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一系列可乐定样药物中α2-肾上腺素能受体选择性与抗惊厥作用之间的关系。

The relationship between alpha 2-adrenoceptor selectivity and anticonvulsant effect in a series of clonidine-like drugs.

作者信息

Papanicolaou J, Summers R J, Vajda F J, Louis W J

出版信息

Brain Res. 1982 Jun 10;241(2):393-7. doi: 10.1016/0006-8993(82)91086-1.

Abstract

Clonidine and the 4 clonidine-like drugs: 44-549, lofexidine, guanfacine, and CP-14,304-18, had anticonvulsant activity against pentylenetetrazole-induced convulsions in rats. The magnitude and dose range over which anticonvulsant effects were observed was related to the selectivity of the compounds for alpha 2 and alpha 1 adrenoceptors. Selective alpha 2 adrenoceptor agonists may form a new group of anticonvulsants.

摘要

可乐定及4种可乐定样药物:44-549、洛非西定、胍法辛和CP-14,304-18,对大鼠戊四氮诱导的惊厥具有抗惊厥活性。观察到抗惊厥作用的强度和剂量范围与化合物对α2和α1肾上腺素能受体的选择性有关。选择性α2肾上腺素能受体激动剂可能构成一类新的抗惊厥药物。

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