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.

01 Sep 1979·Naunyn-Schmiedeberg's Archives of PharmacologyQ4 · MEDICINE

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

Q4 · MEDICINE

Article

Author: 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.

01 Jan 1977·PsychopharmacologyQ3 · MEDICINE

Clinical pharmacological studies of tandamine, a potential antidepressive drug

Q3 · MEDICINE

Article

Author: Karabi Ghose ; P. Turner ; Raihana S. B. Ehsanullah ; D. Witts ; Marilyn J. Kirby

Tandamine hydrochloride, a thiopyranoindole, was more active than desmethylimipramine in inhibiting the tyramine pressor response after single oral doses in human volunteers. When compared with a placebo, tandamine was found to possess significant anticholinergic activity, to reduce appetite and to produce sedation. Compared with clomipramine, it caused a smaller inhibition of 5-HT but a more marked inhibition of dopamine uptake into human platelets. Further clinical and pharmacological studies with tandamine may help to elucidate the respective roles of different monoamines in depression, sedation and appetite.

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KEGG	Wiki	ATC	Drug Bank
-	Tandamine	-	DB09192

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Indication	Highest Phase	Country/Location	Organization	Date
Depressive Disorder	Preclinical	US	Ayerst Laboratories, Inc.	05 May 1976

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