[Effect of physiologic concentrations of local anesthetics of the procaine series on the structural and functional state of cerebral synaptosome membranes].
Studies are presented of the effect of procaine group anesthetics on rat brain synaptosome stability to dodecyl sulfate and on catalytic properties of the membrane bound alkaline phosphatase. The dose curves of detergent stability are characterized by two maxima, one at 3.10(-4) M for tetracaine, 2.10(-6) M for lidocaine and 5.10(-5) M for procaine; the other being at 10(-3) M for all anesthetics. The curves of Vmax and KM versus procaine concentration to exhibit the minimum at 5.10(-7) M and maximum at 3,2.10(-6) M. Procaine at 5.10(-7) M increases enthalpy and enthropy of membraneous alkaline phosphatase. It is suggested that interactions between anesthetics and centers of high affinity lead to synaptosome structural rearrangements, which affect the properties of membraneous enzymes.
D000469:Alkaline Phosphatase; D000818:Animals; D001921:Brain / Q000648:ultrastructure*; D002384:Catalysis; D004305:Dose-Response Relationship, Drug; D066298:In Vitro Techniques; D008012:Lidocaine / Q000494:pharmacology*; D011343:Procaine / Q000494:pharmacology*; D051381:Rats; D012967:Sodium Dodecyl Sulfate; D013574:Synaptosomes / Q000187:drug effects* / Q000201:enzymology; D013748:Tetracaine / Q000494:pharmacology*; D013816:Thermodynamics
D013748:Tetracaine; D012967:Sodium Dodecyl Sulfate; D011343:Procaine; D008012:Lidocaine; D000469:Alkaline Phosphatase
Vliianie fiziologicheskikh kontsentratsiĭ lokal'nykh anestetikov prokainovogo riada na strukturnoe i funktsional'noe sostoianie sinaptosomal'nykh membran mozga.