• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

基于计算机的pA2值估计及相关分析的进展。

Developments of computer-based estimation of pA2 values and associated analysis.

作者信息

Stone M, Angus J A

出版信息

J Pharmacol Exp Ther. 1978 Dec;207(3):705-18.

PMID:731426
Abstract

The standard statistical-computing package GLIM is used to analyze data from agonist-antagonist studies for the estimation of the dissociation constant of the antagonist. The method follows the general approach of D.R. Waud (Analysis of dose-response curves. In Methods in Pharmacology, vol. 3, Smooth Muscle, ed. by E.E. Daniel and M. Paton, Plenum Press, New York, 1975) in employing an iterative nonlinear least-squares curve-fitting procedure. However, it differs in two important respects: 1) it is interactive; and 2) it allows linear adjustments for covariates and experimental design variables. This paper develops develops an alternative useful formulation of departure from simple competitivity and also a graphical display called a "Clark plot" showing how the spacings of the dose-response lines fit the theory of simple competitive antagonism. This plot provides an alternative to the popular Schild plot for which, of necessity, the zero antagonist (control) dose-response line is heavily used both in the experimental design and in the analysis associated with it.

摘要

标准统计计算软件包GLIM用于分析激动剂-拮抗剂研究的数据,以估算拮抗剂的解离常数。该方法遵循D.R. 沃德(《剂量反应曲线分析》。载于《药理学方法》第3卷,平滑肌,E.E. 丹尼尔和M. 佩顿编,普伦蒂斯出版社,纽约,1975年)的一般方法,采用迭代非线性最小二乘曲线拟合程序。然而,它在两个重要方面有所不同:1)它是交互式的;2)它允许对协变量和实验设计变量进行线性调整。本文提出了一种偏离简单竞争性的有用替代公式,以及一种名为“克拉克图”的图形显示,展示了剂量反应线的间距如何符合简单竞争性拮抗理论。该图为常用的希尔德图提供了一种替代方案,对于希尔德图,在实验设计及其相关分析中都必然大量使用零拮抗剂(对照)剂量反应线。

相似文献

1
Developments of computer-based estimation of pA2 values and associated analysis.基于计算机的pA2值估计及相关分析的进展。
J Pharmacol Exp Ther. 1978 Dec;207(3):705-18.
2
Antagonist inhibition curves and the measurement of dissociation constants.拮抗剂抑制曲线和解离常数的测定。
Br J Pharmacol. 1997 Jan;120(1):13-8. doi: 10.1038/sj.bjp.0700865.
3
The Clark plot: a semi-historical case study.克拉克图:一个半历史性的案例研究。
J Pharm Pharmacol. 1980 Feb;32(2):81-6. doi: 10.1111/j.2042-7158.1980.tb12857.x.
4
Construction of antagonist dose-response curves for estimation of pA2-values by Schild-plot analysis and detection of allosteric interactions.构建拮抗剂剂量反应曲线,用于通过Schild图分析估计pA2值并检测变构相互作用。
Br J Pharmacol. 1992 Jul;106(3):710-6. doi: 10.1111/j.1476-5381.1992.tb14399.x.
5
Naloxazone treatment in the guinea pig ileum in vitro reveals second functional opioid receptor site.纳洛沙宗对豚鼠离体回肠的治疗揭示了第二个功能性阿片受体位点。
J Pharmacol Exp Ther. 1987 Jan;240(1):138-44.
6
The use of drug-receptor affinity measures in the differentiation of receptors.药物-受体亲和力测定在受体鉴别中的应用。
Fed Proc. 1982 May;41(7):2323-7.
7
On the use of a dynamic approach to the estimation of dissociation constants for reversible competitive antagonists.关于使用动态方法估计可逆竞争性拮抗剂的解离常数
J Pharmacol Exp Ther. 1981 Feb;216(2):352-6.
8
The design of pharmacological experiments using unbiased models of agonist-antagonist interaction.使用激动剂-拮抗剂相互作用的无偏模型进行药理实验的设计。
J Pharmacol Exp Ther. 1978 Jun;205(3):617-23.
9
Tissue response as a functional discriminator of receptor heterogeneity: effects of mixed receptor populations on Schild regressions.作为受体异质性功能判别指标的组织反应:混合受体群体对希尔德回归的影响
Mol Pharmacol. 1992 Apr;41(4):699-707.
10
A new method for estimation of agonist dissociation constants (KA): directly fitting the postinactivation concentration-response curve to a nested hyperbolic equation.一种估计激动剂解离常数(KA)的新方法:将失活后浓度-反应曲线直接拟合为嵌套双曲线方程。
J Pharmacol Exp Ther. 1989 Apr;249(1):61-9.

引用本文的文献

1
Distortion of K estimates of endothelin-1 ET and ET receptor antagonists in pulmonary arteries: Possible role of an endothelin-1 clearance mechanism.肺动脉中内皮素-1(ET)和 ET 受体拮抗剂 K 估计值的扭曲:可能是内皮素-1 清除机制的作用。
Pharmacol Res Perspect. 2017 Dec;5(6). doi: 10.1002/prp2.374.
2
Pharmacological analysis of cannabinoid receptor activity in the rat vas deferens.大鼠输精管中大麻素受体活性的药理学分析。
Br J Pharmacol. 2001 Mar;132(6):1281-91. doi: 10.1038/sj.bjp.0703930.
3
Pharmacological studies on prostanoid receptors in the rabbit isolated saphenous vein: a comparison with the rabbit isolated ear artery.
兔离体隐静脉中前列腺素受体的药理学研究:与兔离体耳动脉的比较。
Br J Pharmacol. 1996 Jan;117(1):13-20. doi: 10.1111/j.1476-5381.1996.tb15148.x.
4
Extended concentration-response curves used to reflect full agonist efficacies and receptor occupancy-response coupling ranges.用于反映完全激动剂效力和受体占有率-反应偶联范围的延长浓度-反应曲线。
Br J Pharmacol. 1995 Jul;115(5):745-52. doi: 10.1111/j.1476-5381.1995.tb14996.x.
5
Vascular studies with histamine in vitro.组胺的体外血管研究。
Agents Actions. 1981 Apr;11(1-2):116-8. doi: 10.1007/BF01991477.
6
Seasonal variation in responses of the toad renal vasculature to adrenaline.蟾蜍肾血管系统对肾上腺素反应的季节性变化。
Naunyn Schmiedebergs Arch Pharmacol. 1982 Sep;320(3):246-54. doi: 10.1007/BF00510136.
7
Resistance of adrenergic neurotransmission in the toad heart to adrenoceptor blockade.蟾蜍心脏中肾上腺素能神经传递对肾上腺素能受体阻断的抗性。
Naunyn Schmiedebergs Arch Pharmacol. 1981;317(4):331-8. doi: 10.1007/BF00501315.
8
Estimation of pKB values for histamine H2-receptor antagonists using an in vitro acid secretion assay.使用体外胃酸分泌试验估算组胺H2受体拮抗剂的pKB值。
Br J Pharmacol. 1980 Mar;68(3):413-23. doi: 10.1111/j.1476-5381.1980.tb14555.x.
9
The classification of peripheral 5-HT2-like receptors using tryptamine agonist and antagonist analogues.使用色胺激动剂和拮抗剂类似物对外周5-HT2样受体进行分类。
Br J Pharmacol. 1986 Nov;89(3):493-9. doi: 10.1111/j.1476-5381.1986.tb11149.x.
10
Differences in agonist dissociation constant estimates for 5-HT at 5-HT2-receptors: a problem of acute desensitization?5-羟色胺在5-HT2受体上激动剂解离常数估计值的差异:急性脱敏问题?
Br J Pharmacol. 1988 Oct;95(2):569-77. doi: 10.1111/j.1476-5381.1988.tb11678.x.