Interaction of calcium and local anesthetics with skeletal muscle microsomes

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Title Interaction of calcium and local anesthetics with skeletal muscle microsomes
Publication Type thesis
School or College College of Pharmacy
Department Pharmacology & Toxicology
Author Bondani, Augusto
Date 1969-08
Description The influence of Ca++, several drugs, and pH on the binding of Ca++ by skeletal muscle microsomes was studies in vitro. A mass-law graphic analysis of the results revealed the presence of three distinct species of Ca++-binding sites in the microsomes, and the binding at only one of these sites was antagonized by local anesthetics and quinidine. These drugs also decreased the maximum Ca++-binding capacity of the microsomes. Caffeine and ouabain exerted no effect on the binding at any of the sites. Procaine was also bound by microsomes, and this binding was antagonized by Ca++ which also decreased the maximum procaine-binding capacity of microsomes. The sites that bind procaine and Ca++ are not identical because the maximum-binding capacities of the interacting sites are distinctly different. The influence of pH on the ability of drugs to antagonized Ca++-binding indicates that the displacing activity increases as the percerntage of the drug in the nonionized form increases. All of the data obtained in the above studies are consistent with the interpretation that local anesthetics of the procaine type and quinidine noncompetitively antagonize the binding at Ca++ by microsomes. The pharmacological significance of a noncompetitive interaction may be related to the property of local anesthetics and quinidine to increase contractile tension in skeletal muscle rather than to their ability to stabilize the cell membrane.
Type Text
Publisher University of Utah
Subject Pharmacokinetics; Drug Studies
Subject MESH Calcium; Microsomes; Proteins
Dissertation Institution University of Utah
Dissertation Name PhD
Language eng
Relation is Version of Digital reproduction of "Interaction of calcium and local anesthetics with skeletal muscle microsomes." Spencer S. Eccles Health Sciences Library. Print version of "Interaction of calcium and local anesthetics with skeletal muscle microsomes." available at J. Willard Marriott Library Special Collection. QP6.5 1969 .B6.
Rights Management © Augusto Bondani.
Format application/pdf
Format Medium application/pdf
Format Extent 702,589 bytes
Identifier undthes,4810
Source Original: University of Utah Spencer S. Eccles Health Sciences Library (no longer available).
Master File Extent 702,619 bytes
ARK ark:/87278/s6w66njz
Setname ir_etd
ID 190840
Reference URL https://collections.lib.utah.edu/ark:/87278/s6w66njz
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