Abstract:
RATIONALE:Serotonin (5-HT) and norepinephrine (NE) re-uptake inhibitors (SNRIs) have been proposed to have a higher efficacy and/or faster onset of action than previously available antidepressants. OBJECTIVES:We examined in biochemical, electrophysiological and behavioural assays the antidepressant properties of (S)-(-)-4-[(3-fluorophenoxy)-phenyl]methyl-piperidine (F-98214-TA), a compound that displays very high affinity for 5-HT and NE transporters. RESULTS:F-98214-TA potently inhibited the uptake of both 5-HT and NE into rat brain synaptosomes (IC50 = 1.9 and 11.2 nM, respectively) and decreased the electrical activity of dorsal raphe serotonergic neurones (ED50 = 530.3 microg/kg i.v.), an effect completely abolished by the 5-HT(1A) antagonist WAY100,635. In acute behavioural assays in mice, the orally administered compound potentiated the 5-hydroxy-tryptophan (5-HTP)-induced syndrome [minimal effective dose (MED) = 10 mg/kg], antagonized the hypothermia induced by a high dose of apomorphine (ED50 = 2 mg/kg) and reduced the immobility in the tail suspension test (MED = 10 mg/kg). Moreover, it also decreased the immobility in the forced swimming test in mice and rats (30 mg/kg, p.o.). Chronic administration of F-98214-TA (14 days, 30 mg kg(-1) day(-1), p.o.) attenuated the hyperactivity induced by olfactory bulbectomy in rats, confirming its antidepressant-like properties. Interestingly, the same dosage regimen significantly increased the social interaction time in rats, suggesting an additional potential anxiolytic activity. In most assays the compound was more potent than fluoxetine, venlafaxine and desipramine. CONCLUSIONS:F-98214-TA is a novel SNRI that displays greater potency than other reference antidepressants in animal models predictive of antidepressant and anxiolytic activities.
journal_name
Psychopharmacology (Berl)journal_title
Psychopharmacologyauthors
Artaiz I,Zazpe A,Innerárity A,Del Olmo E,Díaz A,Ruiz-Ortega JA,Castro E,Pena R,Labeaga L,Pazos A,Orjales Adoi
10.1007/s00213-005-0087-3subject
Has Abstractpub_date
2005-11-01 00:00:00pages
400-13issue
3eissn
0033-3158issn
1432-2072journal_volume
182pub_type
杂志文章abstract:RATIONALE:Animal models of alcohol-seeking are useful for understanding alcohol addiction and for treatment development, but throughput in these models is limited by the extensive pretraining required to overcome the aversive taste of ethanol. Work by Augier et al. (Psychopharmacology 231: 4561-4568, 2014) indicates th...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-017-4824-1
更新日期:2018-04-01 00:00:00
abstract:RATIONALE:Varenicline is believed to work, in part, by reducing craving responses to smoking cues and by reducing general levels of craving; however, these hypotheses have never been evaluated with craving assessed in the natural environments of treatment-seeking smokers. OBJECTIVES:Ecological momentary assessment pro...
journal_title:Psychopharmacology
pub_type: 杂志文章,随机对照试验
doi:10.1007/s00213-012-2698-9
更新日期:2012-09-01 00:00:00
abstract::The 2-[14C]deoxyglucose method was used to compare the effects of the acute administration of cocaine by two different routes, intravenous and intraperitoneal, on rates of local cerebral glucose utilization in freely moving rats. Doses were initially chosen on the basis of their ability to elicit equivalent increases ...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF02244931
更新日期:1993-01-01 00:00:00
abstract::Haloperidol disposition has been associated with reversible metabolism: it is reversibly reduced to its metabolite, reduced haloperidol, which has less pharmacologic activity than the parent compound. To characterize the interconversion process, six healthy male schizophrenics were administered a single dose of 10 mg ...
journal_title:Psychopharmacology
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1007/BF02253726
更新日期:1990-01-01 00:00:00
abstract::This study tested placebo responses in psychomotor performance when caffeine or alcohol was expected. Fifty male university students were assigned to one of four placebo groups or to a no-treatment control group. Two groups received placebo caffeine and two received placebo alcohol. Subjects performed 12 trials on a p...
journal_title:Psychopharmacology
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1007/BF02245081
更新日期:1994-07-01 00:00:00
abstract::In order to study the role of dopamine (DA) in the regulation of seizure mechanisms in man, a non-emetic dose of apomorphine, a direct stimulant of DA receptors, was administered to eight patients effected by different types of epilepsy. The EEG changes induced by apomorphine administration in comparison to those elic...
journal_title:Psychopharmacology
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1007/BF00427814
更新日期:1983-01-01 00:00:00
abstract:RATIONALE:Little is known about the smoking topography characteristics of heavy cannabis users. Such measures may be able to predict cannabis use-related outcomes and could be used to validate self-reported measures of cannabis use. OBJECTIVES:The current study was conducted to measure cannabis smoking topography char...
journal_title:Psychopharmacology
pub_type: 临床试验,杂志文章
doi:10.1007/s00213-011-2480-4
更新日期:2012-03-01 00:00:00
abstract:RATIONALE:Electrophysiological studies have identified a scalp potential, the late positive potential (LPP), which is modulated by the emotional intensity of observed stimuli. Previous work has shown that the LPP reflects the modulation of activity in extrastriate visual cortical structures, but little is known about t...
journal_title:Psychopharmacology
pub_type: 杂志文章,随机对照试验
doi:10.1007/s00213-011-2426-x
更新日期:2012-02-01 00:00:00
abstract:RATIONALE:Chronic stress and corticosterone have been shown to affect serotonin (5-HT) neurotransmission; however, the influence of stress on the activity of the dorsal raphe nucleus (DRN), the main source of 5-HT in the forebrain, is not well understood. In particular, it is unknown if and how stress modifies DRN 5-HT...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-018-5045-y
更新日期:2018-12-01 00:00:00
abstract:RATIONALE:There is a requirement to ensure that UK armed forces are provided with the best possible medical countermeasures to prevent or mitigate the effects of exposure to nerve agents. When pretreatments are under consideration, it is of particular importance to ensure that they do not in themselves give rise to adv...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-002-1324-7
更新日期:2003-03-01 00:00:00
abstract:RATIONALE:Studies of ethanol's effects on TSH carried out during the daytime, when its secretion is at its nadir, do not reflect the true action of alcohol on TSH secretion since TSH peak occurs at night. OBJECTIVE:The present study investigated the effects of alcohol on the serum concentrations of TSH in healthy volu...
journal_title:Psychopharmacology
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1007/s00213-003-1532-9
更新日期:2003-11-01 00:00:00
abstract:INTRODUCTION:Alterations in protein kinase (PKA) protein levels have been implicated in the regulation of responses to and development of cocaine addiction. However, the contribution of differences in PKA intracellular cascade to the known sex differences in responses to cocaine is not well understood. This study exami...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-008-1411-5
更新日期:2009-04-01 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::It has been shown that pretreatment with dopamine (DA) receptor blockers disrupts the effect of intravenously (IV) and intracerebrally (ICV), but not intraperitoneally (IP) administered cocaine on place preference conditioning (PPC). The present study was undertaken to further evaluate possible differences between IV ...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00735892
更新日期:1988-01-01 00:00:00
abstract::Effects of two dosages of rubidium chloride on exploration, locomotion, rearing and immobility were assessed for male and female rats in an exploration box and an open field. In contrast to previous findings, rubidium was found to decrease locomotion and rearing in the exploratory box, and also to decrease locomotion ...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00426740
更新日期:1979-03-22 00:00:00
abstract::Roxindole is a potent autoreceptor-selective dopamine agonist with additional properties as a serotonin reuptake inhibitor and 5-HT1A agonist. In order to get more insight into its mode of action in various psychiatric populations, we evaluated the effects of subchronic roxindole treatment on pituitary and adrenal hor...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF02246221
更新日期:1995-02-01 00:00:00
abstract::The increasing interest in subjective well-being and quality of life of schizophrenic patients represents a conceptual shift in therapeutic outcome criteria. Symptom reduction alone was the most essential outcome parameter for a long time; with the development of atypical antipsychotics more ambitious success criteria...
journal_title:Psychopharmacology
pub_type: 杂志文章,评审
doi:10.1007/s00213-002-1052-z
更新日期:2002-06-01 00:00:00
abstract::Food intake of four adult male baboons (Papio c. anubis) was monitored during daily experimental sessions lasting 22 h. Food was available under a two-component operant schedule. Following completion of the first "procurement component" response requirement, access to food, i.e., a meal, became available under the sec...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00439545
更新日期:1989-01-01 00:00:00
abstract::A simple new method, the "tape test" has been developed for studying the enhancement of learning by drugs in "learning-dull" rats. A piece of adhesive tape is pressed on the left front pad of the rats. The time of tape removal by the animal, i.e., the problem-solving time is measured. In our experiments the selected l...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00423313
更新日期:1976-07-09 00:00:00
abstract::Acute and chronic effects of ethosuximide (40, 80, and 120 mg/kg), phenytoin (2.5, 5, and 7.5 mg/kg), clonazepam (0.25, 0.5, and 0.75 mg/kg), and valproic acid (40, 80, and 120 mg/kg) were examined in pigeons performing under a delayed-matching-to-sample procedure. Acute administration of clonazepam or valproic acid p...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00180828
更新日期:1986-01-01 00:00:00
abstract::The results confirm that NMDA receptor blockade can result in improved retention performance of mice in step-down passive avoidance. A series of behavioural variations and analyses revealed that memory in the task depended mainly on the appearance of the grid that had been associated with shock, rather than on the exe...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF02244300
更新日期:1991-01-01 00:00:00
abstract::Young adult rats (5 months) were compared with aged (28 months) rats in their ability to learn and perform in a diazepam drug discrimination. Both groups of rats were drug naive at the onset of the experiment. Adult and aged animals learned to discriminate diazepam. In general, the response rates under both drug and v...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00187245
更新日期:1987-01-01 00:00:00
abstract:RATIONALE:Withdrawal seizure-prone and withdrawal seizure-resistant mice were selectively bred to exhibit differences in handling-induced convulsion severity during ethanol withdrawal. The glutamatergic system has been implicated in seizure activity as well as ethanol withdrawal symptoms. OBJECTIVE:This study assessed...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s002130050933
更新日期:1999-04-01 00:00:00
abstract:RATIONALE AND OBJECTIVE:Drug-associated memories are hypothesized to underlie the high risk of relapse in addiction. Recent studies show that post-retrieval extinction training erases fear memories by reconsolidation blockade. Here, we examine the efficacy of this non-invasive procedure in rats with drug-associated mem...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-011-2545-4
更新日期:2012-05-01 00:00:00
abstract:RATIONALE:Converging evidence suggests that dopaminergic and serotonergic mechanisms affect distinct aspects of cognitive performance. Experiments using the rodent five-choice reaction time task have established a critical role for dopaminergic mechanisms in the rat medial prefrontal cortex (mPFC), but have yielded onl...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-002-1227-7
更新日期:2003-01-01 00:00:00
abstract:RATIONALE:During the last few decades, alcohol use disorders (AUD) have reached an epidemic prevalence, yet social influences on alcoholism have not been fully addressed. Several factors can modulate alcohol intake. On one hand, stress can reinforce ethanol-induced behaviors and be an important component in AUD and alc...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-019-05408-8
更新日期:2020-03-01 00:00:00
abstract:RATIONALE:We recently reported that simultaneous exposure to amphetamine and various stressors resulted in reduced hypothalamic-pituitary-adrenal (HPA) and glycemic responses to the stressors. Since this is a new and relevant phenomenon, we wanted to further explore this interaction. OBJECTIVES:This study aims (i) to ...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/s00213-017-4675-9
更新日期:2017-10-01 00:00:00
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
更新日期:1977-08-16 00:00:00
abstract::Two experiments were conducted to test the hypothesis that tolerance to the hypothermic effect of ethanol fails to develop if rats are denied the unconditional stimulus represented by hypothermia. In both experiments, rats were injected with either ethanol (1.9 or 2.5 g/kg) or saline and given microwave hyperthermia (...
journal_title:Psychopharmacology
pub_type: 杂志文章
doi:10.1007/BF00175187
更新日期:1986-01-01 00:00:00
abstract:RATIONALE:Zotepine is an antipsychotic drug with proven efficacy for treatment of acute episodes of schizophrenia. Antipsychotic drugs also require to be effective in prevention of recurrence. OBJECTIVE:This trial was designed to compare the effects of zotepine and placebo in the prevention of recurrence of acute epis...
journal_title:Psychopharmacology
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1007/s002130000452
更新日期:2000-06-01 00:00:00