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[各种β受体阻滞剂的pA2比较]

[Comparison of the pA2 of various beta blocking agents].

作者信息

Spach M O, Miesch F, Schwartz J

出版信息

Nouv Presse Med. 1975 Dec 31;4(46 Suppl):3221-2.

PMID:3766
Abstract

The drug industry is now putting out specific beta 1 or beta 2 beta-blocking agents. The pA2 of various beta-blocking agents were determined on isolated organs-guinea pig atrium and trachea: practolol and acebutolol were considered as specific beta-1 inhibitors; butoxamine was a specific beta-2 inhibitor, while pindolol, oxprenolol, propranolol and alprenolol were specificity free. The pA2 quantifies the action exerted by an inhibitor. Cardioselectivity is expressed by the pA2 left atrium/pA2 trachea ratio. It exceeds 1 000 for practolol, it equals 30 for acebutolol, and is very slight for butoxamine. The pA2 therefore gives a good idea of the potential of the various drugs on the animal's isolated organ. However, these data cannot safely be extrapolated to man. Hence the necessity of conducting clinical pharmacological studies.

摘要

制药行业目前正在推出特定的β1或β2β受体阻滞剂。在离体器官——豚鼠心房和气管上测定了各种β受体阻滞剂的pA2:醋氨心安和美托洛尔被视为特定的β1抑制剂;布托巴胺是特定的β2抑制剂,而吲哚洛尔、氧烯洛尔、普萘洛尔和阿普洛尔则无特异性。pA2量化了抑制剂所发挥的作用。心脏选择性由pA2左心房/pA2气管比值表示。醋氨心安的该比值超过1000,美托洛尔为30,布托巴胺则非常小。因此,pA2能很好地反映各种药物在动物离体器官上的潜力。然而,这些数据不能安全地外推至人体。因此有必要进行临床药理学研究。

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