Pancuronium, vecuronium, and d-tubocurarine inhibit and succinylcholine stimulates choline acetyltransferase activity. 1990

J R Kambam, and V E Janson, and P Day, and B V Sastry
Department of Anesthesiology, Vanderbilt University Medical Center, Nashville, Tennessee 37232.

The effects of the nondepolarizing muscle relaxants (NDMR), pancuronium, vecuronium, and d-tubocurarine and a depolarizing muscle relaxant, succinylcholine, were studied on choline acetyltransferase (ChAT) activity. A radiochemical assay was used in the determination of ChAT activity using purified placental enzyme. Pancuronium at concentrations of 10(-7) M, 10(-6) M, 10(-5) M, 10(-4) M, and 10(-3) M inhibited ChAT activity by 3, 10, 15, 40 and 85 per cent, respectively; vecuronium at concentrations of 10(-6) M, 10(-5) M, 10(-4) M, and 10(-3) M inhibited ChAT activity by 5, 10, 26 and 57 per cent, respectively; d-tubocurarine at concentrations of 10(-6) M, 10(-5) M, 10(-4) M, and 10(-3) M inhibited ChAT activity by 0, 4, 12.5 and 29 per cent, respectively; whereas succinylcholine at concentrations of 10(-7) M, 10(-6) M, 10(-5) M, and 10(-4) M activated ChAT activity by 8, 10, 1, and 2 per cent, respectively. Even though our present data demonstrated a significant dose-dependent inhibitory effect on ChAT activity by pancuronium, vecuronium and d-tubocurarine, it is unlikely that this inhibitory effect will contribute to the mechanism of action of NDMR. Our data, however, may suggest an additional mechanism for the phenomena of tetanic and train-of-four fades that are seen following the administration of nondepolarizing muscle relaxants.

UI MeSH Term Description Entries
D007475 Ion Exchange Resins High molecular weight, insoluble polymers which contain functional groups that are capable of undergoing exchange reactions (ION EXCHANGE) with either cations or anions. Ion Exchange Resin,Exchange Resin, Ion,Exchange Resins, Ion,Resin, Ion Exchange,Resins, Ion Exchange
D010197 Pancuronium A bis-quaternary steroid that is a competitive nicotinic antagonist. As a neuromuscular blocking agent it is more potent than CURARE but has less effect on the circulatory system and on histamine release. Pancuronium Bromide,Pancuronium Curamed,Pancuronium Organon,Pavulon,Bromide, Pancuronium
D012044 Regression Analysis Procedures for finding the mathematical function which best describes the relationship between a dependent variable and one or more independent variables. In linear regression (see LINEAR MODELS) the relationship is constrained to be a straight line and LEAST-SQUARES ANALYSIS is used to determine the best fit. In logistic regression (see LOGISTIC MODELS) the dependent variable is qualitative rather than continuously variable and LIKELIHOOD FUNCTIONS are used to find the best relationship. In multiple regression, the dependent variable is considered to depend on more than a single independent variable. Regression Diagnostics,Statistical Regression,Analysis, Regression,Analyses, Regression,Diagnostics, Regression,Regression Analyses,Regression, Statistical,Regressions, Statistical,Statistical Regressions
D002250 Carbon Radioisotopes Unstable isotopes of carbon that decay or disintegrate emitting radiation. C atoms with atomic weights 10, 11, and 14-16 are radioactive carbon isotopes. Radioisotopes, Carbon
D002795 Choline O-Acetyltransferase An enzyme that catalyzes the formation of acetylcholine from acetyl-CoA and choline. EC 2.3.1.6. Choline Acetylase,Choline Acetyltransferase,Acetylase, Choline,Acetyltransferase, Choline,Choline O Acetyltransferase,O-Acetyltransferase, Choline
D004305 Dose-Response Relationship, Drug The relationship between the dose of an administered drug and the response of the organism to the drug. Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D013390 Succinylcholine A quaternary skeletal muscle relaxant usually used in the form of its bromide, chloride, or iodide. It is a depolarizing relaxant, acting in about 30 seconds and with a duration of effect averaging three to five minutes. Succinylcholine is used in surgical, anesthetic, and other procedures in which a brief period of muscle relaxation is called for. Succinyldicholine,Suxamethonium,Anectine,Celocurine,Dicholine Succinate,Ditilin,Listenon,Lysthenon,Myorelaxin,Quelicin,Succicuran,Succinylcholine Chloride,Succinylcholine Dibromide,Succinylcholine Dichloride,Succinylcholine Dichloride, Di-H2O,Succinylcholine Diiodide,Succinylcholine Diperchlorate,Succinylcholine Iodide,Suxamethonium Bromide,Suxamethonium Chloride,Bromide, Suxamethonium,Dibromide, Succinylcholine,Dichloride, Succinylcholine,Diiodide, Succinylcholine,Diperchlorate, Succinylcholine,Succinate, Dicholine,Succinylcholine Dichloride, Di H2O
D014403 Tubocurarine A neuromuscular blocker and active ingredient in CURARE; plant based alkaloid of Menispermaceae. Tubocurare,Tubocurarine Chloride,d-Tubocurare,d-Tubocurarine
D014673 Vecuronium Bromide Monoquaternary homolog of PANCURONIUM. A non-depolarizing neuromuscular blocking agent with shorter duration of action than pancuronium. Its lack of significant cardiovascular effects and lack of dependence on good kidney function for elimination as well as its short duration of action and easy reversibility provide advantages over, or alternatives to, other established neuromuscular blocking agents. NC-45,Norcuron,ORG-NC 45,ORG-NC-45,ORG-NC45,Vecuronium,Vecuronium Bromide, Quaternary Ion,Vecuronium Citrate,Vecuronium Hydrobromide,Vecuronium Hydrochloride,Vecuronium Maleate,Vecuronium Phosphate,Bromide, Vecuronium,Citrate, Vecuronium,Hydrobromide, Vecuronium,Hydrochloride, Vecuronium,Maleate, Vecuronium,NC 45,NC45,ORG NC 45,ORG NC45,ORGNC 45,ORGNC45,Phosphate, Vecuronium

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