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对二甲氨基苯甲醛的β-肾上腺素能受体刺激特性

Beta-adrenoceptor stimulating properties of para-dimethylaminobenzaldehyde.

作者信息

Ghouri M S, Shibata S

出版信息

Br J Pharmacol. 1970 Jun;39(2):447-54. doi: 10.1111/j.1476-5381.1970.tb12907.x.

Abstract
  1. Studies on the various isolated tissues indicate that para-dimethylaminobenzaldehyde (DMAB) is a beta-adrenoceptor stimulant. DMAB is antagonized by the beta-adrenoceptor blocking agent, MJ 1999, but not by the alpha-adrenoceptor blocking agent, phentolamine.2. A study of dose-response relationships suggests a competitive interaction between MJ 1999 and DMAB.3. DMAB was about 122 times less potent than isoprenaline on the isolated guinea-pig tracheal preparation. The effects of DMAB on isolated rabbit atria were not only very weak, but were also very brief. On this tissue, DMAB was respectively 72,000 and 55,400 times less active than isoprenaline in producing positive chronotropic and inotropic effects. DMAB caused the relaxation of the guinea-pig taenia coli and the rabbit ileum. These actions were very weak in comparison with those of isoprenaline.4. These results suggest that a compound (DMAB) structurally different from isoprenaline may mimic isoprenaline responses by stimulating beta-adrenoceptors through different mechanisms.
摘要
  1. 对各种离体组织的研究表明,对二甲氨基苯甲醛(DMAB)是一种β-肾上腺素能受体兴奋剂。DMAB可被β-肾上腺素能受体阻断剂MJ 1999拮抗,但不能被α-肾上腺素能受体阻断剂酚妥拉明拮抗。

  2. 一项剂量反应关系研究表明,MJ 1999与DMAB之间存在竞争性相互作用。

  3. 在离体豚鼠气管制备物上,DMAB的效力约为异丙肾上腺素的122分之一。DMAB对离体兔心房的作用不仅非常微弱,而且非常短暂。在该组织上,DMAB在产生正性变时和变力作用方面的活性分别比异丙肾上腺素低72,000倍和55,400倍。DMAB可使豚鼠结肠带和兔回肠松弛。与异丙肾上腺素相比,这些作用非常微弱。

  4. 这些结果表明,一种结构不同于异丙肾上腺素的化合物(DMAB)可能通过不同机制刺激β-肾上腺素能受体来模拟异丙肾上腺素的反应。

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