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PubMedDate not supplied

Phenylalkyl 1,2-diamines as sigma-receptor ligands: the discovery of novel antidepressant agents.

This article focuses on the study of phenylalkyl 1,2-diamines as sigma-receptor ligands for the discovery of antidepressant agents. We synthesized N-chain substituted phenylalkyl 1,2-diamine derivatives. Phenylalkyl 1,2-diamines are one of the most important class of therapeutical medicines useful in managing central nervous system diseases and have been used mainly to treat obesity, narcolepsy, minimal brain dysfunction, and mild depression. In the present study, we found that phenylalkyl 1,2-diamine and amide compounds were strongly bound to the sigma-receptors and showed a potent activity of mice forced swimming test. Our article, after briefly outlining the background and nature of sigma-receptor ligands, explores the antidepressant activity of phenylalkyl 1,2-diamines.

Animals↗
PubMed1992

Benzo[b]thiophenes, II: Novel benzo[b]thienylhydrazine and 1,3,4-oxadiazole derivatives as potential antidepressant agents.

Three novel series of benzo[b]thiophene derivatives bearing various hydrazone, hydrazine and 1,3,4-oxadiazole moieties were synthesized as potential antidepressant agents. 22 Compounds were evaluated for their in vitro inhibitory effect on monoamine oxidase enzyme (MAO) type A. Several compounds inhibited MAO stronger than pargyline hydrochloride. Maximum inhibitions of 83% and 90% were observed with 1-benzyl-2-(3-chlorobenzo[b]thienyl-2-carbonyl)hydrazine (24) and 1-[2-(4-chlorophenyl)ethyl]-2-(3-chlorobenzo[b]thienyl-2- carbonyl)hydrazine (35), respectively.

Animals↗
PubMed1983

[Analysis of acute and chronic effects of antidepressive agents in a learned helplessness model in mice].

In experimental learned helplessness in mice determined by preliminary inavoidable aversive exposure, activity of tricyclic antidepressants (desipramine, chlorimipramine, amitryptyline), type A MAO inhibitors (pyrazidol), and atypical (zimelidine, trazodon, befuralin) antidepressants as well as that of potential antidepressants (LIS-30, DZK-153) were determined upon chronic administration. The tricyclic compounds, befuralin and DZK-153 removed learned helplessness only after 14 days of administration. The substances with a predominant serotoninomimetic action (zimelidin, trazodon in high doses, pyrazidol, LIS-30) showed high efficacy following 6 days of administration. Single administration of the substances under study did not make it possible to disclose their specific antidepressant activity.

Animals↗
PubMed1975

[Postsynaptic attack of tricyclic antidepressive agents in the circulatory system].

Tricyclic antidepressives (TA) exert differential effects on the circulatory system, though all of them have one principle in common: inhibition of back resorption of noradrenaline in the adrenergic synapses. Of more importance, however, seems to be the dose rather than the type of substance used. Smaller doses were found to potentiate the pressoric effects of noradrenaline, while higher doses frequently had an inhibitory action. In rats pretreated with 6-OH-dopamine, only an inhibitory action has been established. It is concluded that the TA must have a postsynaptic influence that becomes effective either through the membrane receptors and/or other factors within the cell.

Amitriptyline↗
PubMed1994

[The effect of antidepressive agents on suicide in depressive patients].

Antidepressants do not only lead to a decrease of depression, they also reduce the frequency of suicidal ideations. Due to insufficient data and contradictory findings it is not possible to determine clearly whether certain antidepressants are more effective in reducing suicidality than others. Nevertheless, there are some findings on selective serotonin reuptake inhibitors which support this hypothesis (Baldwin et al., 1991; Möller, 1992). The hypothesis that antidepressants with a certain mode of action might evoke suicidality in depressive patients under certain circumstances, has not been corrobarated by data derived from controlled studies (Mann u. Kapur, 1991; Derby et al., 1992). The general hypothesis based on clinical experience that non-sedating or activating antidepressants are possibly problematical in depressive suicidal patients, should nevertheless be kept in mind for safety's sake. In rare cases antidepressants like other psychopharmacological drugs, such as benzodiazepines, can evoke aggressive/autoaggressive behaviour.

Antidepressive Agents↗
PubMed1997

[Antidepressive agents and breast feeding].

Postpartum blues occurs in 50-80% of women. A few percent of the cases are classified as serious postpartum depression, requiring antidepressant treatment. There is a growing understanding that women should continue to breast-feed in this situation. Data concerning the transfer of antidepressants into breast milk has been researched. Calculations of the infant relative dose via breast milk were done for the drugs concerned. Few antidepressants have been studied at steady state conditions in nursing mothers. Nortriptyline and amitriptyline have minimal relative doses and can be used when breast-feeding. Doxepine should be avoided, as should lithium, which has a significant transfer. Among the serotonine-reuptake inhibitors fluoxetine has been well studied in breast milk. Since fluoxetine has a long half life and a high transfer, sertraline and possibly paroxetine are better alternatives, but the latter has not yet been studied in repeated doses. Moclobemide also lacks data from multiple dose studies, but extrapolation to steady state indicates that the relative dose is small. More observational studies should be carried out in infants breast-fed by mothers using antidepressants. In the meantime, doctors prescribing antidepressant drugs to nursing mothers should see that the infants are monitored for side effects.

Antidepressive Agents↗
PubMed1994

[Antidepressive agents in non-depressive disorders].

The evaluation of effect of psychotropic medications required clarification of operating diagnostic and of scales sensitive to change. In a second time, these allowed to demonstrate that some antidepressant agents act on pure obsessive-compulsive disorder and on pure panic disorder, i.e. without associated depression. These antidepressants below to different chemical families, but their common action is to act on two main synaptic transmissions: the noradrenergic and the serotoninergic paths.

Antidepressive Agents↗
PubMed1988

Electrophysiological effects of maprotiline, a tetracyclic antidepressant agent, on isolated cardiac preparations.

We studied the effects of maprotiline, a tetracyclic antidepressant agent, on transmembrane potentials recorded from papillary muscles of guinea pigs and sinoatrial nodes of rabbits, using standard microelectrode techniques. Maprotiline (10-100 microM) produced dose-dependent decreases in the maximum rate of rise (Vmax) and action potential duration in papillary muscles, while the resting potential (Em) was not significantly affected. Maprotiline also shifted the Vmax-Em relation to more negative potentials. The slow action potentials of papillary muscles elicited by high [K+]o were also depressed by the drug application. In sinoatrial node cells, maprotiline (above 10 microM) reduced heart rate, Vmax, and action potential amplitude, and increased the action potential duration at half-amplitude. The slope of the phase 4 depolarization was decelerated by the drug. These results suggest that maprotiline depresses not only the fast inward sodium current but also the slow inward calcium current, and that relatively high concentrations of maprotiline exert an inhibitory effect on the electrical activity of the fast- and slow-response fibers of the hearts.

Action Potentials↗
PubMed1979

Substituted 3-amino-1,1-diaryl-2-propanols as potential antidepressant agents.

Following the discovery that 3-(dimethylamino)-1,1-diphenyl-2-propanol hydrobromide (1) possesses potent reserpine-prevention activity in mice, a series of analogues of 1 was synthesized and evaluated as potential antidepressant agents. Several routes to analogues of 1 were evaluated, the most generally applicable of which was the regiospecific ring opening of a suitably functionalized 1,1-diaryl-2,3-epoxypropane (obtained in three stages from the corresponding benzophenone) with the appropriate amine. The more interesting compounds of the series were evaluated for their propensity to cause undesirable peripheral anticholinergic effects, all compounds tested being markedly less active than imipramine on this parameter. On the basis of its good activity in biochemical and pharmacological animal models of depression, together with its relative lack of anticholinergic side effects, 1-(3-chlorophenyl)-3-(dimethylamino)-1-phenyl-2-propanol hydrochloride (20, BRL 14342) was chosen for further evaluation.

Animals↗
PubMed2002

[Breast feeding and treatment with antidepressive agents. A literature review].

Depression after delivery occurs frequently and, apart from being very painful, it may cause disturbance in the child's development. A number of these depressions are so severe that medical antidepressant treatment is indicated. This raises the question whether this kind of treatment should call for interruption of breast-feeding. The problem is, however, that breast-feeding is of major importance to the child, as well as to the mother. A review of present knowledge about the excretion of antidepressants in breast milk and the reports on the possible effects on the child would be useful, in order to create a qualified basis for decision-making, together with the patient, on whether or not to interrupt the breast-feeding. Furthermore, examination of the references would result in concrete guidelines for the most appropriate way of dealing with the treatment, if it is decided to continue the breast-feeding.

Antidepressive Agents↗
PubMed1978

Antidepressant agents. 9. 3,3-Diphenylcyclobutylamines, a new class of central stimulants.

3,3-Diphenylcyclobutylamine (4), N-methyl-3,3-diphenylcyclobutylamine (6), and N,N-dimethyl-3,3-diphenyl-cyclobutylamine (7) have been prepared and tested as potential antidepressant agents. The secondary (6) and tertiary (7) amines strongly decrease the accumulation of NA and 5-HT in brain slices in vitro and in vivo. The cyclobutylamines also cause motor stimulation. The most potent compound in this respect is the tertiary amine 7. The increase in locomotion is not blocked by pretreatment with phenoxybenzamine, methergoline, or alpha-methyltyrosine. Pretreatment with pimozide or reserpine reduces the hyperactivity induced by 7. This hyperstimulation seems to be caused by a mechanism of action which differs from that of amphetamine. 7 may cause increase in locomotion by release of dopamine from granular stores.

5-Hydroxytryptophan↗
PubMed1998

Pharmacokinetic assessment of the sites of first-pass metabolism of BMS-181101, an antidepressant agent, in rats.

The relative contribution of the gut and the liver to the first-pass metabolism of BMS-181101 (3-[3-[4-(5-methoxy-4-pyrimidinyl)-1-piperazinyl]propyl]-5-fluoro-1H-ind ole dihydrochloride), a potential antidepressant agent, has been evaluated in rats. Nine male Sprague-Dawley rats were divided into three groups of three and each rat received a single 20 mg kg(-1) dose of [14C]BMS-181101 via a 30 min constant-rate intravenous infusion, a 30-min constant-rate intraportal infusion or oral gavage. Serial blood samples were collected for 8 h after dosing and plasma was analysed for unchanged BMS-181101 and total radioactivity. Extraction ratios for BMS-181101 by the gut and liver were calculated on the basis of ratios of the area under the plasma BMS-181101 concentration-time curve. The gut had a high intrinsic capacity for metabolizing BMS-181101-extraction ratios were 93% and 10% for the gut and liver, respectively. After oral administration BMS-181101 is sequentially exposed to the gut then the liver. As a result, the contribution of the gut to the overall first-pass effect (ca. 93%) was significantly greater than that of the liver (ca. 0.7%). The estimated total first-pass effect of 94% for BMS-181101 in rats is in excellent agreement with the observed absolute oral bioavailability of 6%. These results clearly illustrate the importance of metabolic activity in the gut for orally administered BMS-181101.

Administration, Oral↗
PubMed1992

Effects of chronic administration and withdrawal of antidepressant agents on circadian activity rhythms in rats.

Experimental and clinical studies indicate that clinical depression may be associated with disturbances of circadian rhythms. To explore the interaction between circadian rhythmicity, behavioral state, and monoaminergic systems, the present study investigated the effects of chronic administration and withdrawal of the following antidepressant agents on circadian wheel-running rhythms of laboratory rats: a) moclobemide, a reversible and selective monoamine oxidase (MAO) type A inhibitor; b) Ro 19-6327, a selective MAO type B inhibitor; c) desipramine, a preferential norepinephrine reuptake inhibitor; d) clomipramine and e) fluoxetine, both serotonin reuptake inhibitors; and f) levoprotiline, an atypical antidepressant whose biochemical mechanism is still unknown. Wheel-running activity rhythms were studied in three inbred strains of laboratory rats (ACI, BH, LEW) under constant darkness (DD). Two of these inbred strains (BH and LEW) show profound abnormalities in their circadian activity rhythms, namely, a reduced overall level of activity and bimodal or multimodal activity patterns. Chronic treatment with moclobemide and desipramine consistently increased the overall level, as well as the circadian amplitude, of the activity rhythm. Furthermore, the abnormal activity pattern of the LEW strain was changed into a unimodal activity pattern like that of other laboratory rats. The free-running period tau was slightly shortened by moclobemide and dramatically shortened by desipramine. Effects of moclobemide and desipramine treatment on overall activity level and duration were reversed shortly after termination of treatment, whereas long aftereffects were observed for the free-running period. All other substances tested had no systematic effects on the activity rhythms of any of the strains. The fact that moclobemide and desipramine altered the period, amplitude, and pattern of circadian activity rhythms is consistent with the hypothesis that monoaminergic transmitters play a significant role in the neuronal control of behavioral state and circadian rhythmicity. Although the present study found that some antidepressives affect parameters of circadian rhythmicity, it could not demonstrate a common effect of all classes of antidepressives.

Animals↗
PubMed1996

[Controlled long-term prevention of unipolar depression with antidepressive agents of the second generation (SSRI)].

Relapse and recurrence are common following successful short-term treatment of unipolar depression. Evidence from a number of controlled double-blind investigations indicates that a patient with a history of depressive episodes is best protected against future episodes by being maintained on the same antidepressant agent at the same dose that was used to treat the acute episode. Newer agents, such as paroxetine, sertraline, and fluoxetine, have been studied in controlled manner for up to one year. The effectiveness of the SSRI in preventing recurrence of depression has been well established in six investigations.

Antidepressive Agents, Second-Generation↗