Mepiprazole, a new psychotropic drug: effects on uptake and retention of monoamines in rat brain synaptosomes.


:The influence of mepiprazole (EMD 16,923), a new pyrazol-ylalkyl-piperazine derivative, on the uptake of 3H-norepinephrine (NE), 3H-dopamine (DA), and 3H-serotonin (5-HT) into rat brain synaptosomes from cerebral cortex, corpus striatum, and hypothalamus was investigated in comparison with several psychotropic drugs, including oxypertine, d-amphetamine, imipramine, desipramine, chlorimipramine, amitriptyline, and chlorpromazine in vitro. Mepiprazole was a relatively weak inhibitor of monoamine uptake and exhibited its strongest action on the hypothalamic 5-HT uptake, being almost equipotent with desipramine (IC50 = 0.9 MUM). Furthermore, the influence of the drugs on the retention of 3H-amines previously taken up by whole rat brain synaptosomes was studied. Unlike the tricyclic antidepressants, mepiprazole as well as oxypertine and d-amphetamine markedly increased the efflux of radioactivity during a 20-min incubation at 37 degrees C at low concentrations (10(-6) to 10(-5) M), whereas at 10(-4) M all drugs greatly enhanced the efflux. The ability of mepiprazole to increase 5-HT concentration at the receptor level by a combination of neuronal uptake inhibition and release is discussed in relationship to the central actions of the drug.




Placheta P,Singer E,Kriwanek W,Hertting G




Has Abstract


1976-08-17 00:00:00












  • 2-Bromoterguride-a potential atypical antipsychotic drug without metabolic effects in rats.

    abstract:RATIONALE:Recently, we showed that 2-bromoterguride acted as a dopamine D2 receptor partial agonist, a serotonin 5-HT2A and α2C-adrenergic receptor antagonist, and exhibited antidopaminergic efficacy in amphetamine-induced locomotion (AIL) in rats without inducing catalepsy. OBJECTIVE:To extend our knowledge on the an...


    pub_type: 杂志文章


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

    更新日期:2016-08-01 00:00:00

  • Selective attenuation of the antinociceptive effects of mu opioids by the putative dopamine D3 agonist 7-OH-DPAT.

    abstract:RATIONALE:The purpose of the present investigation was to evaluate the effects of the D3 agonist (+/-)-7-hydroxy-dipropylaminotetralin (7-OH-DPAT), various dopamine (DA) agonists and DA antagonists on the antinociceptive effects of mu opioids. METHODS:Antinociception was assessed using a warm-water tail-withdrawal pro...


    pub_type: 杂志文章


    authors: Cook CD,Rodefer JS,Picker MJ

    更新日期:1999-06-01 00:00:00

  • The practical significance of nortriptyline plasma control. A prospective evaluation under routine conditions in endogenous depression.

    abstract::The problem of the advantage of using nortriptyline (NT) plasma level during treatment for endogenous depression has been approached. In an ordinary psychiatric department, 34 patients had their NT level checked the second week of treatment and their dosage subsequently adjusted, if it was outside the recommended ther...


    pub_type: 临床试验,杂志文章


    authors: Sørensen B,Kragh-Sørensen P,Larsen NE,Hvidberg EF

    更新日期:1978-09-15 00:00:00

  • Role of CA2+/calmodulin on ethanol neurobehavioral effects.

    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...


    pub_type: 杂志文章


    authors: Baliño P,Ledesma JC,Aragon CM

    更新日期:2014-12-01 00:00:00

  • The time and space machine: continuous measurement of drug-induced behavior patterns in the rat.

    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...


    pub_type: 杂志文章


    authors: Stoff DM,Stauderman K,Wyatt RJ

    更新日期:1983-01-01 00:00:00

  • The sigma1 (sigma1) receptor activation is a key step for the reactivation of cocaine conditioned place preference by drug priming.

    abstract:RATIONALE:Cocaine-seeking behavior can be investigated in rodents using the conditioned place preference (CPP) paradigm, in which the drug-paired environment serves as a conditioned stimulus. Such approach allowed to previously demonstrate the importance of the neuromodulatory sigma1 (sigma1) receptor in acquisition of...


    pub_type: 杂志文章


    authors: Romieu P,Meunier J,Garcia D,Zozime N,Martin-Fardon R,Bowen WD,Maurice T

    更新日期:2004-09-01 00:00:00

  • Effects of dopamine antagonists in a two-way active avoidance procedure in rats: interactions with 8-OH-DPAT, ritanserin, and prazosin.

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    pub_type: 杂志文章


    authors: Prinssen EP,Kleven MS,Koek W

    更新日期:1996-11-01 00:00:00

  • Tolerance and selective cross-tolerance to the motivational effects of opioids.

    abstract::The issue of whether tolerance develops to the motivational effects of opioids was addressed by use of an unbiased place preference conditioning procedure. Administration of the mu-opioid agonists morphine or fentanyl produced dose-related preferences for the drug-associated place in control rats. In contrast, the kap...


    pub_type: 杂志文章


    authors: Shippenberg TS,Emmett-Oglesby MW,Ayesta FJ,Herz A

    更新日期:1988-01-01 00:00:00

  • Higher anhedonia during withdrawal from initial opioid exposure is protective against subsequent opioid self-administration in rats.

    abstract:RATIONALE:Understanding factors contributing to individual differences in vulnerability to opioid addiction is essential for developing more effective preventions and treatments, yet few reliable behavioral predictors of subsequent opioid self-administration have been identified in rodents. Sensitivity to the acute eff...


    pub_type: 杂志文章


    authors: Swain Y,Muelken P,Skansberg A,Lanzdorf D,Haave Z,LeSage MG,Gewirtz JC,Harris AC

    更新日期:2020-08-01 00:00:00

  • The relationship between chronic ethanol exposure and cigarette smoking in the laboratory and the natural environment.

    abstract::Few studies have examined the association between ethanol use and cigarette smoking topography. In particular, no study has objectively investigated the relationship between chronic ethanol exposure and cigarette smoking. The aim of this study was to quantify the relationship between cigarette smoking and past and cur...


    pub_type: 杂志文章


    authors: Keenan RM,Hatsukami DK,Pickens RW,Gust SW,Strelow LJ

    更新日期:1990-01-01 00:00:00

  • Correlates of individual differences in compensatory nicotine self-administration in rats following a decrease in nicotine unit dose.

    abstract:RATIONALE:The ability of tobacco harm reduction strategies to produce significant reductions in toxin exposure is limited by compensatory increases in smoking behavior. Characterizing factors contributing to the marked individual variability in compensation may be useful for understanding this phenomenon and assessing ...


    pub_type: 杂志文章


    authors: Harris AC,Pentel PR,LeSage MG

    更新日期:2009-09-01 00:00:00

  • Cocaine-induced reinstatement in rats: evidence for a critical role of cocaine stimulus properties.

    abstract:RATIONALE:The exact behavioral nature of drug-induced reinstatement of drug seeking is still debated. As an incentive, the drug can have general facilitatory influences on appetitive behaviors. As an interoceptive stimulus, the drug can acquire discriminative properties and control behavior. OBJECTIVE:This study asses...


    pub_type: 杂志文章


    authors: Keiflin R,Isingrini E,Cador M

    更新日期:2008-05-01 00:00:00

  • Individual and morphological differences in the behavioural response to apomorphine in rats.

    abstract::The topography of stereotyped behaviour produced by apomorphine in rats was studied by using either a scoring system, based on observation in a wire cage, or by quantification of horizontal and vertical activities, and of the total distances run in an open field, using an automatic recording system. The latter design ...


    pub_type: 杂志文章


    authors: Havemann U,Magnus B,Möller HG,Kuschinsky K

    更新日期:1986-01-01 00:00:00

  • Effect of depletion of brain 5-hydroxytryptamine by 5,7-dihydroxytryptamine on ethanol tolerance and dependence in the rat.

    abstract::Brain 5-hydroxytryptamine (5-HT) was depleted in rats by intraventricular injection with 5,7-dihyroxytryptamine (5,7-DHT) prior to feeding rats a liquid diet containing ethanol. After withdrawal of ethanol, withdrawal reactions were significantly less severe in 5-HT-depleted rats than control rats. Sleeping times afte...


    pub_type: 杂志文章


    authors: Wood JM

    更新日期:1980-01-01 00:00:00

  • N-acetylcysteine augmentation in serotonin reuptake inhibitor refractory obsessive-compulsive disorder.

    abstract:RATIONALE:Dysfunction of glutamatergic neurotransmission has been implicated in the pathophysiology of obsessive-compulsive disorder (OCD) and recent clinical reports suggest that some glutamate modulating agents are efficacious in the treatment of this disorder. N-acetylcysteine (NAC) is a readily available amino acid...


    pub_type: 信件


    authors: Lafleur DL,Pittenger C,Kelmendi B,Gardner T,Wasylink S,Malison RT,Sanacora G,Krystal JH,Coric V

    更新日期:2006-01-01 00:00:00

  • Effects of fluprazine (DU27716) and ethanol on target biting behavior and intruder-evoked attacks.

    abstract::The effects of an "aggression"-reducing drug, fluprazine, and an "aggression"-enhancing drug, ethanol, were evaluated in mice using the target biting and resident-intruder paradigms. Under baseline conditions there was a high target biting rate immediately after the delivery of a 2.0 mA tail shock, an intermediate tar...


    pub_type: 杂志文章


    authors: Wagner GC,Carelli RM

    更新日期:1987-01-01 00:00:00

  • The scopolamine model as a pharmacodynamic marker in early drug development.

    abstract:RATIONALE:Drug development is a high-risk and high failure enterprise, and studies that provide an early read on the pharmacodynamic activity of novel compounds could save time and money, increasing the efficiency of the drug development process. OBJECTIVE:Preclinical and clinical experiments were designed to examine ...


    pub_type: 杂志文章,随机对照试验


    authors: Lenz RA,Baker JD,Locke C,Rueter LE,Mohler EG,Wesnes K,Abi-Saab W,Saltarelli MD

    更新日期:2012-03-01 00:00:00

  • Evidence for the involvement of NMDA receptors in the antidepressant-like effect of nicotine in mouse forced swimming and tail suspension tests.

    abstract:RATIONALE:The antidepressant action of acute nicotine administration in clinical and animal studies is well recognized. But the underlying mechanism for this effect has not been carefully discovered. OBJECTIVES:We attempted to evaluate the possible role of N-Methyl-D-aspartate (NMDA) receptors in the antidepressant-li...


    pub_type: 杂志文章


    authors: Haj-Mirzaian A,Kordjazy N,Haj-Mirzaian A,Ostadhadi S,Ghasemi M,Amiri S,Faizi M,Dehpour A

    更新日期:2015-10-01 00:00:00

  • Psilocybin with psychological support improves emotional face recognition in treatment-resistant depression.

    abstract:RATIONALE:Depressed patients robustly exhibit affective biases in emotional processing which are altered by SSRIs and predict clinical outcome. OBJECTIVES:The objective of this study is to investigate whether psilocybin, recently shown to rapidly improve mood in treatment-resistant depression (TRD), alters patients' e...


    pub_type: 杂志文章


    authors: Stroud JB,Freeman TP,Leech R,Hindocha C,Lawn W,Nutt DJ,Curran HV,Carhart-Harris RL

    更新日期:2018-02-01 00:00:00

  • Buprenorphine versus methadone in the treatment of opioid-dependent cocaine users.

    abstract::This study compared the efficacy of buprenorphine to methadone for decreasing cocaine use in patients with combined opioid and cocaine use. Participants (n = 51) were enrolled in a 26-week treatment program and randomly assigned to either buprenorphine or methadone. Dosing was double-blind and double-dummy. Patients w...


    pub_type: 临床试验,杂志文章,随机对照试验


    authors: Strain EC,Stitzer ML,Liebson IA,Bigelow GE

    更新日期:1994-12-01 00:00:00

  • Amphetamine and maternal behavior: dose response relationships.

    abstract::Primiparous rats received 0.05, 0.25, 0.50, or 1.50 mg d-amphetamine/kg body weight, injected IP, when offspring reached 3-4 and 10-11 days of age. A multidimensional analysis of their maternal behavior revealed that at doses as low as 0.25 mg/kg, amphetamine had a disruptive effect on mother-pup intercontact interval...


    pub_type: 杂志文章


    authors: Piccirillo M,Alpert JE,Cohen DJ,Shaywitz BA

    更新日期:1980-01-01 00:00:00

  • Electrolytic lesions and pharmacological inhibition of the dorsal raphe nucleus prevent stressor potentiation of morphine conditioned place preference in rats.

    abstract:RATIONALE:Exposure to a single session of uncontrollable inescapable shock (IS), but not to identical controllable escapable shock, produces a potentiation of morphine's rewarding properties that is unusual in that the stressor can be given a number of days before the drug administration in an environment quite differe...


    pub_type: 杂志文章


    authors: Will MJ,Der-Avakian A,Bland ST,Grahn RE,Hammack SE,Sparks PD,Pepin JL,Watkins LR,Maier SF

    更新日期:2004-01-01 00:00:00

  • Inhibition of brain dopa-decarboxylase by RO 4-4602 infused ICV blocks alcohol drinking induced in rats by cyanamide.

    abstract::Following the stereotaxic implantation of chronic cannulae for intracerebroventricular (ICV) infusion, rats were given an alcohol preference test to establish their preferred concentration in comparison with water. After alcohol was removed, 15 mg/kg cyanamide was then injected subcutaneously for 4 days in order to ma...


    pub_type: 杂志文章


    authors: Miñano FJ,Myers RD

    更新日期:1989-01-01 00:00:00

  • The role of serotonin in schizophrenia: an overview of the nomenclature, distribution and alterations of serotonin receptors in the central nervous system.

    abstract::Serotonin is a neurotransmitter that is widely distributed throughout the central nervous system. The role of serotonin in schizophrenia is still unclear. Postmortem studies of serotonin receptor subtypes in schizophrenia have been inconclusive for the most part. The most promising findings involve a reduction in 5-HT...


    pub_type: 杂志文章,评审


    authors: Ohuoha DC,Hyde TM,Kleinman JE

    更新日期:1993-01-01 00:00:00

  • Combined effects of buprenorphine and a nondrug alternative reinforcer on i.v. cocaine self-administration in rats maintained under FR schedules.

    abstract::Although previous studies have shown that pharmacological agents, such as buprenorphine, and alternative nondrug reinforcers, such as money or sweetened solutions, reduce cocaine self-administration, few studies have examined the combined effects of these two approaches. The purpose of the present study was to evaluat...


    pub_type: 杂志文章


    authors: Comer SD,Lac ST,Wyvell CL,Carroll ME

    更新日期:1996-06-01 00:00:00

  • Antagonism of the antidepressant-like effects of clenbuterol by central administration of beta-adrenergic antagonists in rats.

    abstract:RATIONALE:Stimulation of central beta(2) adrenergic receptors produces antidepressant-like effects on behavior. At present, it is not known what brain sites are involved in mediating such effects, although some recent evidence suggests the importance of the dorsal hippocampus. OBJECTIVE:Experiments were carried out to...


    pub_type: 杂志文章


    authors: Zhang HT,Huang Y,O'Donnell JM

    更新日期:2003-10-01 00:00:00

  • Joint effects of stress and chronic cannabis use on prospective memory.

    abstract:RATIONALE:Prospective memory pervades our daily lives and failures can have detrimental consequences. This ability to execute delayed intentions may be impacted by stress, yet few studies have examined these effects. Moreover, as many cannabis users report using cannabis to cope with stress, it is important to understa...


    pub_type: 杂志文章


    authors: Cuttler C,Spradlin A,Nusbaum AT,Whitney P,Hinson JM,McLaughlin RJ

    更新日期:2019-06-01 00:00:00

  • An ethopharmacological analysis of the behavioral effects of 8-OH-DPAT.

    abstract::Several behaviors associated with the serotonin syndrome have been reported in rats following administration of the 5-HT1A receptor agonist 8-OH-DPAT. The present investigation approached this phenomenon from an ethopharmacological perspective, and provided a detailed temporal analysis of the behavioral effects of thi...


    pub_type: 杂志文章


    authors: Blanchard RJ,Shepherd JK,Armstrong J,Tsuda SF,Blanchard DC

    更新日期:1993-01-01 00:00:00

  • A comparison of some psychological and physiological effects exerted by zetidoline (DL308) and by oxazepam.

    abstract::In a double-blind, balanced crossover study, eight healthy male volunteers ingested either DL-308 (10 mg), DL-308 (20 mg), oxazepam (30 mg) or placebo. Subjective estimates of coordination and anxiety, objective performance measurements and cardiovascular measurements were taken at 1, 3, 5 and 8 h after ingestion. DL-...


    pub_type: 临床试验,杂志文章,随机对照试验


    authors: Herbert M,Standen PJ,Short AH,Birmingham AT

    更新日期:1983-01-01 00:00:00

  • A reappraisal of the interaction between tricyclic antidepressants and reserpine-like drugs.

    abstract::The administration of trycyclic antidepressants followed by reserpine-like drugs elicits a pattern of stereotyped locomotor activity. Using desmethylimipramine (DMI) followed by tetrabenazine (TBZ), activity could be reliably elicited only in young rats, and only by using very high doses of TBZ. The latency of onset o...


    pub_type: 杂志文章


    authors: Willner P,Clark D

    更新日期:1978-06-15 00:00:00