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豚鼠心房β-肾上腺素能受体的部分激动剂在豚鼠回肠中表现出松弛反应,且与β-肾上腺素能受体刺激无关。

Partial agonists at guinea-pig atrial beta-adrenoceptors display relaxation responses in the guinea-pig ileum independent of beta-adrenoceptor stimulation.

作者信息

Grassby P F, Broadley K J

出版信息

Gen Pharmacol. 1987;18(1):25-31. doi: 10.1016/0306-3623(87)90164-9.

Abstract

The beta-adrenoceptor mediated responses of oxyfedrine, ritodrine, tazolol, prenalterol, salbutamol and carteolol were examined on guinea-pig left and right atrial and ileal preparations. All agonists tested in left and right atrial preparations were partial agonists relative to isoprenaline. All agonists with the exception of salbutamol, which appeared a full agonist, produced relaxation responses significantly greater than isoprenaline in ileal preparations. The response to ritodrine in the ileum was not influenced by practolol, in a concentration which antagonized the responses of ritodrine in the right atria. The response of the ileum to beta-adrenoceptor antagonists of varying lipophyllicity was examined. Propranolol and pindolol both produced relaxation responses relative to their lipophyllicities. No relaxation was observed to atenolol, which exhibits very low lipophyllicity. It is concluded that beta-adrenoceptor agonists exhibit a substantial relaxation of guinea-pig ileum that is independent of beta-adrenoceptor stimulation.

摘要

在豚鼠的左右心房及回肠标本上,研究了奥昔非君、利托君、他唑洛尔、普瑞特罗、沙丁胺醇和卡替洛尔的β-肾上腺素受体介导反应。在左右心房标本中测试的所有激动剂相对于异丙肾上腺素均为部分激动剂。除沙丁胺醇表现为完全激动剂外,所有激动剂在回肠标本中产生的舒张反应均显著大于异丙肾上腺素。回肠中对利托君的反应不受普萘洛尔的影响,普萘洛尔的浓度可拮抗利托君在右心房中的反应。研究了不同亲脂性的β-肾上腺素受体拮抗剂对回肠的反应。普萘洛尔和吲哚洛尔均根据其亲脂性产生舒张反应。对亲脂性极低的阿替洛尔未观察到舒张反应。结论是,β-肾上腺素受体激动剂可使豚鼠回肠产生显著舒张,且该舒张与β-肾上腺素受体刺激无关。

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