The Sound of Evolution
Edrophonium
Mechanism of action:
Edrophonium is a reversible acetylcholinesterase inhibitor and belongs to the quaternary ammonium class of compounds. It binds to the active site of acetylcholinesterase through non-covalent and electrostatic interactions, temporarily inhibiting the enzyme's activity. This increases the concentration of acetylcholine in the synaptic cleft and enhances stimulation of nicotinic acetylcholine receptors at the motor end-plate.
Reference(s):
1. Harel M et al. (1992). Conversion of acetylcholinesterase to butyrylcholinesterase: modeling and mutagenesis. Proc Natl Acad Sci U S A.
2. Saxena A et al. (1997). Differences in active site gorge dimensions of cholinesterases revealed by binding of inhibitors to human butyrylcholinesterase. Biochemistry.
3. Macdonald IR et al. (2012). Probing the peripheral site of human butyrylcholinesterase. Biochemistry.