The ability of antidepressant drugs, electroconvulsive treatment (ECT), or lithium chloride (LiCl), to modify prolactin secretion in the rat was studied. Chlorimipramine, citalopram, fluoxetine, imipramine and zimelidine potentiated the low dose 5‐hydroxytryptophan (5‐HTP)‐induced increase in prolactin secretion, suggesting inhibition of serotonin (5‐HT) uptake by these drugs. Amitriptyline, doxepin, iprindole, mianserin and trazadone inhibited the prolactin stimulating effects of high doses 5‐HTP and quipazine, suggesting that these drugs have 5‐HT receptor blocking properties. Tandamine inhibited only 5‐HTP‐induced increase in prolactin secretion. Chronic administration of imipramine, potentiated the effect of low dose S‐HTP significantly more than an acute dose. Amitriptyline, produced similar inhibition of the 5‐HTP‐induced increase in prolactin secretion after both acute and chronic administration. The ability of bupropion and mazindol to inhibit alpha‐methylparatyrosine‐induced prolactin secretion, and of nomifensine to inhibit reserpine‐induced prolactin secretion, is consistent with other evidence that these agents are indirect dopamine (DA) agonists. Desipramine, acutely, had no effect on any of the above paradigms but after chronic administration, potentiated the effect of low dose 5‐HTP on prolactin secretion. Nortriptyline had no effect on prolactin secretion after acute or chronic treatment. ECT for 10 days did not affect the ability of a 5‐HT agonist or d‐amphetamine to modify prolactin secretion. However, chronic, but not acute, treatment with LiCl markedly enhanced the prolactin response to 5‐HT agonists and reserpine while shifting the dose response curve for d‐amphetamine and apomorphine to the right. These results are discussed in light of current theories of the role of 5‐HT and DA in depression.

1979-09-01·Naunyn-Schmiedeberg's archives of pharmacology4区 · 医学

Effect of acute and chronic treatment of tandamine, a new heterocyclic antidepressant, on biogenic amine metabolism and related activities

4区 · 医学

Article

作者: W. Lippmann ; T. A. Pugsley

The effects of tandamine, a clinically effective heterocyclic antidepressant, administered either acutely (10 mg/kg i.p.) or chronically (10 mg/kg i.p. daily for 21 days) on biogenic amine uptake and metabolism in the rat were determined and a comparison with desipramine was made. Tandamine, similarly to desipramine, blocked norepinephrine (NE) uptake in rat brain and heart following both acute and chronic administration. No effect of tandamine on dopamine (DA) or serotonin (5-HT) uptake was observed. Both drugs lowered endogenous brain NE when given chronically but not acutely. In contrast, no such effect on brain DA and 5-HT or heart NE was observed. Tandamine, like desipramine, administered chronically prior to an intraventricular injection of 3H-NE, produced increases in the decline of 3H-NE as indicated by decreased 3H-NE with increased levels of 3H-normetanephrine in brain stem of rats, suggesting an increased turnover of NE. No such effect was observed following acute treatment. Both drugs increased the behavioural effects of L-Dopa following and acute oral administration, with tandamine appearing superior to desipramine at the lower dose examined (10 mg/kg). Tandamine was 57--833 times less effective in binding to rat brain muscarinic receptors than desipramine, imipramine, butriptyline and amitriptyline, respectively. Thus, tandamine affects biogenic amine mechanism following either acute or chronic administration in a fashion similar to desipramine, but unlike desipramine, it exhibits relatively little anticholinergic properties, a further indication of the potential use of tandamine in the treatment of human depression, particularly where an increase in drive is desired.

1977-01-01·International pharmacopsychiatry

Tandamine--a new norepinephrine reuptake inhibitor. Clinical, psychometric and quantitative EEG studies in depressed patients.

Article

作者: Saletu, B ; Krieger, P ; Grünberger, J ; Schanda, H ; Sletten, I

Tandamine (AY-23,946)- a new norepinephrine reuptake inhibitor with practically no serotonin potentiation, MAO inhibition and anticholinergic activity-was administered in doses from 75 to 200 mg to a group of 20 hospitalized depressed patients. Weekly clinical evaluation including the ECDEU global score. Hamilton score and Zung self-rating score demonstrated a slight improvement which became statistically significant between the 1st and 2nd weeks of therapy. While the 'thymoleptic' properties of the drug were weak, a pronouned 'activating/stimulatory' effect of the drug was noted. Psychometric tests showed an increase in attention, concentration and psychomotor activity as well as an improvement in FPI personality dimensions 'depression' and 'inhibition', while the Taylor anxiety score did not reveal any changes. Digital computer period analysis of the EEG demonstrated, 6 h after oral administration of 50 mg tandamine, a decrease of slow waves, a significant increase of fast activity as well as a significant attenuation of the amplitude variability. Such changes are reminiscent of the pharmaco-EEG profile of psychostimulatory drugs and may represent the neurophysiological correlate for the activating/stimulatory properties of tandamine. Our finding suggest that the well-tolerated drug may be of some benefit for retarded depressions.

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