Amphetamine acts as a channel blocker of the acetylcholine receptor
NON-COMPETITIVE inhibitors (NCIs) of the nicotinic receptors (AChR) comprise a wide range of compounds. The chemical scaffold of amphetamine is similar to those of some NCIs. We investigated the effects of amphetamine (1–100 μM) on the muscle AChR by recording single-channel currents. The drug reduc...
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| Veröffentlicht in: | Neuroreport 1999-07, Vol.10 (10), p.2175-2181 |
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| container_title | Neuroreport |
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| creator | Spitzmaul, Guillermo F del Carmen Esandi, María Bouzat, Cecilia |
| description | NON-COMPETITIVE inhibitors (NCIs) of the nicotinic receptors (AChR) comprise a wide range of compounds. The chemical scaffold of amphetamine is similar to those of some NCIs. We investigated the effects of amphetamine (1–100 μM) on the muscle AChR by recording single-channel currents. The drug reduces the duration of the open state in a concentration-dependent manner and causes the appearance of brief closings, resembling the action of open-channel blockers. The forward rate constant for the blocking process is of the order of 10 M s and the blocking process is voltage dependent. The results are consistent with the steric block of the open channel as the primary action of amphetamine. At high drug concentrations the mechanism of inhibition deviates from that of classical open-channel blockers. |
| doi_str_mv | 10.1097/00001756-199907130-00032 |
| format | Article |
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At high drug concentrations the mechanism of inhibition deviates from that of classical open-channel blockers.</description><identifier>ISSN: 0959-4965</identifier><identifier>EISSN: 1473-558X</identifier><identifier>DOI: 10.1097/00001756-199907130-00032</identifier><identifier>PMID: 10424694</identifier><language>eng</language><publisher>Hagerstown, MD: Lippincott Williams & Wilkins, Inc</publisher><subject>Amphetamine - pharmacology ; Animals ; Biological and medical sciences ; Cell Line ; Cell receptors ; Cell structures and functions ; Fundamental and applied biological sciences. 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The chemical scaffold of amphetamine is similar to those of some NCIs. We investigated the effects of amphetamine (1–100 μM) on the muscle AChR by recording single-channel currents. The drug reduces the duration of the open state in a concentration-dependent manner and causes the appearance of brief closings, resembling the action of open-channel blockers. The forward rate constant for the blocking process is of the order of 10 M s and the blocking process is voltage dependent. The results are consistent with the steric block of the open channel as the primary action of amphetamine. At high drug concentrations the mechanism of inhibition deviates from that of classical open-channel blockers.</description><subject>Amphetamine - pharmacology</subject><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Cell Line</subject><subject>Cell receptors</subject><subject>Cell structures and functions</subject><subject>Fundamental and applied biological sciences. Psychology</subject><subject>Humans</subject><subject>Mice</subject><subject>Molecular and cellular biology</subject><subject>Monoamines receptors (catecholamine, serotonine, histamine, acetylcholine)</subject><subject>Patch-Clamp Techniques</subject><subject>Receptors, Cholinergic - drug effects</subject><issn>0959-4965</issn><issn>1473-558X</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1999</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqF0U2LFDEQBuAgiju7-hekD-Kt11S-67gMrgoLXhS8hXS6mh433T0mPSz7780448dFDIGE8FQVvGGsAX4NHO1bXhdYbVpARG5B8ra-SPGEbUBZ2Wrtvj5lG44aW4VGX7DLUr5Vghzcc3YBXAllUG3Y9mbaj7SGaTdTE-JamlB3E8cwz5SaLi3xnnKzDM06HgGtjymOSzryTJH265JfsGdDSIVens8r9uX23efth_bu0_uP25u7NiowokXVcdeJoJ0ZSMpeAgorgSJwKzSC6UQUItgBFHJthO2krRfR91H1wRh5xd6c-u7z8v1AZfXTrkRKKcy0HIo3iAIt2P_CSrhzGip0JxjzUkqmwe_zbgr50QP3x6T9r6T976T9z6Rr6avzjEM3Uf9X4SnaCl6fQSgxpCGHOe7KH-fQgTr2USf2sKSVcrlPhwfKfqSQ1tH_66PlD3Tuk0I</recordid><startdate>19990713</startdate><enddate>19990713</enddate><creator>Spitzmaul, Guillermo F</creator><creator>del Carmen Esandi, María</creator><creator>Bouzat, Cecilia</creator><general>Lippincott Williams & Wilkins, Inc</general><general>Lippincott Williams and Wilkins</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7TK</scope><scope>7X8</scope></search><sort><creationdate>19990713</creationdate><title>Amphetamine acts as a channel blocker of the acetylcholine receptor</title><author>Spitzmaul, Guillermo F ; del Carmen Esandi, María ; Bouzat, Cecilia</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4162-94b08b2a586fe33d3192731ec10725916b2c22a7f14905627b379052ddc4da663</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1999</creationdate><topic>Amphetamine - pharmacology</topic><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Cell Line</topic><topic>Cell receptors</topic><topic>Cell structures and functions</topic><topic>Fundamental and applied biological sciences. Psychology</topic><topic>Humans</topic><topic>Mice</topic><topic>Molecular and cellular biology</topic><topic>Monoamines receptors (catecholamine, serotonine, histamine, acetylcholine)</topic><topic>Patch-Clamp Techniques</topic><topic>Receptors, Cholinergic - drug effects</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Spitzmaul, Guillermo F</creatorcontrib><creatorcontrib>del Carmen Esandi, María</creatorcontrib><creatorcontrib>Bouzat, Cecilia</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Neurosciences Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Neuroreport</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Spitzmaul, Guillermo F</au><au>del Carmen Esandi, María</au><au>Bouzat, Cecilia</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Amphetamine acts as a channel blocker of the acetylcholine receptor</atitle><jtitle>Neuroreport</jtitle><addtitle>Neuroreport</addtitle><date>1999-07-13</date><risdate>1999</risdate><volume>10</volume><issue>10</issue><spage>2175</spage><epage>2181</epage><pages>2175-2181</pages><issn>0959-4965</issn><eissn>1473-558X</eissn><abstract>NON-COMPETITIVE inhibitors (NCIs) of the nicotinic receptors (AChR) comprise a wide range of compounds. 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| ispartof | Neuroreport, 1999-07, Vol.10 (10), p.2175-2181 |
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| language | eng |
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| source | MEDLINE; Journals@Ovid Complete |
| subjects | Amphetamine - pharmacology Animals Biological and medical sciences Cell Line Cell receptors Cell structures and functions Fundamental and applied biological sciences. Psychology Humans Mice Molecular and cellular biology Monoamines receptors (catecholamine, serotonine, histamine, acetylcholine) Patch-Clamp Techniques Receptors, Cholinergic - drug effects |
| title | Amphetamine acts as a channel blocker of the acetylcholine receptor |
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