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Alcohol and local anesthetic effects on Na+-dependent Ca2+ fluxes in brain synaptic membrane vesicles.

Abstract：

:Resealed synaptic plasma membrane vesicles exhibit Na+-dependent Ca2+ transport activity which may participate in regulation of free Ca2+ concentrations in nerve endings. Sodium chloride-loaded vesicles took up Ca2+ from the external medium (150 mM KCl-25 mM Tris/HCl) in the presence of an outward-directed Na+ gradient, a Ca2+ concentration of 38.6 microM producing half-maximal uptake at 23 degrees. Methanol (5-200 mM) and low concentrations of ethanol (5-25 mM) enhanced the Na+-dependent Ca2+ influx measured at 23 degrees. Higher ethanol concentrations (100-600 mM), as well as 1-propanol and 1-butanol (10-200 mM), produced only inhibition of Ca2+ fluxes. Dixon plot analysis of the inhibitory phase revealed that ethanol inhibited Ca2+ uptake in an apparently competitive manner with respect to Ca2+ concentration, and the Ki obtained from these experiments was 1.01 M ethanol. The inhibition of Ca2+ fluxes by butanol was non-competitive, and the Ki was 68.6 mM. The local anesthetics dibucaine and tetracaine also inhibited Ca2+ fluxes with IC50 values of 1.8 mM for tetracaine and 0.46 mM for dibucaine. The possible physiologic consequences of this inhibition of Na+-Ca2+ countertransport is synaptic membranes by the alcohols and local anesthetics are discussed with regard to neuronal transmission and membrane conductance.

journal_name

Biochem Pharmacol

journal_title

Biochemical pharmacology

authors

Michaelis ML,Michaelis EK

doi

10.1016/0006-2952(83)90612-3

subject

Has Abstract

pub_date

1983-03-15 00:00:00

pages

963-9

issue

6

eissn

0006-2952

issn

1873-2968

pii

0006-2952(83)90612-3

journal_volume

32

pub_type

杂志文章

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