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Active ingredient: Lidocaine - Chemisty and Biological Activity

Chemisty and Biological Activity

Chemical Formula

C14H22N2O

Chemical Name

2-diethylamino-N-(2,6-dimethylphenyl)-ethanamide

Chemical Structure

Molecular Weight

234.337 g/mol

Physical State

Solid

Melting Point

68.5oC (boiling point 181oC)

Water Solubility

4100 mg/L

Isoelectric Point

8.01

Organisms Affected

Humans and other mammals

Phase 1 Metabolising Enzyme (1-st Step of Metabolism)

CYP1A2; CYP2D6

Primary Drug Target
NameVoltage-gated sodium channel
Gene NameSCN5A
SynonymsSodium channel protein type V alpha subunit; Voltage-gated sodium channel alpha subunit Nav1.5; Sodium channel protein, cardiac muscle alpha-subunit; HH1
Specific FunctionThis protein mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na+ ions may pass in accordance with their electrochemical gradient. It is a tetrodotoxin-resistant Na+ channel isoform. This channel is responsible for the initial upstroke of the action potential in the electrocardiogram

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