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可乐定诱导鸡睡眠过程中涉及的中枢α-肾上腺素能受体的立体选择性

Stereoselectivity of central alpha-adrenoceptors involved in sleep induced by clonidine in chickens.

作者信息

Dabiré H, Mouillé P, Joly G, Schmitt H

出版信息

Neuropharmacology. 1985 Aug;24(8):709-12. doi: 10.1016/0028-3908(85)90003-6.

Abstract

The stereoselectivity of central alpha 2-adrenoceptors involved in sleep induced in chicks by clonidine, suggested by the results observed with the stereoisomers of idazoxan, was further investigated with the stereoisomers of (imidazolinyl-2)-2-dihydro-2,3-benzofurane (S9871) and those of (imidazolinyl-2)-2-benzocyclobutane (S10089). As for the stereoisomers of idazoxan, there was not a good separation between the effects of the stereoisomers of S10089. In contrast, there was a clearcut separation between the effects of (+)S9871 (antagonist) and (-)S9871 (no effect against the action of clonidine). Therefore, these results strongly support the view that central alpha 2-adrenoceptors which mediate sedation are stereoselective for alpha 2-antagonists.

摘要

通过咪唑克生的立体异构体观察到的结果表明,可乐定诱导雏鸡睡眠所涉及的中枢α2 - 肾上腺素能受体的立体选择性,用(咪唑啉基 - 2)-2 - 二氢 - 2,3 - 苯并呋喃(S9871)的立体异构体和(咪唑啉基 - 2)-2 - 苯并环丁烷(S10089)的立体异构体作了进一步研究。至于咪唑克生的立体异构体,S10089的立体异构体的效应之间没有很好的区分。相比之下,(+)S9871(拮抗剂)和( - )S9871(对可乐定的作用无影响)的效应之间有明显的区分。因此,这些结果有力地支持了这样一种观点,即介导镇静作用的中枢α2 - 肾上腺素能受体对α2 - 拮抗剂具有立体选择性。

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