The influence of some aminoalkanolic xanthone derivatives on central nervous and cardiovascular systems in rodents.

Bollettino chimico farmaceutico Pub Date : 2004-09-01
Tadeusz Librowski, Ryszard Czarnecki, Magdalena Jastrzebska-Wiesek, Wlodzimierz Opoka, Henryk Marona
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Abstract

A series of appropriate aminoalkanolic derivatives 2- or 4-methylxanthone was synthesized and evaluated for anticonvulsant activity in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole seizure threshold (scPtz) assays, and for neurotoxicity (TOX). The most interesting result was the anticonvulsant activity of (R,S)-2N-(6-chloro-2-xanthonemethyl-2N-methylamino-1-propanol hydrochloride (II, which displayed anti-MES and anti-scPtz activity. Some of the obtained compounds (I - IV and V - VII) were also tested for their effect on the circulatory system (the effect on normal electrocardiogram, protection against adrenaline-, barium-, calcium- and/or strophanthine-induced arrhythmias, the effect on the arterial blood pressure and respiratory movements) and acute toxicity.

某些氨基醇类山酮衍生物对啮齿动物中枢神经和心血管系统的影响。
合成了一系列合适的氨基烷醇衍生物2-或4-甲基山酮,并在最大电击发作(MES)和皮下戊四唑发作阈值(scPtz)试验中评估其抗惊厥活性,以及神经毒性(TOX)。最有趣的结果是(R,S)- 2n -(6-氯-2-黄嘌呤甲基- 2n -甲氨基-1-丙醇盐化物(II)的抗惊厥活性,具有抗mes和抗scptz活性。所获得的一些化合物(I - IV和V - VII)也测试了它们对循环系统的影响(对正常心电图的影响,对肾上腺素、钡、钙和/或斯特芬碱引起的心律失常的保护,对动脉血压和呼吸运动的影响)和急性毒性。
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