尼群地平可区分大鼠大脑皮层切片中α1-肾上腺素能受体介导的第二信使反应。
Niguldipine discriminates between alpha 1-adrenoceptor-mediated second messenger responses in rat cerebral cortex slices.
作者信息
Robinson J P, Kendall D A
机构信息
Department of Physiology and Pharmacology, University of Nottingham Medical School.
出版信息
Br J Pharmacol. 1990 May;100(1):3-4. doi: 10.1111/j.1476-5381.1990.tb12041.x.
Abstract
The effect of both isomers of niguldipine, a highly selective alpha 1-adrenoceptor antagonist and dihydropyridine calcium channel blocker, on noradrenaline-stimulated inositol phosphate (IP) accumulation and adenosine 3':5'-cyclic monophosphate (cyclic AMP) potentiation was examined. Both isomers inhibited noradrenaline-stimulated IP accumulation. (+)-Niguldipine was 100 fold more potent than (-)-niguldipine. Potentiation of beta-adrenoceptor-stimulated cyclic AMP by noradrenaline was only partially inhibited by both isomers. The dihydropyridine, israpidine, did not inhibit either second messenger response. This study provides further evidence that the alpha 1-adrenoceptors mediating IP accumulation and cyclic AMP potentiation are different.
摘要
研究了尼群地平的两种异构体（一种高度选择性的α1肾上腺素能受体拮抗剂和二氢吡啶类钙通道阻滞剂）对去甲肾上腺素刺激的肌醇磷酸（IP）积累和腺苷3':5'-环磷酸（环磷酸腺苷）增强作用的影响。两种异构体均抑制去甲肾上腺素刺激的IP积累。（+）-尼群地平的效力比（-）-尼群地平强100倍。两种异构体仅部分抑制去甲肾上腺素对β肾上腺素能受体刺激的环磷酸腺苷的增强作用。二氢吡啶类药物伊拉地平对两种第二信使反应均无抑制作用。该研究进一步证明，介导IP积累和环磷酸腺苷增强作用的α1肾上腺素能受体是不同的。
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9
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