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普萘洛尔和α-甲基普萘洛尔(ICI 77602)对麻醉犬血管及心脏对异丙肾上腺素反应的拮抗作用。

The antagonism by propranolol and alpha-methylpropranolol (ICI 77602) of vascular and cardiac responses to isoprenaline in anaesthetized dogs.

作者信息

Fitzgerald J D, O'Donnell S R

出版信息

Clin Exp Pharmacol Physiol. 1978 Nov-Dec;5(6):579-86. doi: 10.1111/j.1440-1681.1978.tb00713.x.

Abstract
  1. In anaesthetized dogs, alpha-methylpropranolol was less potent than propranolol in antagonizing both vascular (hind limb perfusion pressure) and cardiac heart rate) responses to isoprenaline. 2. alpha-Methylpropranolol was more potent in antagonizing vascular than cardiac responses to isoprenaline, but this selectivity was no greater than that seen also with propranolol. 3. Isoprenaline sensitivity was greater in the hind limb than the heart and vascular-selective antagonism was more pronounced in those dogs in which this differential sensitivity was the greatest. 4. Introduction of an alpha-methyl group into propranolol decreases its beta-adrenoceptor antagonist potency but does not enhance vascular selectivity.
摘要
  1. 在麻醉犬中,α-甲基普萘洛尔在拮抗异丙肾上腺素引起的血管(后肢灌注压)和心脏(心率)反应方面,其效力低于普萘洛尔。2. α-甲基普萘洛尔在拮抗异丙肾上腺素引起的血管反应方面比心脏反应更有效,但这种选择性并不比普萘洛尔更高。3. 后肢对异丙肾上腺素的敏感性高于心脏,在这种差异敏感性最大的犬中,血管选择性拮抗作用更为明显。4. 在普萘洛尔中引入α-甲基会降低其β-肾上腺素能受体拮抗剂的效力,但不会增强血管选择性。

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