Szücks Z, Szentendrei T, Fekete M I
EGIS Pharmaceuticals, Biochemical Department, Budapest, Hungary.
Pol J Pharmacol Pharm. 1987 Mar-Apr;39(2):185-93.
The effect of a new antidepressant drug: EGYT-475 (Trelibet) and its metabolites: EGYT-1354 and EGYT-2760 on the K+-stimulated overflow of 3H-noradrenaline from rat brain cortical slices was studied. The parent compound and EGYT-1354 were ineffective at a concentration of 10(-4) mole/l but EGYT-2760 increased both the spontaneous and the potassium-evoked tritium release in the concentration range of 10(-8)-10(-5) mole/l. The increasing effect of EGYT-2760 on the basal tritium outflow was similar to that of D-amphetamine: it could be prevented by neuronal uptake inhibitors (cocaine and desipramine) and did not depend on the extracellular Ca++ concentration. EGYT-2760 and D-amphetamine enhanced the K+-induced 3H-noradrenaline overflow too, however this effect of D-amphetamine was abolished in the presence of cocaine and desipramine, while the effect of EGYT-2760 remained unaffected. EGYT-2760 did not possess presynaptic alpha 2-adrenoceptor antagonist property: it could not antagonize the inhibitory effect of clonidine.
研究了一种新型抗抑郁药物EGYT - 475（曲利贝特）及其代谢产物EGYT - 1354和EGYT - 2760对大鼠脑皮质切片中钾离子刺激的3H - 去甲肾上腺素释放的影响。母体化合物和EGYT - 1354在浓度为10^(-4)摩尔/升时无效，但EGYT - 2760在10^(-8) - 10^(-5)摩尔/升的浓度范围内增加了自发和钾诱发的氚释放。EGYT - 2760对基础氚流出的增加作用与D - 苯丙胺相似：它可被神经元摄取抑制剂（可卡因和地昔帕明）阻止，且不依赖于细胞外钙离子浓度。EGYT - 2760和D - 苯丙胺也增强了钾离子诱导的3H - 去甲肾上腺素释放，然而D - 苯丙胺的这种作用在可卡因和地昔帕明存在时被消除，而EGYT - 2760的作用不受影响。EGYT - 2760不具有突触前α2 - 肾上腺素能受体拮抗剂特性：它不能拮抗可乐定的抑制作用。
