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Muscle-type nicotinic receptor
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<h2 id="activation">Activation</h2> <p><a href="/facts/Tetraethylammonium/kbXMoR1H">Tetraethylammonium (TEA)</a> is a molecule found to be a weak <a href="/facts/Agonist/nz8U5NNp">agonist</a> 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.<a class="footnote-ref" id="fnref:2" href="#fn:2"><sup>2</sup></a> </p> <h2 id="inhibition">Inhibition</h2> <p><a href="/facts/Lidocaine/MxtjXuzI">Lidocaine</a>, a <a href="/facts/Local_anesthetic/5aA2qews">local anesthetic</a>, 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.<a class="footnote-ref" id="fnref:3" href="#fn:3"><sup>3</sup></a> <a href="/facts/Diethylamine/wlVINVXe">Diethylamine (DEA)</a>, 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.<a class="footnote-ref" id="fnref:4" href="#fn:4"><sup>4</sup></a> 2,6-<a href="/facts/Dimethylaniline/G75Y4YST">Dimethylaniline (DMA)</a>, 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 <a href="/facts/Non-competitive_inhibition/kgDxxVSx">non-competitive inhibition</a> and restricting the channel from opening.<a class="footnote-ref" id="fnref:5" href="#fn:5"><sup>5</sup></a> </p><p><a href="/facts/Benzocaine/2xMLUQf0">Benzocaine</a> and <a href="/facts/Tetracaine/1DdLV4w8">tetracaine</a> are also <a href="/facts/Local_anesthetic/5aA2qews">local anesthetics</a> that have an inhibitory effect on the muscle‐type nicotinic receptor. <a href="/facts/Benzocaine/2xMLUQf0">Benzocaine</a> is a permanently uncharged species that inhibits the receptor by plugging the pore of the opened channel.<a class="footnote-ref" id="fnref:6" href="#fn:6"><sup>6</sup></a> <a href="/facts/Tetracaine/1DdLV4w8">Tetracaine</a> is a permanently positively charged species. It can bind to the receptor at different sites in both the open and closed conformations.<a class="footnote-ref" id="fnref:7" href="#fn:7"><sup>7</sup></a> Both of these local anesthetics enhance nAChR <a href="/facts/Desensitization_(receptor)/6nRoa28r">desensitization</a>.<a class="footnote-ref" id="fnref:8" href="#fn:8"><sup>8</sup></a><a class="footnote-ref" id="fnref:9" href="#fn:9"><sup>9</sup></a> </p> <h2 id="ligands">Ligands</h2> <h3>Agonist</h3> <ul><li><a href="/facts/Acetylcholine/v1d3wRUd">Acetylcholine</a></li></ul> <h3>Partial Agonists</h3> <ul><li><a href="/facts/Carbachol/LlX8PM5H">Carbachol</a></li> <li><a href="/facts/Suxamethonium/LgaWdMuy">Suxamethonium</a><a class="footnote-ref" id="fnref:10" href="#fn:10"><sup>10</sup></a></li></ul> <h3>Antagonists</h3> <ul><li><a href="/facts/%25CE%2591-Bungarotoxin/6YSRjdQy">α-Bungarotoxin</a><a class="footnote-ref" id="fnref:11" href="#fn:11"><sup>11</sup></a></li> <li><a href="/facts/%25CE%2591-Conotoxin/EXqt4sSo">α-Conotoxin</a></li> <li><a href="/facts/Hexamethonium/5xpAm1T2">Hexamethonium</a></li> <li><a href="/facts/Pancuronium/MnwT0Hk8">Pancuronium</a></li> <li><a href="/facts/Tubocurarine/o8AhgYY9">Tubocurarine</a></li></ul> <h2 id="see-also">See also</h2> <ul><li><a href="/facts/Nicotinic_acetylcholine_receptor/k2s2pPHr">Nicotinic acetylcholine receptor</a></li> <li><a href="/facts/Ganglion_type_nicotinic_receptor/3m4rqQdN">Ganglion type nicotinic receptor</a></li></ul> <h2 id="references">References</h2> <ol> <li id="fn:1"><p>Rang HP, Dale MM, Ritter JM, Moore PK, et al. (2003). Pharmacology (5th ed.). Churchill Livingstone. p. 138. ISBN 978-0-443-07145-4. <a href="978-0-443-07145-4" target="_blank">978-0-443-07145-4</a> <a href="#fnref:1" class="footnote-back-ref">↩</a></p></li> <li id="fn:2"><p>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 href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2343137" target="_blank">https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2343137</a> <a href="#fnref:2" class="footnote-back-ref">↩</a></p></li> <li id="fn:3"><p>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. <a href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4753328" target="_blank">https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4753328</a> <a href="#fnref:3" class="footnote-back-ref">↩</a></p></li> <li id="fn:4"><p>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. <a href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4753328" target="_blank">https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4753328</a> <a href="#fnref:4" class="footnote-back-ref">↩</a></p></li> <li id="fn:5"><p>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. <a href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5121239" target="_blank">https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5121239</a> <a href="#fnref:5" class="footnote-back-ref">↩</a></p></li> <li id="fn:6"><p>Cobo, 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. <a href="https://pubmed.ncbi.nlm.nih.gov/31158437" target="_blank">https://pubmed.ncbi.nlm.nih.gov/31158437</a> <a href="#fnref:6" class="footnote-back-ref">↩</a></p></li> <li id="fn:7"><p>Cobo, 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. PMC 6092513. PMID 30135641. <a href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6092513" target="_blank">https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6092513</a> <a href="#fnref:7" class="footnote-back-ref">↩</a></p></li> <li id="fn:8"><p>Cobo, 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. <a href="https://pubmed.ncbi.nlm.nih.gov/31158437" target="_blank">https://pubmed.ncbi.nlm.nih.gov/31158437</a> <a href="#fnref:8" class="footnote-back-ref">↩</a></p></li> <li id="fn:9"><p>Cobo, 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. PMC 6092513. PMID 30135641. <a href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6092513" target="_blank">https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6092513</a> <a href="#fnref:9" class="footnote-back-ref">↩</a></p></li> <li id="fn:10"><p>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. <a href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1181640" target="_blank">https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1181640</a> <a href="#fnref:10" class="footnote-back-ref">↩</a></p></li> <li id="fn:11"><p>"Acetylcholine". Neurosci.pharm, MBC 3320. Archived from the original on 2007-12-27. <a href="https://web.archive.org/web/20071227192643/http://www.neurosci.pharm.utoledo.edu/MBC3320/nicotinic.htm" target="_blank">https://web.archive.org/web/20071227192643/http://www.neurosci.pharm.utoledo.edu/MBC3320/nicotinic.htm</a> <a href="#fnref:11" class="footnote-back-ref">↩</a></p></li> </ol>