Muscle-type nicotinic receptor

The muscle-type nicotinic receptor is a type of nicotinic acetylcholine receptor, consisting of the subunit combination (α1)2β1δε (adult receptor) or (α1)2β1δγ (fetal receptor).[1]

It is located in the neuromuscular junction, where activation yields EPSP, mainly by increased Na+ and K+ conductance.

Inhibitors

Mechanisms of Inhibition

Lidocaine 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.[2] Diethylamine (DEA), 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] 2,6-Dimethylaniline (DMA), 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.[3]

Ligands

Agonist

Partial Agonists

Antagonists

See also
  • Ganglion type nicotinic receptor

References
  1. Rang HP, Dale MM, Ritter JM, Moore PK, et al. (2003). Pharmacology (5th ed.). Churchill Livingstone. p. 138. ISBN 978-0-443-07145-4.
  2. Alberola-Die A, Fernández-Ballester G, González-Ros JM, Ivorra I, Morales A (2016-02-15). "Muscle-Type Nicotinic Receptor Blockade by Diethylamine, the Hydrophilic Moiety of Lidocaine". Frontiers in Molecular Neuroscience. 9: 12. doi:10.3389/fnmol.2016.00012. PMC 4753328. PMID 26912995.
  3. Alberola-Die A, Fernández-Ballester G, González-Ros JM, Ivorra I, Morales A (2016-11-24). "Muscle-Type Nicotinic Receptor Modulation by 2,6-Dimethylaniline, a Molecule Resembling the Hydrophobic Moiety of Lidocaine". Frontiers in Molecular Neuroscience. 9: 127. doi:10.3389/fnmol.2016.00127. PMC 5121239. PMID 27932949.
  4. Marshall CG, Ogden DC, Colquhoun D (September 1990). "The actions of suxamethonium (succinyldicholine) as an agonist and channel blocker at the nicotinic receptor of frog muscle". The Journal of Physiology. 428: 155–74. doi:10.1113/jphysiol.1990.sp018205. PMC 1181640. PMID 2133043.
  5. "Acetylcholine". Neurosci.pharm, MBC 3320. Archived from the original on 2007-12-27.
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