Quantitative Proteomic Approach Reveals Altered Metabolic Pathways in Response to the Inhibition of Lysine Deacetylases in A549 Cells under Normoxia and Hypoxia.

Growing evidence is showing that acetylation plays an essential role in cancer, but studies on the impact of KDAC inhibition (KDACi) on the metabolic profile are still in their infancy. Here, we analyzed, by using an iTRAQ-based quantitative proteomics approach, the changes in the proteome of -mutated non-small cell lung cancer (NSCLC) A549 cells in response to trichostatin-A (TSA) and nicotinamide (NAM) under normoxia and hypoxia. Part of this response was further validated by molecular and biochemical analyses and correlated with the proliferation rates, apoptotic cell death, and activation of ROS scavenging mechanisms in opposition to the ROS production.

Amineptine, response timing, and time discrimination in the albino rat.

Experiment 1 recorded the effects of single (doses of 1, 5, 10, and 20 mg/kg) and repeated intraperitoneal injections (10 mg/kg) of amineptine (a tricyclic antidepressant drug) on the performance of albino rats in differential reinforcement of low rate (DRL) of 30 s, fixed-interval (FI) of 60 s, and signalled continuous reinforcement (CRF-SD) schedules. In the second experiment, the effects of repeated (10 mg/kg) and single injections (20 mg/kg) were assessed on the discrimination of the duration of auditory stimuli (2 and 8 s). A dose-related increase in response rates was observed in FI and DRL, correlating with a dose-related impairment in the temporal regulation of performance.

Amineptine improves the performance of dogs in a complex temporal regulation schedule.

Amineptine is a tricyclic antidepressant with activating properties, that stimulates spontaneous locomotor activity in rodents and elevates mood in humans. It mainly inhibits dopamine uptake and weakly increased dopamine release. Formulating the hypothesis that this drug would decrease waiting capacity, we decided to test amineptine in a Differential Reinforcement of Response Duration schedule (DRRD 9 s Limited Hold 1.

[Contribution of electrophysiology to the study of tianeptine and other antidepressive agents].

Intravenous perfusion of tianeptine reduces the frequency of coeruleus locus neural discharge. It does not affect the rate of neural discharge in the dorsal raphe, increase the rate of neural discharge in the ventral tegument air and the rate of discharge in the pyramidal cells of the hippocampus (CA1). In comparison, intravenous perfusion of clomipramine decreases the rate of neural discharge in the coeruleus locus, the dorsal raphe, the ventral tegument air (temporarily) and the pyramidal cells of the hippocampus.

Effects of tianeptine on spontaneous alternation, simple and concurrent spatial discrimination learning and on alcohol-induced alternation deficits in mice.

The effects of systemic administration of tianeptine, a new psychotropic agent with antidepressant properties, were investigated on spontaneous alternation behavior, and on simple and concurrent spatial discrimination, in normal mice of the BALB/c strain. Tianeptine increased rates of spontaneous T-maze alternation, facilitated retention of a T-maze left-right discrimination, and speeded up acquisition of concurrent discrimination in a radial maze. These effects were consistent across successive experiments with a dose of 10mg/kg; lower doses (2.

[Electrophysiological study of tianeptine, a new enhancer of serotonin uptake with antidepressant activity].

Tianeptine is a clinically effective antidepressant, not chemically related to classical tricyclic compounds. Its mechanism of action preferentially involves central serotoninergic transmissions, by increasing uptake after acute and chronic administration in rat brain and platelets and in human platelets. We studied the effects of tianeptine on three currently used electrophysiological methods: Ro4-1284 induced PGO waves in the cat, neocortical EEG activity in the acute rat preparation and sleep-wakefulness modifications in chronically implanted rats.

Structure-activity relationships of tricyclic antidepressants, with special reference to tianeptine.

Structure-activity relationships in the classical antidepressant (imipramine-like) series show a relative lack of specificities: Compounds should simply have a nucleus consisting of two phenyl rings and a third, seven-member central ring. This central ring may have one, several, or no heteroatoms, and it may or may not be saturated. The side chain may be attached to any one of the atoms of the central ring, but it must be short (two or three carbon atoms), and have a terminal amine group (secondary, tertiary, or included in a ring).

Pharmacological properties of (N-dicyclopropylmethyl) amino-2-oxazoline (S 3341), an alpha-2 adrenoceptor agonist.

Pharmacological actions of (N-dicyclopropylmethyl)-amino-2-oxazoline (S 3341), an agonist of alpha-2 adrenoceptors, were examined in acute animal studies. In the normotensive anaesthetized dog S 3341 (0.3 mg/kg, i.

[Amineptine, a new antidepressant: pharmacological review (author's transl)].

Amineptine is a tricyclic derivative with a 7-carbon chain of aminoacids. Chemical alterations of the aminoacid chain have revealed its importance in the shaping of the pharmacological effects. The drug is rapidly absorbed.

[New therapeutic indications for a dopamine antagonist, Piribedyl].

Evidence has been found for the view that piribedil stimulates peripheral and central dopamine receptors. Piribedil stimulates the nigro-striatal pathway and has been shown to be an effective antiparkinsonian agent. The stimulation of dopamine receptors in the meso-limbic and/or meso-cortical pathways lead to propose its use in the treatment of affective disorders (maia and depression).

[Influence of the administration of psychopharmacological compounds on the take up time of an alimentary material in the hamster and a study of the associated behaviour (author's transl)].

The take up time of a standardized alimentary material is a simple component of hamster hoarding behaviour. This value was modified by administrations of the following compounds: diazepam, chlorpromazine, meprobamate, apomorphine, d-amphetamine, piribedil, fenfluramine, sulpiride, imipramine, phenobarbital, clonidine and morphine. The change consisted of a varying increase in the take up time, dependent upon the substance and dosage.

Apomorphine and piribedil in rats: biochemical and pharmacologic studies.

We studied the biochemical and pharmacologic modes of action of piribedil and apomorphine in the rat. Although both drugs have many points in common, they are also different in many of their manifestations. Apomorphine causes high-intensity, short-duration stereotyped behavior; it is distributed within the brain in uneven fashion, the striatum being the area of lowest concentration as measured by fluorometry.