Drug intelligence / Profile preview

hexamethonium

Development stage
Discontinued
Modality
Small Molecules
Administration
Oral, Intravenous, Subcutaneous
01

Overview

Hexamethonium is a small molecule, quaternary ammonium compound that acts as a non-depolarizing ganglionic blocker and prototypical nicotinic cholinergic antagonist. It selectively blocks neuronal nicotinic acetylcholine receptors (nAChRs) at autonomic ganglia by binding primarily within or on the ion channel pore of the receptor, rather than at the acetylcholine binding site. This results in inhibition of both sympathetic and parasympathetic nervous system transmission at preganglionic sites. Hexamethonium does not affect muscarinic acetylcholine receptors or skeletal neuromuscular junctions. Historically, it was used to treat hypertension but has been replaced by more specific agents due to its broad autonomic effects and side effect profile; it is now mainly used as a research tool[1][2][3][5].

Other names
HexoniumhexamethonehexathonideHexamethonumN,N,N,N',N',N'-hexamethylhexane-1,6-diaminium
02

Targets

M1 (Muscarinic acetylcholine receptor M1)CHRM2 (M2)CHRM3 (M3)CHRNA4 (nAChR α4)

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