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两种磷酸二酯酶抑制剂(罂粟碱和茶碱)对兔心房变时性反应中H1和H2受体激动剂刺激增强作用的比较。

A comparison of the augmentation of H1 and H2 receptor agonist stimulation of rabbit atrial chronotropic response by two phosphodiesterase inhibitors, papaverine and theophylline.

作者信息

Hughes M J

出版信息

Res Commun Chem Pathol Pharmacol. 1978 Aug;21(2):251-70.

PMID:694224
Abstract

Papaverine and theophylline both increase the chronotropic response of isolated rabbit atria, however, the maximum stimulation following papaverine is much smaller than that obtained with theophylline. When these phosphodiesterase inhibitors are used in conjunction with histamine (H1 and H2 receptor agonist), 2-(2-aminoethyl) pyrazole (H2 agonist) and 3-(2-aminoethyl) triazole (H1 agonist) the responses are all considerably more than additive. This suggests that both H1 and H2 histamine receptors can activate adenyl cyclase and therefore increase the formation of cyclic AMP in spite of reports that only H2 receptors stimulate adenyl cyclase.

摘要

罂粟碱和茶碱均可增强离体兔心房的变时反应,然而,罂粟碱引起的最大刺激远小于茶碱。当这些磷酸二酯酶抑制剂与组胺(H1和H2受体激动剂)、2-(2-氨基乙基)吡唑(H2激动剂)和3-(2-氨基乙基)三唑(H1激动剂)联合使用时,反应均显著大于相加效应。这表明,尽管有报道称只有H2受体可刺激腺苷酸环化酶,但H1和H2组胺受体均可激活腺苷酸环化酶,从而增加环磷酸腺苷的生成。

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