Development of Tolerance in Mice to the Sedative Effects of the Neuroactive Steroid Minaxolone Following Chronic Exposure
Minaxolone is a potent ligand for the neurosteroid binding site of the GABA A receptor. In radioligand binding studies to rat brain membranes, minaxolone caused a 69% increase in [ 3H]muscimol binding and a 25% increase in [ 3H]flunitrazepam binding and inhibited the binding of [ 3H]TBOB with an IC...
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| Veröffentlicht in: | Pharmacology, biochemistry and behavior biochemistry and behavior, 1997-09, Vol.58 (1), p.1-8 |
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| creator | Marshall, Fiona H Stratton, Sharon C Mullings, Joanne Ford, Elaine Worton, Stella P Oakley, Nigel R Hagan, Russell M |
| description | Minaxolone is a potent ligand for the neurosteroid binding site of the GABA
A receptor. In radioligand binding studies to rat brain membranes, minaxolone caused a 69% increase in [
3H]muscimol binding and a 25% increase in [
3H]flunitrazepam binding and inhibited the binding of [
3H]TBOB with an IC
50 of 1 μM. In mice, minaxolone (100 mg/kg, orally) had marked sedative effects as indicated by a reduction in locomotor activity. Chronic dosing with minaxolone (100 mg/kg, orally, once daily for 7 days) resulted in a loss of sedative response to an acute dose of the drug, indicating the development of tolerance. Chronic dosing with temazepam (10 mg/kg, orally, once daily for 7 days) resulted in the development of tolerance to an acute dose of temazepam; however, the two drugs did not appear to be cross-tolerant, indicating that they may have a different mechanism of action at the level of the GABA
A receptor. |
| doi_str_mv | 10.1016/S0091-3057(96)00132-3 |
| format | Article |
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A receptor. In radioligand binding studies to rat brain membranes, minaxolone caused a 69% increase in [
3H]muscimol binding and a 25% increase in [
3H]flunitrazepam binding and inhibited the binding of [
3H]TBOB with an IC
50 of 1 μM. In mice, minaxolone (100 mg/kg, orally) had marked sedative effects as indicated by a reduction in locomotor activity. Chronic dosing with minaxolone (100 mg/kg, orally, once daily for 7 days) resulted in a loss of sedative response to an acute dose of the drug, indicating the development of tolerance. Chronic dosing with temazepam (10 mg/kg, orally, once daily for 7 days) resulted in the development of tolerance to an acute dose of temazepam; however, the two drugs did not appear to be cross-tolerant, indicating that they may have a different mechanism of action at the level of the GABA
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A receptor. In radioligand binding studies to rat brain membranes, minaxolone caused a 69% increase in [
3H]muscimol binding and a 25% increase in [
3H]flunitrazepam binding and inhibited the binding of [
3H]TBOB with an IC
50 of 1 μM. In mice, minaxolone (100 mg/kg, orally) had marked sedative effects as indicated by a reduction in locomotor activity. Chronic dosing with minaxolone (100 mg/kg, orally, once daily for 7 days) resulted in a loss of sedative response to an acute dose of the drug, indicating the development of tolerance. Chronic dosing with temazepam (10 mg/kg, orally, once daily for 7 days) resulted in the development of tolerance to an acute dose of temazepam; however, the two drugs did not appear to be cross-tolerant, indicating that they may have a different mechanism of action at the level of the GABA
A receptor.</description><subject>Anesthetics - pharmacology</subject><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Dose-Response Relationship, Drug</subject><subject>Drug Tolerance</subject><subject>Flunitrazepam - metabolism</subject><subject>Flunitrazepam - pharmacology</subject><subject>GABA</subject><subject>GABA A receptor</subject><subject>GABA Agonists - metabolism</subject><subject>GABA Modulators - metabolism</subject><subject>GABA Modulators - pharmacology</subject><subject>GABA-A Receptor Antagonists</subject><subject>Hypnotics and Sedatives - pharmacology</subject><subject>Hypnotics. Sedatives</subject><subject>In Vitro Techniques</subject><subject>Locomotor activity Mice</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Membranes - metabolism</subject><subject>Mice</subject><subject>Mice, Inbred Strains</subject><subject>Minaxolone</subject><subject>Motor Activity - drug effects</subject><subject>Muscimol - metabolism</subject><subject>Neuropharmacology</subject><subject>Neurosteroid</subject><subject>Pharmacology. Drug treatments</subject><subject>Pregnanolone - analogs & derivatives</subject><subject>Pregnanolone - pharmacology</subject><subject>Psychology. Psychoanalysis. Psychiatry</subject><subject>Psychopharmacology</subject><subject>Radioligand Assay</subject><subject>Rats</subject><subject>Temazepam</subject><subject>Temazepam - metabolism</subject><subject>Temazepam - pharmacology</subject><subject>Tolerance</subject><issn>0091-3057</issn><issn>1873-5177</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1997</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkc1uEzEURi0EKqHwCJW8QAgWA_4bG69QFdKCVGCRsrY89jU1csbBngnt23cmibLt6kr-zmdb9yB0QclHSqj8tCZE04aTVr3X8gMhlLOGP0ML-lnxpqVKPUeLE_ISvar1LyFEMKnO0JlmUhDJFujhK-wg5e0G-gHngG9zgmJ7Bzj2-Eec5pDxcAd4Dd4OcQd4FQK4oc7wfP4TxpKt20frAUqOfur19j6n3AO-yinl_7H_g5d3JffR4dX9NtexwGv0IthU4c1xnqPfV6vb5bfm5tf19-XlTeMEI0PTeasF9dq1AK3zXAROiQhMORu0ZZbIjlkanFVCECVZJ0E50nmvWVCttvwcvTvcuy353wh1MJtYHaRke8hjNUozJiljT4JUUcYFncH2ALqSay0QzLbEjS0PhhIzuzF7N2ZevNHS7N0YPvUujg-M3Qb8qXWUMeVvj7mtzqYwe4j1hDE6WeViwr4cMJi2totQTHURJmU-lsmM8Tk-8ZFHwaGsZw</recordid><startdate>19970901</startdate><enddate>19970901</enddate><creator>Marshall, Fiona H</creator><creator>Stratton, Sharon C</creator><creator>Mullings, Joanne</creator><creator>Ford, Elaine</creator><creator>Worton, Stella P</creator><creator>Oakley, Nigel R</creator><creator>Hagan, Russell M</creator><general>Elsevier Inc</general><general>Elsevier Science</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>7QG</scope><scope>7TK</scope><scope>7X8</scope></search><sort><creationdate>19970901</creationdate><title>Development of Tolerance in Mice to the Sedative Effects of the Neuroactive Steroid Minaxolone Following Chronic Exposure</title><author>Marshall, Fiona H ; Stratton, Sharon C ; Mullings, Joanne ; Ford, Elaine ; Worton, Stella P ; Oakley, Nigel R ; Hagan, Russell M</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c420t-bda941d9c5ee5cd34f3104f27caf9a2a06b2a1fca7440762b6e7c0bdd92f759a3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1997</creationdate><topic>Anesthetics - pharmacology</topic><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Dose-Response Relationship, Drug</topic><topic>Drug Tolerance</topic><topic>Flunitrazepam - metabolism</topic><topic>Flunitrazepam - pharmacology</topic><topic>GABA</topic><topic>GABA A receptor</topic><topic>GABA Agonists - metabolism</topic><topic>GABA Modulators - metabolism</topic><topic>GABA Modulators - pharmacology</topic><topic>GABA-A Receptor Antagonists</topic><topic>Hypnotics and Sedatives - pharmacology</topic><topic>Hypnotics. Sedatives</topic><topic>In Vitro Techniques</topic><topic>Locomotor activity Mice</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Membranes - metabolism</topic><topic>Mice</topic><topic>Mice, Inbred Strains</topic><topic>Minaxolone</topic><topic>Motor Activity - drug effects</topic><topic>Muscimol - metabolism</topic><topic>Neuropharmacology</topic><topic>Neurosteroid</topic><topic>Pharmacology. Drug treatments</topic><topic>Pregnanolone - analogs & derivatives</topic><topic>Pregnanolone - pharmacology</topic><topic>Psychology. Psychoanalysis. Psychiatry</topic><topic>Psychopharmacology</topic><topic>Radioligand Assay</topic><topic>Rats</topic><topic>Temazepam</topic><topic>Temazepam - metabolism</topic><topic>Temazepam - pharmacology</topic><topic>Tolerance</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Marshall, Fiona H</creatorcontrib><creatorcontrib>Stratton, Sharon C</creatorcontrib><creatorcontrib>Mullings, Joanne</creatorcontrib><creatorcontrib>Ford, Elaine</creatorcontrib><creatorcontrib>Worton, Stella P</creatorcontrib><creatorcontrib>Oakley, Nigel R</creatorcontrib><creatorcontrib>Hagan, Russell M</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>Animal Behavior Abstracts</collection><collection>Neurosciences Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Pharmacology, biochemistry and behavior</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Marshall, Fiona H</au><au>Stratton, Sharon C</au><au>Mullings, Joanne</au><au>Ford, Elaine</au><au>Worton, Stella P</au><au>Oakley, Nigel R</au><au>Hagan, Russell M</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Development of Tolerance in Mice to the Sedative Effects of the Neuroactive Steroid Minaxolone Following Chronic Exposure</atitle><jtitle>Pharmacology, biochemistry and behavior</jtitle><addtitle>Pharmacol Biochem Behav</addtitle><date>1997-09-01</date><risdate>1997</risdate><volume>58</volume><issue>1</issue><spage>1</spage><epage>8</epage><pages>1-8</pages><issn>0091-3057</issn><eissn>1873-5177</eissn><coden>PBBHAU</coden><abstract>Minaxolone is a potent ligand for the neurosteroid binding site of the GABA
A receptor. In radioligand binding studies to rat brain membranes, minaxolone caused a 69% increase in [
3H]muscimol binding and a 25% increase in [
3H]flunitrazepam binding and inhibited the binding of [
3H]TBOB with an IC
50 of 1 μM. In mice, minaxolone (100 mg/kg, orally) had marked sedative effects as indicated by a reduction in locomotor activity. Chronic dosing with minaxolone (100 mg/kg, orally, once daily for 7 days) resulted in a loss of sedative response to an acute dose of the drug, indicating the development of tolerance. Chronic dosing with temazepam (10 mg/kg, orally, once daily for 7 days) resulted in the development of tolerance to an acute dose of temazepam; however, the two drugs did not appear to be cross-tolerant, indicating that they may have a different mechanism of action at the level of the GABA
A receptor.</abstract><cop>New York, NY</cop><pub>Elsevier Inc</pub><pmid>9264062</pmid><doi>10.1016/S0091-3057(96)00132-3</doi><tpages>8</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0091-3057 |
| ispartof | Pharmacology, biochemistry and behavior, 1997-09, Vol.58 (1), p.1-8 |
| issn | 0091-3057 1873-5177 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_79226122 |
| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Anesthetics - pharmacology Animals Biological and medical sciences Dose-Response Relationship, Drug Drug Tolerance Flunitrazepam - metabolism Flunitrazepam - pharmacology GABA GABA A receptor GABA Agonists - metabolism GABA Modulators - metabolism GABA Modulators - pharmacology GABA-A Receptor Antagonists Hypnotics and Sedatives - pharmacology Hypnotics. Sedatives In Vitro Techniques Locomotor activity Mice Male Medical sciences Membranes - metabolism Mice Mice, Inbred Strains Minaxolone Motor Activity - drug effects Muscimol - metabolism Neuropharmacology Neurosteroid Pharmacology. Drug treatments Pregnanolone - analogs & derivatives Pregnanolone - pharmacology Psychology. Psychoanalysis. Psychiatry Psychopharmacology Radioligand Assay Rats Temazepam Temazepam - metabolism Temazepam - pharmacology Tolerance |
| title | Development of Tolerance in Mice to the Sedative Effects of the Neuroactive Steroid Minaxolone Following Chronic Exposure |
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