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1-(2-嘧啶基)-哌嗪(一种伊沙匹隆代谢物)的中枢作用。

The central action of 1-(2-pyrimidinyl)-piperazine, an ipsapirone metabolite.

作者信息

Tatarczyńska E, Pawłowski L, Chojnacka-Wójcik E, Maj J

机构信息

Institute of Pharmacology, Polish Academy of Sciences, Kraków.

出版信息

Pol J Pharmacol Pharm. 1989 Jan-Feb;41(1):51-61.

PMID:2587437
Abstract

The central action of 1-(2-pyrimidinyl)-piperazine (1-PP), a metabolite of ipsapirone, was studied in mice and rats. 1-PP decreased the locomotor activity and slightly increased the body temperature at an ambient temperature of 21 degrees C, not changing it at an ambient temperature of 28 degrees C. The examined substance antagonized clonidine effects (hypothermia, locomotor hypoactivity, stimulation of the hind limb flexor reflex of the spinal rat). Stimulation of the flexor reflex by St 587, an alpha 1-adrenoceptor agonist was not blocked by 1-PP. 1-PP-induced stimulation of the flexor reflex was blocked by cyproheptadine, ketanserin and pirenperone, but not by prazosin or yohimbine. Given in high doses, 1-PP evoked a flat body posture syndrome, but not forepaw treading or head twitches. The obtained results indicate that 1-PP has mainly an alpha 2-adrenolytic action and differs from ipsapirone in its profile.

摘要

对伊沙匹隆的代谢产物1-(2-嘧啶基)-哌嗪(1-PP)的中枢作用在小鼠和大鼠中进行了研究。在21摄氏度的环境温度下,1-PP降低了运动活性并略微升高了体温,而在28摄氏度的环境温度下则无此变化。所研究的物质拮抗可乐定的作用(体温过低、运动活动减弱、刺激脊髓大鼠后肢屈肌反射)。α1-肾上腺素能受体激动剂St 587对屈肌反射的刺激未被1-PP阻断。1-PP诱导的屈肌反射刺激被赛庚啶、酮色林和哌仑西平阻断,但未被哌唑嗪或育亨宾阻断。高剂量给药时,1-PP引发了平卧式体位综合征,但未引发前爪踏地或头部抽搐。所得结果表明,1-PP主要具有α2-肾上腺素能阻断作用,其作用特征与伊沙匹隆不同。

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