Abstract:
: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.
journal_name
Psychopharmacology (Berl)journal_title
Psychopharmacologyauthors
Placheta P,Singer E,Kriwanek W,Hertting Gdoi
10.1007/BF00496865subject
Has Abstractpub_date
1976-08-17 00:00:00pages
295-301issue
3eissn
0033-3158issn
1432-2072journal_volume
48pub_type
杂志文章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...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-016-4356-0
更新日期:2016-08-01 00:00:00
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...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s002130050999
更新日期:1999-06-01 00:00:00
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...
journal_title:Psychopharmacology
pub_type: 临床试验,杂志文章
doi:10.1007/BF00428027
更新日期:1978-09-15 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::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: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...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-004-1814-x
更新日期:2004-09-01 00:00:00
abstract::Using a conditioned avoidance procedure in rats, the present study examined the ability of 8-OH-DPAT, ritanserin, and prazosin to alter the effects of the dopamine antagonists, raclopride and haloperidol, on avoidance- and on escape responding. The 5-HT1A agonist 8-OH-DPAT (0.16 mg/kg) significantly enhanced the inhib...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s002130050124
更新日期:1996-11-01 00:00:00
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...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF02431542
更新日期:1988-01-01 00:00:00
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...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-020-05532-w
更新日期:2020-08-01 00:00:00
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...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF02245794
更新日期:1990-01-01 00:00:00
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 ...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-009-1567-7
更新日期:2009-09-01 00:00:00
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...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-008-1083-1
更新日期:2008-05-01 00:00:00
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 ...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00172869
更新日期:1986-01-01 00:00:00
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...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00427597
更新日期:1980-01-01 00:00:00
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...
journal_title:Psychopharmacology
pub_type: 信件
doi:10.1007/s00213-005-0246-6
更新日期:2006-01-01 00:00:00
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...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00217061
更新日期:1987-01-01 00:00:00
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 ...
journal_title:Psychopharmacology
pub_type: 杂志文章,随机对照试验
doi:10.1007/s00213-011-2456-4
更新日期:2012-03-01 00:00:00
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...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-015-4004-0
更新日期:2015-10-01 00:00:00
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...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-017-4754-y
更新日期:2018-02-01 00:00:00
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...
journal_title:Psychopharmacology
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1007/BF02247469
更新日期:1994-12-01 00:00:00
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...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00435314
更新日期:1980-01-01 00:00:00
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...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-003-1572-1
更新日期:2004-01-01 00:00:00
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...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00444688
更新日期:1989-01-01 00:00:00
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...
journal_title:Psychopharmacology
pub_type: 杂志文章,评审
doi:10.1007/BF02245003
更新日期:1993-01-01 00:00:00
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...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF02246018
更新日期:1996-06-01 00:00:00
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...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-003-1512-0
更新日期:2003-10-01 00:00:00
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...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-019-5184-9
更新日期:2019-06-01 00:00:00
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...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF02247363
更新日期:1993-01-01 00:00:00
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-...
journal_title:Psychopharmacology
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1007/BF00427573
更新日期:1983-01-01 00:00:00
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...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00426790
更新日期:1978-06-15 00:00:00