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N-[(2,6-Dimethylphenoxy)alkyl]aminoalkanols-their physicochemical and anticonvulsant properties.N-[(2,6-二甲基苯氧基)烷基]氨基链烷醇——它们的物理化学性质和抗惊厥特性
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α-Spinasterol, a TRPV1 receptor antagonist, elevates the seizure threshold in three acute seizure tests in mice.α-菠菜甾醇是一种瞬时受体电位香草酸亚型1（TRPV1）受体拮抗剂，在小鼠的三项急性癫痫发作试验中提高了癫痫发作阈值。
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新型-[(苯氧基)烷基]-和-[(苯氧基)乙氧基乙基]氨基烷醇的设计、合成及抗惊厥-镇痛活性

Design, synthesis and anticonvulsant-analgesic activity of new -[(phenoxy)alkyl]- and -[(phenoxy)ethoxyethyl]aminoalkanols.

作者信息

Rapacz Anna, Waszkielewicz Anna M, Pańczyk Katarzyna, Pytka Karolina, Koczurkiewicz Paulina, Piska Kamil, Pękala Elżbieta, Budziszewska Bogusława, Starek-Świechowicz Beata, Marona Henryk

机构信息

Department of Pharmacodynamics , Faculty of Pharmacy , Jagiellonian University Medical College , Medyczna 9 Str., 30-688 Krakow , Poland.

Department of Bioorganic Chemistry , Faculty of Pharmacy , Jagiellonian University Medical College , Medyczna 9 Str. , 30-688 Krakow , Poland . Email:

出版信息

Medchemcomm. 2016 Nov 11;8(1):220-238. doi: 10.1039/c6md00537c. eCollection 2017 Jan 1.

DOI:10.1039/c6md00537c
PMID:30108708
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6072507/
Abstract

New derivatives of -[(phenoxy)alkyl]- and -[(phenoxy)ethoxyethyl]aminoalkanols have been synthesized and evaluated for their anticonvulsant activity in maximal electroshock (MES), maximal electroshock seizure threshold (MEST), and pentylenetetrazol (PTZ) tests. Their neurotoxicity was evaluated rotarod and chimney tests. The compounds exhibiting the most beneficial activity and protection indices were evaluated for analgesic activity using the formalin test for neurogenic pain. They were also evaluated for their influence on cytotoxic activity using cellular models (HepG2 and CRL-2534 cell lines). Experiments performed using MTT and neutral red cytotoxicity assays showed that all evaluated compounds were safe for normal, glial cells (astrocytes) and did not induce hepatotoxic effects. Based on the results from the studies, the safety of the evaluated compounds was inferred. The most promising compound in this research was 1-{2-[2-(2,3-dimethylphenoxy)ethoxy]ethyl}piperidin-3-ol hydrochloride. Additionally, metabolism prediction for the compound has been performed.

摘要

已合成了-[(苯氧基)烷基]-和-[(苯氧基)乙氧基乙基]氨基链烷醇的新型衍生物，并在最大电休克（MES）、最大电休克惊厥阈值（MEST）和戊四氮（PTZ）试验中评估了它们的抗惊厥活性。在旋转棒和烟囱试验中评估了它们的神经毒性。使用神经性疼痛的福尔马林试验，对表现出最有益活性和保护指数的化合物进行了镇痛活性评估。还使用细胞模型（HepG2和CRL-2534细胞系）评估了它们对细胞毒性活性的影响。使用MTT和中性红细胞毒性测定法进行的实验表明，所有评估的化合物对正常神经胶质细胞（星形胶质细胞）都是安全的，并且不会诱导肝毒性作用。基于这些研究结果，推断出评估化合物的安全性。本研究中最有前景的化合物是1-{2-[2-(2,3-二甲基苯氧基)乙氧基]乙基}哌啶-3-醇盐酸盐。此外，还对该化合物进行了代谢预测。