cognitive symptoms. There is thus a great need for research aiming at identifying novel targets for treatment of this indicati...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/s00213-010-2039-9

    authors: Damgaard T,Plath N,Neill JC,Hansen SL

    更新日期:2011-03-01 00:00:00

  • Chronic ethanol exposure results in increased acute functional tolerance in selected lines of HAFT and LAFT mice.

    abstract:RATIONALE AND OBJECTIVES:Functional (pharmacodynamic) ethanol tolerance can be evidenced within a single session of exposure to ethanol (acute or within-session tolerance), or after repeated ethanol exposures (chronic or between-session tolerance). To investigate whether acute and chronic tolerance to ethanol are inter...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/s002130100722

    authors: Wu PH,Tabakoff B,Szabó G,Hoffman PL

    更新日期:2001-06-01 00:00:00

  • Phospholipase C, Ca2+, and calmodulin signaling are required for 5-HT2A receptor-mediated transamidation of Rac1 by transglutaminase.

    abstract:RATIONALE:Serotonin and especially serotonin 2A (5-HT(2A)) receptor signaling are important in the etiology and treatment of schizophrenia and affective disorders. We previously reported a novel 5-HT(2A) receptor effector, increased transglutaminase (TGase)-catalyzed transamidation, and activation of the small G protei...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/s00213-010-1984-7

    authors: Dai Y,Dudek NL,Li Q,Muma NA

    更新日期:2011-02-01 00:00:00

  • Role of orexin/hypocretin in conditioned sucrose-seeking in rats.

    abstract:RATIONALE:The orexin/hypocretin system has recently been implicated in reward-seeking, especially for highly salient food and drug rewards. We reasoned that this system may be strongly engaged during periods of reward restriction, including food restriction. OBJECTIVES:This study examined the involvement of the orexin...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/s00213-012-2902-y

    authors: Cason AM,Aston-Jones G

    更新日期:2013-03-01 00:00:00

  • Effect of combined or separate administration of piracetam and choline on learning and memory in the rat.

    abstract::Different groups of rats received combined or separate administration of different doses of piracetam (P1:100, P2:200, and P4:400 mg/kg) and choline (C1:100 and C2:200 mg/kg). Compared to control treatment, C1 significantly improved performance in a delayed alternation (DA) task, while P1, P2, P4 or P1C1 had no effect...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00215480

    authors: Ennaceur A,Delacour J

    更新日期:1987-01-01 00:00:00

  • The effects of haloperidol on the EEG spectrum.

    abstract::A placebo-controlled study with six normal volunteers was carried out using 1 mg haloperidol IM. In some EEG frequency bands, the power density due to haloperidol appeared to increase or decrease depending on the subject. Nevertheless, if the results of the six subjects are taken together, the effects of haloperidol a...

    journal_title:Psychopharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1007/BF00431753

    authors: Wieneke GH,Verhoeven WM,Westenberg HG,de Wilde H,Lopes da Silva FH,van Praag M,Storm van Leeuwen W

    更新日期:1981-01-01 00:00:00

  • Discriminative stimulus properties of the atypical antidepressant, mirtazapine, in rats: a pharmacological characterization.

    abstract:RATIONALE:Though interoceptive properties of antidepressants have been described, discriminative stimulus (DS) properties of mirtazapine, which does not affect monoamine reuptake, remain uncharacterized. OBJECTIVES:The objectives of the study are to train rats to recognize a mirtazapine DS, then perform substitution s...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/s00213-008-1259-8

    authors: Dekeyne A,Millan MJ

    更新日期:2009-04-01 00:00:00

  • Effects of accumbens DALA microinjections on brain stimulation reward and behavioral activation in intact and 6-OHDA treated rats.

    abstract::The effects of bilateral nucleus accumbens microinjections of d-ala-met-enkephalinamide (DALA) were assessed in behavioral activation and lateral hypothalamic self-stimulation (LHSS) rate-frequency curve-shift paradigms in normal and accumbens 6-OHDA (4.0 micrograms) treated rats. Microinjections of DALA (2.5 microgra...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/BF02244999

    authors: Johnson PL,Stellar JR

    更新日期:1994-05-01 00:00:00

  • Amygdaloid zif268 participated in the D-cycloserine facilitation effect on the extinction of conditioned fear.

    abstract:RATIONALE:The involvement of glutamate in fear extinction is perhaps the most promising in terms of facilitating clinical interventions for posttraumatic stress disorder (PTSD). This study was aimed at elucidating the possible role of zif268 on the D-cycloserine (DCS) facilitation effect on extinction. OBJECTIVE:We in...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/s00213-015-4042-7

    authors: Wu IT,Tang TH,Ko MC,Chiu CY,Lu KT

    更新日期:2015-10-01 00:00:00

  • Alcohol-associated conditioned reinforcement.

    abstract::Research was conducted to examine the ability of alcohol to impart conditioned reinforcement. Rats were allowed to self-administer solutions of either saline or alcohol (25, 50, and 100 mg/kg/infusion) by the intragastric route. Superimposed on the infusion interval was a buzzer (conditioned reinforcing stimulus). Tes...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00492355

    authors: Smith SG,Werner TE,Davis WM

    更新日期:1977-08-16 00:00:00

  • Quantitative assessment of the microstructure of rat behavior: II. Distinctive effects of dopamine releasers and uptake inhibitors.

    abstract::The effects of four indirect dopamine agonists, d-amphetamine (0.25-4.0 mg/kg), cocaine (2.5-40.0 mg/kg), GBR 12909 (10.0-30.0 mg/kg), and nomifensine (5.0-20.0 mg/kg), on the behavioral organization of movements in an unconditioned motor paradigm were investigated in rats. The extended scaling hypothesis using the fl...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/BF02245696

    authors: Paulus MP,Callaway CW,Geyer MA

    更新日期:1993-01-01 00:00:00

  • Anxiogenic properties of beta-CCE and FG 7142: a review of promises and pitfalls.

    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

    authors: Thiébot MH,Soubrié P,Sanger D

    更新日期:1988-01-01 00:00:00

  • Precipitating factors in spontaneous recurrence of methamphetamine psychosis.

    abstract::This paper examines noradrenergic hyperactivity in response to stress in the development of spontaneous recurrences of methamphetamine (MAP) psychosis, a phenomenon known as flashbacks, in studies of psychedelic drug use. We studied predictors of flashbacks in 36 subjects with flashbacks, along with 80 subjects with a...

    journal_title:Psychopharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1007/s002130050453

    authors: Yui K,Ishiguro T,Goto K,Ikemoto S

    更新日期:1997-12-01 00:00:00

  • Stress- and cue-elicited craving and reactivity in marijuana-dependent individuals.

    abstract:RATIONALE:Cue-elicited craving and stress responses have been identified as predictors of relapse in drug dependence, but little research exists on the contribution of these factors to marijuana use specifically. OBJECTIVES:The aims of the present study were to evaluate (1) responses to a psychological stressor, (2) r...

    journal_title:Psychopharmacology

    pub_type: 杂志文章,随机对照试验

    doi:10.1007/s00213-011-2376-3

    authors: McRae-Clark AL,Carter RE,Price KL,Baker NL,Thomas S,Saladin ME,Giarla K,Nicholas K,Brady KT

    更新日期:2011-11-01 00:00:00

  • Relationship between ecstasy use and depression: a study controlling for poly-drug use.

    abstract:RATIONALE:3,4-Methylenedioxymethamphetamine (MDMA or "ecstasy") causes serotonin neuron damage in laboratory animals. The serotonin system is known to be important in the regulation of mood. Previous research has shown that MDMA users score higher on self-report ratings of depression than controls. However, MDMA users ...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/s00213-003-1705-6

    authors: Roiser JP,Sahakian BJ

    更新日期:2004-05-01 00:00:00