Trazium esilate (EGYT-3615) is structurally an as-triazino isoquinolinium salt which showed considerable activity in pharmacological tests characteristic for antidepressants (antagonism of tetrabenazine, potentiation of yohimbine, behavioral despair). The compound exhibited minimal sedative effect. Some findings suggest that it influences the central dopaminergic system. The drug potentiated actions of amphetamine such as stereotypy and hypermotility. It differentially blocked the hypothermic and the stereotypy inducing action of apomorphine. Trazium esilate also inhibited the cataleptic state provoked by bulbocapnine in mice. In higher dose it decreased the plasma prolactin level in rats. The compound potentiated the effect of norepinephrine on isolated vas deferens of the rat. Trazium esilate is a weak displacer on a1-, a2- and D2-receptors, however, it induced a2-receptor desenzitization after repeated treatment. It had no influence on rat brain cortical noradrenaline and striatal dopamine release evoked by high K+ concentration, but it increased the spontaneous dopamine outflow in rat striatum. The compound also elevated the striatal dopamine and DOPAC levels both after acute and chronic treatment.

01 Jan 1989·Acta pharmaceutica Hungarica

[Pharmacokinetic and metabolic study of EGYT-3615 in rats].

Article

Author: Fekete, M ; Magyar, K ; Tamás, J ; Lengyel, J

Polish journal of pharmacology and pharmacy

Studies on serum binding of some drugs.

Article

Author: Magyar, K ; Kalász, H ; Kerecsen, L ; Szökö, E

Binding of three potential antidepressive compounds, EGYT-3615, EGYT-475 (trelibet) and EGYT-2760 to human serum was investigated by equilibrium dialysis method using radiolabelled drugs. All three compounds bound to serum proteins and the binding was sensitive to pH and salt concentration. The binding of trelibet and EGYT-3615 was not saturable at a wide range of drug concentration. The results show that EGYT-3615 has both specific and non-specific, while trelibet has only non-specific binding sites on serum proteins.

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Indication	Highest Phase	Country/Location	Organization	Date
Depressive Disorder, Major	Phase 2	HU	Egis SA	-
Depressive Disorder, Major	Phase 1	-	Egis Gyógyszergyár Zrt.	-

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