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Open AccessJournal ArticleDOI

Some quantitative uses of drug antagonists

TLDR
Various applications of pAx measurements are discussed based on the hypothesis that drugs and drug antagonists compete for receptors according to the mass law, and a new measure, pAh, is introduced to express the activity of unsurmountable antagonists.
Abstract
Various applications of pAx measurements are discussed based on the hypothesis that drugs and drug antagonists compete for receptors according to the mass law. Examples are given illustrating the use of pAx measurements to identify agonists which act on the same receptors and to compare the receptors of different tissues. Tests of competitive and noncompetitive antagonism are considered in relation to the antagonisms acetylcholine-atropine, histamine-atropine and acetylcholine-cinchonidine. A new measure, pAh, is introduced to express the activity of unsurmountable antagonists.

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Citations
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Journal ArticleDOI

Definition and antagonism of histamine H 2 -receptors.

TL;DR: H2-receptor antagonist, a new group of drugs, may help to unravel the physiology of histamine and gastrin.
Journal ArticleDOI

Functional comparisons of three glutamate transporter subtypes cloned from human motor cortex

TL;DR: Three glutamate transporters expressed in human motor cortex, termed EAAT1, EAAT2, and EAAT3 (for excitatory amino acid transporter), have been characterized by their molecular cloning and functional expression to provide a foundation for understanding the role of glutamate transportters in human excitesmission and in neuropathology.
Journal ArticleDOI

Operational models of pharmacological agonism

TL;DR: An alternative model is proposed, representing the cognitive and transducer functions of a receptor, that describes agonist action with one fewer parameter than the traditional model, and provides a chemical definition of intrinsic efficacy making this parameter experimentally accessible in principle.
Book ChapterDOI

The Classification of Adrenoceptors (Adrenergic Receptors). An Evaluation from the Standpoint of Receptor Theory

TL;DR: A wide variety of tissues undergo a change of functional state on exposure to noradrenaline or adrenaline, and agents which produce responses in tissues by interacting with adrenoceptors are referred to, for convenience, as adrenergic agonists.
Journal ArticleDOI

G Protein-Coupled Receptor Allosterism and Complexing

TL;DR: It is proposed that the study of allosteric phenomena will become of progressively greater import to the drug discovery process due to the advent of newer and more sensitive GPCR screening technologies.
References
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Journal ArticleDOI

Definition and antagonism of histamine H 2 -receptors.

TL;DR: H2-receptor antagonist, a new group of drugs, may help to unravel the physiology of histamine and gastrin.
Journal ArticleDOI

pA, a new scale for the measurement of drug antagonism

TL;DR: This is the first of a set of three papers in the Journal that were to transform the study of drug antagonism and Schild proposed and validated a new measure of antagonist action, pA, and showed how pAx measurements could provide a reproducible and statistically satisfactory index of the effectiveness of an antagonist action.
Journal ArticleDOI

The Use of Chemical Potentials as Indices of Toxicity

TL;DR: A number of investigation have been published in which attempts are made to correlate the chemical or physical properties of substances with the intensity of their toxic action as mentioned in this paper, where the experiments consisted in the determination of the molar concentrations of the compounds which produced equi-toxic on a selected organism.
Journal Article

The pharmacology of vascular smooth muscle.

TL;DR: As one of the part of book categories, pharmacology of vascular smooth muscle always becomes the most wanted book.
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