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尼卡地平与异丙肾上腺素在人和豚鼠离体气道中的相互作用。

The nicardipine-isoprenaline interaction in human and guinea-pig isolated airways.

作者信息

Sarriá B, Zhang Y, Naline E, Brisac A M, Laurent S, Cortijo J, Advenier C

机构信息

Faculté de Médecine Paris-Ouest, Laboratoire de Pharmacologie, Paris, France.

出版信息

Fundam Clin Pharmacol. 1994;8(1):26-33. doi: 10.1111/j.1472-8206.1994.tb00776.x.

Abstract

The effects of the dihydropyridine calcium antagonist nicardipine on the concentration-response curves of relaxant compounds acting through the adenylate-cyclase/cAMP system (isoprenaline, forskolin, adenosine and theophylline) or by the cGMP pathway (sodium nitroprusside) were studied on human isolated bronchus and guinea-pig isolated trachea. These effects were compared with those of nifedipine (a dihydropyridine derivative) and theophylline (a non-selective phosphodiesterase inhibitor). Nicardipine, in the range of 0.01 to 1 microM, significantly potentiated the relaxant effects of isoprenaline, forskolin, adenosine and theophylline, whereas the effects of sodium nitroprusside were significantly potentiated at 10 microM only. These results suggest that nicardipine behaves as an inhibitor of phosphodiesterases III and IV. One such effect may be involved in the potentiation of the isoprenaline relaxation of human and guinea-pig isolated airways.

摘要

在人离体支气管和豚鼠离体气管上,研究了二氢吡啶类钙拮抗剂尼卡地平对通过腺苷酸环化酶/cAMP系统起作用的舒张化合物(异丙肾上腺素、福斯可林、腺苷和茶碱)或通过cGMP途径起作用的舒张化合物(硝普钠)浓度-效应曲线的影响。将这些影响与硝苯地平(一种二氢吡啶衍生物)和茶碱(一种非选择性磷酸二酯酶抑制剂)的影响进行了比较。在0.01至1微摩尔范围内,尼卡地平显著增强了异丙肾上腺素、福斯可林、腺苷和茶碱的舒张作用,而硝普钠的作用仅在10微摩尔时显著增强。这些结果表明,尼卡地平表现为磷酸二酯酶III和IV的抑制剂。这种效应之一可能参与了异丙肾上腺素对人和豚鼠离体气道舒张作用的增强。

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