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Antagonism of Inhalant and Volatile Anesthetic Enhancement of Glycine Receptor Function
Recent studies suggest that alcohols, volatile anesthetics, and inhaled drugs of abuse, which enhance γ-aminobutyric acid, type A, and glycine receptor-activated ion channel function, may share common or overlapping molecular sites of action on these receptors. To investigate this possibility, thes...
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| Published in: | The Journal of biological chemistry 2001-07, Vol.276 (27), p.24959-24964 |
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| container_end_page | 24964 |
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| container_title | The Journal of biological chemistry |
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| creator | Beckstead, M J Phelan, R Mihic, S J |
| description | Recent studies suggest that alcohols, volatile anesthetics, and inhaled drugs of abuse, which enhance γ-aminobutyric acid,
type A, and glycine receptor-activated ion channel function, may share common or overlapping molecular sites of action on
these receptors. To investigate this possibility, these compounds were applied singly and in combination to wild-type glycine
α 1 receptors expressed in Xenopus laevis oocytes. Data obtained from concentration-response curves of the volatile anesthetic enflurane constructed in the presence
and absence of ethanol, chloroform, or toluene were consistent with competition for a common binding pocket on these receptors.
A mutant glycine receptor, insensitive to the enhancing effects of ethanol but not anesthetics or inhalants, demonstrated
antagonism of anesthetic and inhalant effects on this receptor. Although ethanol (25â200 m m ) had no effect on its own in this receptor, it was able to inhibit reversibly the enhancing effect of enflurane, toluene,
and chloroform in a concentration-dependent manner. These data suggest the existence of overlapping molecular sites of action
for ethanol, inhalants, and volatile anesthetics on glycine receptors and illustrate the feasibility of pharmacological antagonism
of the effects of volatile anesthetics. |
| doi_str_mv | 10.1074/jbc.M011627200 |
| format | article |
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type A, and glycine receptor-activated ion channel function, may share common or overlapping molecular sites of action on
these receptors. To investigate this possibility, these compounds were applied singly and in combination to wild-type glycine
α 1 receptors expressed in Xenopus laevis oocytes. Data obtained from concentration-response curves of the volatile anesthetic enflurane constructed in the presence
and absence of ethanol, chloroform, or toluene were consistent with competition for a common binding pocket on these receptors.
A mutant glycine receptor, insensitive to the enhancing effects of ethanol but not anesthetics or inhalants, demonstrated
antagonism of anesthetic and inhalant effects on this receptor. Although ethanol (25â200 m m ) had no effect on its own in this receptor, it was able to inhibit reversibly the enhancing effect of enflurane, toluene,
and chloroform in a concentration-dependent manner. These data suggest the existence of overlapping molecular sites of action
for ethanol, inhalants, and volatile anesthetics on glycine receptors and illustrate the feasibility of pharmacological antagonism
of the effects of volatile anesthetics.</description><identifier>ISSN: 0021-9258</identifier><identifier>EISSN: 1083-351X</identifier><identifier>DOI: 10.1074/jbc.M011627200</identifier><identifier>PMID: 11346643</identifier><language>eng</language><publisher>United States: American Society for Biochemistry and Molecular Biology</publisher><subject><![CDATA[Anesthetics, Inhalation - antagonists & inhibitors ; Animals ; Binding Sites ; Chloroform - administration & dosage ; Chloroform - metabolism ; Dose-Response Relationship, Drug ; Drug Interactions ; Electrophysiology ; Enflurane - administration & dosage ; Enflurane - metabolism ; Ethanol - administration & dosage ; Ethanol - metabolism ; Oocytes - drug effects ; Oocytes - metabolism ; Receptors, Glycine - drug effects ; Receptors, Glycine - physiology ; Toluene - administration & dosage ; Toluene - metabolism ; Trichloroethanes - administration & dosage ; Trichloroethanes - metabolism ; Xenopus laevis]]></subject><ispartof>The Journal of biological chemistry, 2001-07, Vol.276 (27), p.24959-24964</ispartof><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c426t-28f5d81a04e0fbcb82a6b353f16136062da06c20b285ac697dd6d0ea31a745b63</citedby><cites>FETCH-LOGICAL-c426t-28f5d81a04e0fbcb82a6b353f16136062da06c20b285ac697dd6d0ea31a745b63</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/11346643$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Beckstead, M J</creatorcontrib><creatorcontrib>Phelan, R</creatorcontrib><creatorcontrib>Mihic, S J</creatorcontrib><title>Antagonism of Inhalant and Volatile Anesthetic Enhancement of Glycine Receptor Function</title><title>The Journal of biological chemistry</title><addtitle>J Biol Chem</addtitle><description>Recent studies suggest that alcohols, volatile anesthetics, and inhaled drugs of abuse, which enhance γ-aminobutyric acid,
type A, and glycine receptor-activated ion channel function, may share common or overlapping molecular sites of action on
these receptors. To investigate this possibility, these compounds were applied singly and in combination to wild-type glycine
α 1 receptors expressed in Xenopus laevis oocytes. Data obtained from concentration-response curves of the volatile anesthetic enflurane constructed in the presence
and absence of ethanol, chloroform, or toluene were consistent with competition for a common binding pocket on these receptors.
A mutant glycine receptor, insensitive to the enhancing effects of ethanol but not anesthetics or inhalants, demonstrated
antagonism of anesthetic and inhalant effects on this receptor. Although ethanol (25â200 m m ) had no effect on its own in this receptor, it was able to inhibit reversibly the enhancing effect of enflurane, toluene,
and chloroform in a concentration-dependent manner. These data suggest the existence of overlapping molecular sites of action
for ethanol, inhalants, and volatile anesthetics on glycine receptors and illustrate the feasibility of pharmacological antagonism
of the effects of volatile anesthetics.</description><subject>Anesthetics, Inhalation - antagonists & inhibitors</subject><subject>Animals</subject><subject>Binding Sites</subject><subject>Chloroform - administration & dosage</subject><subject>Chloroform - metabolism</subject><subject>Dose-Response Relationship, Drug</subject><subject>Drug Interactions</subject><subject>Electrophysiology</subject><subject>Enflurane - administration & dosage</subject><subject>Enflurane - metabolism</subject><subject>Ethanol - administration & dosage</subject><subject>Ethanol - metabolism</subject><subject>Oocytes - drug effects</subject><subject>Oocytes - metabolism</subject><subject>Receptors, Glycine - drug effects</subject><subject>Receptors, Glycine - physiology</subject><subject>Toluene - administration & dosage</subject><subject>Toluene - metabolism</subject><subject>Trichloroethanes - administration & dosage</subject><subject>Trichloroethanes - metabolism</subject><subject>Xenopus laevis</subject><issn>0021-9258</issn><issn>1083-351X</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2001</creationdate><recordtype>article</recordtype><recordid>eNpFkM1LwzAYxoMobk6vHiUHr51vPpq2xzG2OZgI4tctJGm6ZrTpaDNk_72RCXvh4b38nufwQ-iewJRAxp922kxfgBBBMwpwgcYEcpawlHxfojEAJUlB03yEboZhB_F4Qa7RiBDGheBsjL5mPqht593Q4q7Ca1-rRvmAlS_xZ9eo4BqLZ94OobbBGbyIgDe2tZGJ_Ko5GuctfrPG7kPX4-XBm-A6f4uuKtUM9u7_T9DHcvE-f042r6v1fLZJDKciJDSv0jInCriFShudUyU0S1lFBGECBC0VCENB0zxVRhRZWYoSrGJEZTzVgk3Q9LRr-m4YelvJfe9a1R8lAflnSEZD8mwoFh5Ohf1Bt7Y84_9KIvB4Amq3rX9cb6V2naltK2kmYiTlRVqwX_e0bc8</recordid><startdate>20010706</startdate><enddate>20010706</enddate><creator>Beckstead, M J</creator><creator>Phelan, R</creator><creator>Mihic, S J</creator><general>American Society for Biochemistry and Molecular Biology</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope></search><sort><creationdate>20010706</creationdate><title>Antagonism of Inhalant and Volatile Anesthetic Enhancement of Glycine Receptor Function</title><author>Beckstead, M J ; Phelan, R ; Mihic, S J</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c426t-28f5d81a04e0fbcb82a6b353f16136062da06c20b285ac697dd6d0ea31a745b63</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2001</creationdate><topic>Anesthetics, Inhalation - antagonists & inhibitors</topic><topic>Animals</topic><topic>Binding Sites</topic><topic>Chloroform - administration & dosage</topic><topic>Chloroform - metabolism</topic><topic>Dose-Response Relationship, Drug</topic><topic>Drug Interactions</topic><topic>Electrophysiology</topic><topic>Enflurane - administration & dosage</topic><topic>Enflurane - metabolism</topic><topic>Ethanol - administration & dosage</topic><topic>Ethanol - metabolism</topic><topic>Oocytes - drug effects</topic><topic>Oocytes - metabolism</topic><topic>Receptors, Glycine - drug effects</topic><topic>Receptors, Glycine - physiology</topic><topic>Toluene - administration & dosage</topic><topic>Toluene - metabolism</topic><topic>Trichloroethanes - administration & dosage</topic><topic>Trichloroethanes - metabolism</topic><topic>Xenopus laevis</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Beckstead, M J</creatorcontrib><creatorcontrib>Phelan, R</creatorcontrib><creatorcontrib>Mihic, S J</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><jtitle>The Journal of biological chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Beckstead, M J</au><au>Phelan, R</au><au>Mihic, S J</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Antagonism of Inhalant and Volatile Anesthetic Enhancement of Glycine Receptor Function</atitle><jtitle>The Journal of biological chemistry</jtitle><addtitle>J Biol Chem</addtitle><date>2001-07-06</date><risdate>2001</risdate><volume>276</volume><issue>27</issue><spage>24959</spage><epage>24964</epage><pages>24959-24964</pages><issn>0021-9258</issn><eissn>1083-351X</eissn><abstract>Recent studies suggest that alcohols, volatile anesthetics, and inhaled drugs of abuse, which enhance γ-aminobutyric acid,
type A, and glycine receptor-activated ion channel function, may share common or overlapping molecular sites of action on
these receptors. To investigate this possibility, these compounds were applied singly and in combination to wild-type glycine
α 1 receptors expressed in Xenopus laevis oocytes. Data obtained from concentration-response curves of the volatile anesthetic enflurane constructed in the presence
and absence of ethanol, chloroform, or toluene were consistent with competition for a common binding pocket on these receptors.
A mutant glycine receptor, insensitive to the enhancing effects of ethanol but not anesthetics or inhalants, demonstrated
antagonism of anesthetic and inhalant effects on this receptor. Although ethanol (25â200 m m ) had no effect on its own in this receptor, it was able to inhibit reversibly the enhancing effect of enflurane, toluene,
and chloroform in a concentration-dependent manner. These data suggest the existence of overlapping molecular sites of action
for ethanol, inhalants, and volatile anesthetics on glycine receptors and illustrate the feasibility of pharmacological antagonism
of the effects of volatile anesthetics.</abstract><cop>United States</cop><pub>American Society for Biochemistry and Molecular Biology</pub><pmid>11346643</pmid><doi>10.1074/jbc.M011627200</doi><tpages>6</tpages><oa>free_for_read</oa></addata></record> |
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| ispartof | The Journal of biological chemistry, 2001-07, Vol.276 (27), p.24959-24964 |
| issn | 0021-9258 1083-351X |
| language | eng |
| recordid | cdi_crossref_primary_10_1074_jbc_M011627200 |
| source | ScienceDirect (Online service) |
| subjects | Anesthetics, Inhalation - antagonists & inhibitors Animals Binding Sites Chloroform - administration & dosage Chloroform - metabolism Dose-Response Relationship, Drug Drug Interactions Electrophysiology Enflurane - administration & dosage Enflurane - metabolism Ethanol - administration & dosage Ethanol - metabolism Oocytes - drug effects Oocytes - metabolism Receptors, Glycine - drug effects Receptors, Glycine - physiology Toluene - administration & dosage Toluene - metabolism Trichloroethanes - administration & dosage Trichloroethanes - metabolism Xenopus laevis |
| title | Antagonism of Inhalant and Volatile Anesthetic Enhancement of Glycine Receptor Function |
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