Muscle-type nicotinic receptor


The muscle-type nicotinic receptor is a type of nicotinic acetylcholine receptor, consisting of the subunit combination 2β1δε or 2β1δγ.
It is located in the neuromuscular junction, where activation yields EPSP, mainly by increased Na+ and K+ conductance.

Inhibitors

Mechanisms of Inhibition

has multiple inhibitory actions on the receptor and analysis of the structure of lidocaine has identified the presence of a hydrophobic aromatic ring and a hydrophilic terminal amine. Diethylamine, a molecule that mimics the hydrophilic moiety of lidocaine by way of a positively charged amine, has been found to block the channel when the receptor is open restricting the flow of Na+ and K+ ions. 2,6-Dimethylaniline, a molecule that mimics the hydrophobic moiety of lidocaine, has been found to bind the receptor at inter-subunit crevices of the trans-membrane spanning domain thereby causing non-competitive inhibition and restricting the channel from opening.

Ligands

Agonist