Local anesthetics: hydrophilic and hydrophobic pathways for the drug-receptor reaction.

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Local anesthetics: hydrophilic and hydrophobic pathways for the drug- receptor reaction

The properties of Na channels of the node of Ranvier are altered by neutral, amine, and quaternary local anesthetic compounds. The kinetics of the Na currents are governed by a composite of voltage- and time-dependent gating processes with voltage- and time-dependent block of channels by drug. Conventional measurements of steady-state sodium inactivation by use of 50-ms prepulses show a large n...

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Transdermal delivery of hydrophobic and hydrophilic local anesthetics from o/w and w/o Brij 97-based microemulsions.

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Local anesthetics (LA) have been found to interact with phospholipids and lipids extracted from nerve and muscle. This reaction is demonstrated by: (a) Inhibition by LA of phospholipid (and tissue lipid) facilitated transport of calcium from a methanol: water phase into chloroform. This action is dependent upon the cationic form of the LA. (b) LA increase the electrical resistance of "membranes...

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ژورنال

عنوان ژورنال: Journal of General Physiology

سال: 1977

ISSN: 0022-1295,1540-7748

DOI: 10.1085/jgp.69.4.497