Tetraethylammonium (TEA) is a molecule found to be a weak agonist of the muscle‐type nicotinic receptor. Since receptor activation occurs as isolated bursts, it has been proposed that the receptors have a very low channel‐opening rate constant when bound to TEA.[2]
Inhibitionedit
Lidocaine, a local anesthetic, 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.[3]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.[3] 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.[4]
Benzocaine and tetracaine are also local anesthetics that have an inhibitory effect on the muscle‐type nicotinic receptor. Benzocaine is a permanently uncharged species that inhibits the receptor by plugging the pore of the opened channel.[5]Tetracaine is a permanently positively charged species. It can bind to the receptor at different sites in both the open and closed conformations.[6] Both of these local anesthetics enhance nAChR desensitization.[5][6]
^Rang HP, Dale MM, Ritter JM, Moore PK, et al. (2003). Pharmacology (5th ed.). Churchill Livingstone. p. 138. ISBN978-0-443-07145-4.
^Akk, Gustav; Steinbach, Joe Henry (2003-08-15). "Activation and block of mouse muscle-type nicotinic receptors by tetraethylammonium". The Journal of Physiology. 551 (Pt 1): 155–168. doi:10.1113/jphysiol.2003.043885. ISSN 0022-3751. PMC2343137. PMID 12824448.
^ abAlberola-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. PMC4753328. PMID 26912995.
^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. PMC5121239. PMID 27932949.
^ abCobo, Raúl; Nikolaeva-Koleva, Magdalena; Alberola-Die, Armando; Fernández-Ballester, Gregorio; González-Ros, José Manuel; Ivorra, Isabel; Morales, Andrés (15 July 2020). "Mechanisms of Blockade of the Muscle-Type Nicotinic Receptor by Benzocaine, a Permanently Uncharged Local Anesthetic". Neuroscience. 439: 62–79. doi:10.1016/j.neuroscience.2019.05.043. hdl:10045/107949. ISSN 1873-7544. PMID 31158437. S2CID 171092620.
^ abCobo, Raúl; Nikolaeva, Magdalena; Alberola-Die, Armando; Fernández-Ballester, Gregorio; González-Ros, José M.; Ivorra, Isabel; Morales, Andrés (2018-08-08). "Mechanisms Underlying the Strong Inhibition of Muscle-Type Nicotinic Receptors by Tetracaine". Frontiers in Molecular Neuroscience. 11: 193. doi:10.3389/fnmol.2018.00193. ISSN 1662-5099. PMC6092513. PMID 30135641.
^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. PMC1181640. PMID 2133043.
^. Neurosci.pharm, MBC 3320. Archived from the original on 2007-12-27.
This biochemistry article is a stub. You can help Wikipedia by expanding it.
muscle, type, nicotinic, receptor, muscle, type, nicotinic, receptor, type, nicotinic, acetylcholine, receptor, consisting, subunit, combination, 2β1δε, adult, receptor, 2β1δγ, fetal, receptor, these, receptors, found, neuromuscular, junctions, where, activati. The muscle type nicotinic receptor is a type of nicotinic acetylcholine receptor consisting of the subunit combination a1 2b1de adult receptor or a1 2b1dg fetal receptor 1 These receptors are found in neuromuscular junctions where activation leads to an excitatory postsynaptic potential EPSP mainly by increased Na and K permeability Contents 1 Activation 2 Inhibition 3 Ligands 3 1 Agonist 3 2 Partial Agonists 3 3 Antagonists 4 See also 5 ReferencesActivation editTetraethylammonium TEA is a molecule found to be a weak agonist of the muscle type nicotinic receptor Since receptor activation occurs as isolated bursts it has been proposed that the receptors have a very low channel opening rate constant when bound to TEA 2 Inhibition editLidocaine a local anesthetic 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 3 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 3 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 4 Benzocaine and tetracaine are also local anesthetics that have an inhibitory effect on the muscle type nicotinic receptor Benzocaine is a permanently uncharged species that inhibits the receptor by plugging the pore of the opened channel 5 Tetracaine is a permanently positively charged species It can bind to the receptor at different sites in both the open and closed conformations 6 Both of these local anesthetics enhance nAChR desensitization 5 6 Ligands editAgonist edit AcetylcholinePartial Agonists edit Carbachol Suxamethonium 7 Antagonists edit a Bungarotoxin 8 a Conotoxin Hexamethonium Pancuronium TubocurarineSee also editNicotinic acetylcholine receptor Ganglion type nicotinic receptorReferences edit Rang HP Dale MM Ritter JM Moore PK et al 2003 Pharmacology 5th ed Churchill Livingstone p 138 ISBN 978 0 443 07145 4 Akk Gustav Steinbach Joe Henry 2003 08 15 Activation and block of mouse muscle type nicotinic receptors by tetraethylammonium The Journal of Physiology 551 Pt 1 155 168 doi 10 1113 jphysiol 2003 043885 ISSN 0022 3751 PMC 2343137 PMID 12824448 a b Alberola Die A Fernandez Ballester G Gonzalez 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 Alberola Die A Fernandez Ballester G Gonzalez 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 a b Cobo Raul Nikolaeva Koleva Magdalena Alberola Die Armando Fernandez Ballester Gregorio Gonzalez Ros Jose Manuel Ivorra Isabel Morales Andres 15 July 2020 Mechanisms of Blockade of the Muscle Type Nicotinic Receptor by Benzocaine a Permanently Uncharged Local Anesthetic Neuroscience 439 62 79 doi 10 1016 j neuroscience 2019 05 043 hdl 10045 107949 ISSN 1873 7544 PMID 31158437 S2CID 171092620 a b Cobo Raul Nikolaeva Magdalena Alberola Die Armando Fernandez Ballester Gregorio Gonzalez Ros Jose M Ivorra Isabel Morales Andres 2018 08 08 Mechanisms Underlying the Strong Inhibition of Muscle Type Nicotinic Receptors by Tetracaine Frontiers in Molecular Neuroscience 11 193 doi 10 3389 fnmol 2018 00193 ISSN 1662 5099 PMC 6092513 PMID 30135641 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 Acetylcholine Neurosci pharm MBC 3320 Archived from the original on 2007 12 27 nbsp This biochemistry article is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title Muscle type nicotinic receptor amp oldid 1048210152, wikipedia, wiki, book, books, library,
