On the importance of volatile agents devoid of anesthetic action.
On the importance of volatile agents devoid of anesthetic action.
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关于没有麻醉作用的挥发性药物的重要性。
DOI：
10.1213/00000539-199412000-00001
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发表时间：
1994
影响因子：
5.7
通讯作者：
K. Miller
中科院分区：
文献类型：
--
作者：
D. Raines;K. Miller
在这个问题上，加州大学的研究人员报告说，根据迈耶-奥弗顿脂类溶解度规则预测的某些挥发性和气态Comi化合物实际上根本没有麻醉作用(1)。在这篇社论中，我们将把这一发现放在对非麻醉剂的脂溶化合物的更传统研究的背景下，并讨论非麻醉剂在确定麻醉作用的相关部位方面可能发挥的作用。在许多类似的麻醉药系列中，高级成员缺乏麻醉活性，即使它们是高度脂溶的(2-4)。低同系物的麻醉效力随着连续亚甲基的加入而对数增加到某一点。超过这一点，亚甲基的添加会导致麻醉剂活性的完全丧失，即使在可达到的最高浓度下也是如此。这种行为被称为“麻醉剂切断”。(请参见第1032页的侧栏。)更广泛地说，截止值可以定义为同源序列中较高成员的活性缺失。正醇是研究得最好的同系物麻醉剂。在这个系列中，可以观察到十二醇和十三醇之间的麻醉剂截止点；从甲醇到十二醇的麻醉剂效力增加；然而，十三醇和更高的同系物完全没有麻醉活性[2]。截止点的发生，以及接近截止点的方式，都为未知作用部位的分子药理学和作用机制提供了线索。然而，在考虑这些信息的用处之前，有必要面对某些实验困难。截止的定义，要有任何有用的含义，必须意味着系统处于平衡状态。例如，如果一种化合物的吸收和分配到
n this issue, researchers at the University of California report that certain volatile and gaseous comI pounds predicted by the Meyer-Overton lipid solubility rule to be general anesthetics actually have no anesthetic action at all (1). In this editorial, we will place this finding in the context of more traditional studies of lipid-soluble compounds that are not anesthetics and discuss the role that nonanesthetic agents may play in defining relevant sites of anesthetic action. In many homologous series of anesthetics, higher members lack anesthetic activity even though they are highly lipid soluble (2-4). The anesthetic potency of lower homologues increases logarithmically with the addition of successive methylene groups up to a point. Beyond that point, the addition of methylene groups leads to a complete loss of anesthetic activity even at the highest attainable concentrations. This behavior has been termed ”anesthetic cutoff.” (See the sidebar on page 1032.) More broadly, cutoff can be defined as the absence of activity of higher members of a homologous series. The normal alcohols comprise the best studied homologous series of anesthetics. In this series, anesthetic cutoff is observed between dodecanol and tridecanol; anesthetic potency increases from methanol through dodecanol; however, tridecanol and higher homologues are completely devoid of anesthetic activity (2). The point at which cutoff occurs and, indeed, the way in which cutoff is approached provide clues about both the molecular pharmacology of the unknown site of action and the mechanism of action. However, before considering how useful this information can be, it is necessary to confront certain experimental difficulties. The definition of cutoff, to have any useful meaning, must imply that the system is at equilibrium. For example, if a compound’s uptake and distribution to
不符合迈耶-奥弗顿假说的多卤代和全氟化合物。
影响因子：
5.7
作者：
Koblin,DD;Chortkoff,BS;Laster,MJ;Eger2nd,EI;Halsey,MJ;Ionescu,P
通讯作者：
Ionescu,P