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Edrophonium

依酚溴銨
Mechanism of action:
Edrophonium 是一種可逆性乙醯膽鹼酯酶抑制劑(reversible acetylcholinesterase inhibitor),屬於季銨鹽(quaternary ammonium)類化合物。Edrophonium 以非共價鍵、靜電作用結合於乙醯膽鹼酯酶的活性位點,暫時抑制乙醯膽鹼酯酶的活性。這會使突觸間隙中乙醯膽鹼的濃度上升,增強其對運動終板(motor end-plate)上的菸鹼型乙醯膽鹼受體(nicotinic acetylcholine receptor)的刺激。
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.
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