PA, A NEW SCALE FOR THE MEASUREMENT OF DRUG ANTAGONISM
PA, A NEW SCALE FOR THE MEASUREMENT OF DRUG ANTAGONISM
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DOI：
10.1111/j.1476-5381.1947.tb00336.x
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发表时间：
1947-01-01
期刊：
影响因子：
--
通讯作者：
SCHILD, HO
中科院分区：
文献类型：
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作者：
SCHILD, HO
作者解释了他的量表，建议将其作为表达药物拮抗作用的一种可能的常用方法，并详细介绍了他的自动操作器官浴组件以及他在离体豚鼠回肠上使用药物拮抗剂的常规方法。 p Ax 定义为摩尔浓度以 10 为底的负对数。拮抗剂药物的作用将多剂量（x）的兴奋剂药物的作用降低到单剂量的作用，例如，p A2 哌替啶-组胺 = 5.8 意味着浴液中哌替啶 10-5.8 摩尔将一剂组胺（例如 2 Y）的作用降低到该剂量的组胺（此处为 1y）在拮抗剂不存在时所产生的效果的一半。结果表明，pA 值取决于拮抗剂药物与组织之间的接触长度，但与绝对浓度无关。所使用的兴奋剂药物。 For a given tissue, antagonist, and active drug, the value of pA must be the mean of a random sample of detns. on different individuals, but an antagonist cannot be fully characterized by a single pA value, short of giving the complete time-action and concn.-action relations of the system.作者展示了 2 分钟和 14 分钟后的 4 个 pA 值 pA10 和 PA2 分别提供了多少此类信息。给出了新安特根、苯海拉明、哌替啶和阿托品对抗组胺和乙酰胆碱的特征图。
The author explains his scale, suggests it as a possible common method of expressing drug antagonism, and gives details of his automatically operated organ bath assembly and his routine with drug antagonists on the isolated guinea-pig ileum. p Ax is defined as the negative log to base 10 of the molar concn. of an antagonist drug which will reduce the effect of a multiple dose (x) of a stimulant drug to that of a single dose, e.g., p A2 pethidine-histamine = 5.8 means that pethidine 10-5.8 molar in the bath fluid reduces the effect of a dose of histamine (say 2 Y) to that which half this dose of histamine (here 1y) produces when the antagonist is not present. It is shown that pA values depend on the length of contact between antagonist drug and tissue but are independent of the absolute concn. of the stimulant drug used. For a given tissue, antagonist, and active drug, the value of pA must be the mean of a random sample of detns. on different individuals, but an antagonist cannot be fully characterized by a single pA value, short of giving the complete time-action and concn.-action relations of the system. The author shows how much of such information is supplied by the 4 pA values pA10 and PA2 each after 2 and 14 mins. Figures are given characterizing neo-antergan, benadryl, pethidine, and atropine against histamine and acetylcholine.