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α1-肾上腺素能刺激棕色脂肪细胞的磷脂酰肌醇代谢和呼吸作用。

Alpha 1-adrenergic stimulation of phosphatidylinositol turnover and respiration of brown fat cells.

作者信息

Mohell N, Wallace M, Fain J N

出版信息

Mol Pharmacol. 1984 Jan;25(1):64-9.

PMID:6708936
Abstract

The alpha-adrenergic agonist phenylephrine (in the presence of the beta-adrenergic antagonist alprenolol) stimulated respiration and incorporation of [3H]glycerol and [32P] Pi into phosphatidylinositol of hamster brown fat cells in a concentration-dependent manner. Both responses were preferentially inhibited by prazosin as compared with yohimbine, indicating alpha 1 specificity. Uniquely, prazosin inhibition of phenylephrine-stimulated phosphatidylinositol metabolism had two components, since 30% of the response was inhibited by less than 1 nM prazosin, 10 nM gave no further inhibition, and 100 nM prazosin completely inhibited the response. The phosphatidylinositol response was still present in Ca2+-free buffer, although reduced in magnitude. The concentration relationships of the effects of agonists and antagonists were compared with those of previous results of [3H]prazosin binding and with phenylephrine potency to compete for binding. On the basis of these comparisons, it is suggested that the highly prazosin-sensitive part of the phosphatidylinositol response may be closely associated with receptor occupation.

摘要

α-肾上腺素能激动剂去氧肾上腺素(在β-肾上腺素能拮抗剂阿普洛尔存在的情况下)以浓度依赖的方式刺激仓鼠棕色脂肪细胞的呼吸以及[³H]甘油和[³²P]无机磷酸盐掺入磷脂酰肌醇。与育亨宾相比,这两种反应均优先受到哌唑嗪的抑制,表明具有α₁特异性。独特的是,哌唑嗪对去氧肾上腺素刺激的磷脂酰肌醇代谢的抑制有两个成分,因为小于1 nM的哌唑嗪可抑制30%的反应,10 nM时不再有进一步抑制,而100 nM的哌唑嗪可完全抑制该反应。尽管幅度减小,但在无钙缓冲液中仍存在磷脂酰肌醇反应。将激动剂和拮抗剂作用的浓度关系与先前[³H]哌唑嗪结合的结果以及去氧肾上腺素竞争结合的效力进行了比较。基于这些比较,提示磷脂酰肌醇反应中对哌唑嗪高度敏感的部分可能与受体占据密切相关。

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