Pharmacological Properties of the Enantiomers of Idazoxan: Possible Separation between their Alpha-Adrenoceptor Blocking Effects
The alpha-adrenoceptor blocking properties of the two enantiomers of idazoxan have been investigated in rats, dogs and chicks, as well as their agonistic effects in pithed rats. At peripheral sites, (+) idazoxan was equipotent for blocking both postsynaptic alpha-1 and alpha-2 adrenoceptors of the r...
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| Veröffentlicht in: | Clinical and experimental hypertension (1993) 1986, Vol.A8 (3), p.387-409 |
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| container_title | Clinical and experimental hypertension (1993) |
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| creator | Dabire, Hubert Dausse, Jean-Pierre Mouille, Paule Fournier, Berthe Cardot, Alain Meyer, Philippe Schmitt, Henri |
| description | The alpha-adrenoceptor blocking properties of the two enantiomers of idazoxan have been investigated in rats, dogs and chicks, as well as their agonistic effects in pithed rats. At peripheral sites, (+) idazoxan was equipotent for blocking both postsynaptic alpha-1 and alpha-2 adrenoceptors of the rat and revealed to be a potent antagonist at presynaptic sites of rats and dogs. (−) Idazoxan revealed to be selective for postsynaptic alpha-2 adrenoceptors with an apparent selectivity ratio of about 10. This selectivity of (−) idazoxan was greater in vitro (−) Idazoxan also antagonized presynaptic alpha-2 adrenoceptors of rats and dogs. At central sites, (+) and (−) idazoxan antagonized the hypotension, bradycardia, inhibition of sympathetic nerve activity induced by clonidine in rats and dogs and sedation induced by clonidine and azepexole in chicks. Although (+) idazoxan was more potent than (−) idazoxan, binding studies revealed (−) idazoxan to be more selective than (+) idazoxan at central sites. It is concluded that (+) idazoxan antagonizes both alpha-1 and alpha-2 adrenoceptors and (−) idazoxan is selective for alpha-2 adrenoceptors. In the pithed rat, only (−) idazoxan possesses both alpha-1 and alpha-2 agonistic effects. These results show little differences between the two enantiomers of idazoxan as for those of imidazoline derivatives |
| doi_str_mv | 10.3109/10641968609039612 |
| format | Article |
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At peripheral sites, (+) idazoxan was equipotent for blocking both postsynaptic alpha-1 and alpha-2 adrenoceptors of the rat and revealed to be a potent antagonist at presynaptic sites of rats and dogs. (−) Idazoxan revealed to be selective for postsynaptic alpha-2 adrenoceptors with an apparent selectivity ratio of about 10. This selectivity of (−) idazoxan was greater in vitro (−) Idazoxan also antagonized presynaptic alpha-2 adrenoceptors of rats and dogs. At central sites, (+) and (−) idazoxan antagonized the hypotension, bradycardia, inhibition of sympathetic nerve activity induced by clonidine in rats and dogs and sedation induced by clonidine and azepexole in chicks. Although (+) idazoxan was more potent than (−) idazoxan, binding studies revealed (−) idazoxan to be more selective than (+) idazoxan at central sites. It is concluded that (+) idazoxan antagonizes both alpha-1 and alpha-2 adrenoceptors and (−) idazoxan is selective for alpha-2 adrenoceptors. In the pithed rat, only (−) idazoxan possesses both alpha-1 and alpha-2 agonistic effects. These results show little differences between the two enantiomers of idazoxan as for those of imidazoline derivatives</description><identifier>ISSN: 1064-1963</identifier><identifier>ISSN: 0730-0077</identifier><identifier>EISSN: 1525-6006</identifier><identifier>DOI: 10.3109/10641968609039612</identifier><identifier>PMID: 2873908</identifier><identifier>CODEN: CEHADM</identifier><language>eng</language><publisher>Basel: Informa UK Ltd</publisher><subject>Adrenergic alpha-Antagonists - pharmacology ; agonistic effects ; Animals ; Binding, Competitive ; Biological and medical sciences ; Blood Pressure - drug effects ; Cardiovascular system ; central alpha2 adrenoceptors ; Cerebral Cortex - drug effects ; Chickens ; Clonidine - pharmacology ; Decerebrate State ; Dioxanes - pharmacology ; Dioxins - pharmacology ; Dogs ; Electric Stimulation ; enantiomers ; Female ; Heart Rate - drug effects ; Hypnotics and Sedatives - pharmacology ; Idazoxan ; Isomerism ; Male ; Medical sciences ; Miscellaneous ; Neural Inhibition - drug effects ; peripheral alphal and alpha2 adrenoceptors ; Pharmacology. Drug treatments ; Rats ; Rats, Inbred Strains ; Receptors, Adrenergic, alpha - drug effects ; Synapses - physiology ; Tachycardia - chemically induced</subject><ispartof>Clinical and experimental hypertension (1993), 1986, Vol.A8 (3), p.387-409</ispartof><rights>1986 Informa UK Ltd All rights reserved: reproduction in whole or part not permitted 1986</rights><rights>1987 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c430t-d2322b7d90baaccfacf0966a4459b86a01d4e5a3a884182fe41f8b19175f810a3</citedby><cites>FETCH-LOGICAL-c430t-d2322b7d90baaccfacf0966a4459b86a01d4e5a3a884182fe41f8b19175f810a3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.tandfonline.com/doi/pdf/10.3109/10641968609039612$$EPDF$$P50$$Ginformahealthcare$$H</linktopdf><linktohtml>$$Uhttps://www.tandfonline.com/doi/full/10.3109/10641968609039612$$EHTML$$P50$$Ginformahealthcare$$H</linktohtml><link.rule.ids>314,776,780,4010,27900,27901,27902,59620,60409,61194,61375</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=8071514$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/2873908$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Dabire, Hubert</creatorcontrib><creatorcontrib>Dausse, Jean-Pierre</creatorcontrib><creatorcontrib>Mouille, Paule</creatorcontrib><creatorcontrib>Fournier, Berthe</creatorcontrib><creatorcontrib>Cardot, Alain</creatorcontrib><creatorcontrib>Meyer, Philippe</creatorcontrib><creatorcontrib>Schmitt, Henri</creatorcontrib><title>Pharmacological Properties of the Enantiomers of Idazoxan: Possible Separation between their Alpha-Adrenoceptor Blocking Effects</title><title>Clinical and experimental hypertension (1993)</title><addtitle>Clin Exp Hypertens A</addtitle><description>The alpha-adrenoceptor blocking properties of the two enantiomers of idazoxan have been investigated in rats, dogs and chicks, as well as their agonistic effects in pithed rats. At peripheral sites, (+) idazoxan was equipotent for blocking both postsynaptic alpha-1 and alpha-2 adrenoceptors of the rat and revealed to be a potent antagonist at presynaptic sites of rats and dogs. (−) Idazoxan revealed to be selective for postsynaptic alpha-2 adrenoceptors with an apparent selectivity ratio of about 10. This selectivity of (−) idazoxan was greater in vitro (−) Idazoxan also antagonized presynaptic alpha-2 adrenoceptors of rats and dogs. At central sites, (+) and (−) idazoxan antagonized the hypotension, bradycardia, inhibition of sympathetic nerve activity induced by clonidine in rats and dogs and sedation induced by clonidine and azepexole in chicks. Although (+) idazoxan was more potent than (−) idazoxan, binding studies revealed (−) idazoxan to be more selective than (+) idazoxan at central sites. It is concluded that (+) idazoxan antagonizes both alpha-1 and alpha-2 adrenoceptors and (−) idazoxan is selective for alpha-2 adrenoceptors. In the pithed rat, only (−) idazoxan possesses both alpha-1 and alpha-2 agonistic effects. These results show little differences between the two enantiomers of idazoxan as for those of imidazoline derivatives</description><subject>Adrenergic alpha-Antagonists - pharmacology</subject><subject>agonistic effects</subject><subject>Animals</subject><subject>Binding, Competitive</subject><subject>Biological and medical sciences</subject><subject>Blood Pressure - drug effects</subject><subject>Cardiovascular system</subject><subject>central alpha2 adrenoceptors</subject><subject>Cerebral Cortex - drug effects</subject><subject>Chickens</subject><subject>Clonidine - pharmacology</subject><subject>Decerebrate State</subject><subject>Dioxanes - pharmacology</subject><subject>Dioxins - pharmacology</subject><subject>Dogs</subject><subject>Electric Stimulation</subject><subject>enantiomers</subject><subject>Female</subject><subject>Heart Rate - drug effects</subject><subject>Hypnotics and Sedatives - pharmacology</subject><subject>Idazoxan</subject><subject>Isomerism</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Miscellaneous</subject><subject>Neural Inhibition - drug effects</subject><subject>peripheral alphal and alpha2 adrenoceptors</subject><subject>Pharmacology. Drug treatments</subject><subject>Rats</subject><subject>Rats, Inbred Strains</subject><subject>Receptors, Adrenergic, alpha - drug effects</subject><subject>Synapses - physiology</subject><subject>Tachycardia - chemically induced</subject><issn>1064-1963</issn><issn>0730-0077</issn><issn>1525-6006</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1986</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kEFvFCEYhonR1Fr9AR5MOHgdhYFhGfWyNqs2aeIm6nnyDfPRobIwAZpaT_50qbs2MSY9QXjfh3zfQ8hzzl4JzvrXnCnJe6UV65noFW8fkGPetV2jGFMP673mTS2Ix-RJzpeMcak6fUSOWr0SPdPH5Nd2hrQDE328cAY83aa4YCoOM42WlhnpJkAoLu4w_Xk6m-Bn_AHhDd3GnN3okX7BBRLUTqAjlmvEcAu6RNd-maFZTwlDNLiUmOh7H813Fy7oxlo0JT8ljyz4jM8O5wn59mHz9fRTc_7549np-rwxUrDSTK1o23E19WwEMMaCsaxXCqTs-lErYHyS2IEArSXXrUXJrR55z1ed1ZyBOCF8_69JdeyEdliS20G6GTgbbmUO_8mszIs9s1yNO5zuiIO9mr885JCrO5sgGJfvapqteMdlrb3b11ywscq-jslPQ4EbH9NfRtw3xdt_8BnBl9lAwuEyXqVQrd2zw2-GH6Ow</recordid><startdate>1986</startdate><enddate>1986</enddate><creator>Dabire, Hubert</creator><creator>Dausse, Jean-Pierre</creator><creator>Mouille, Paule</creator><creator>Fournier, Berthe</creator><creator>Cardot, Alain</creator><creator>Meyer, Philippe</creator><creator>Schmitt, Henri</creator><general>Informa UK Ltd</general><general>Taylor & Francis</general><general>Dekker</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></search><sort><creationdate>1986</creationdate><title>Pharmacological Properties of the Enantiomers of Idazoxan: Possible Separation between their Alpha-Adrenoceptor Blocking Effects</title><author>Dabire, Hubert ; Dausse, Jean-Pierre ; Mouille, Paule ; Fournier, Berthe ; Cardot, Alain ; Meyer, Philippe ; Schmitt, Henri</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c430t-d2322b7d90baaccfacf0966a4459b86a01d4e5a3a884182fe41f8b19175f810a3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1986</creationdate><topic>Adrenergic alpha-Antagonists - pharmacology</topic><topic>agonistic effects</topic><topic>Animals</topic><topic>Binding, Competitive</topic><topic>Biological and medical sciences</topic><topic>Blood Pressure - drug effects</topic><topic>Cardiovascular system</topic><topic>central alpha2 adrenoceptors</topic><topic>Cerebral Cortex - drug effects</topic><topic>Chickens</topic><topic>Clonidine - pharmacology</topic><topic>Decerebrate State</topic><topic>Dioxanes - pharmacology</topic><topic>Dioxins - pharmacology</topic><topic>Dogs</topic><topic>Electric Stimulation</topic><topic>enantiomers</topic><topic>Female</topic><topic>Heart Rate - drug effects</topic><topic>Hypnotics and Sedatives - pharmacology</topic><topic>Idazoxan</topic><topic>Isomerism</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Miscellaneous</topic><topic>Neural Inhibition - drug effects</topic><topic>peripheral alphal and alpha2 adrenoceptors</topic><topic>Pharmacology. Drug treatments</topic><topic>Rats</topic><topic>Rats, Inbred Strains</topic><topic>Receptors, Adrenergic, alpha - drug effects</topic><topic>Synapses - physiology</topic><topic>Tachycardia - chemically induced</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Dabire, Hubert</creatorcontrib><creatorcontrib>Dausse, Jean-Pierre</creatorcontrib><creatorcontrib>Mouille, Paule</creatorcontrib><creatorcontrib>Fournier, Berthe</creatorcontrib><creatorcontrib>Cardot, Alain</creatorcontrib><creatorcontrib>Meyer, Philippe</creatorcontrib><creatorcontrib>Schmitt, Henri</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><jtitle>Clinical and experimental hypertension (1993)</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Dabire, Hubert</au><au>Dausse, Jean-Pierre</au><au>Mouille, Paule</au><au>Fournier, Berthe</au><au>Cardot, Alain</au><au>Meyer, Philippe</au><au>Schmitt, Henri</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Pharmacological Properties of the Enantiomers of Idazoxan: Possible Separation between their Alpha-Adrenoceptor Blocking Effects</atitle><jtitle>Clinical and experimental hypertension (1993)</jtitle><addtitle>Clin Exp Hypertens A</addtitle><date>1986</date><risdate>1986</risdate><volume>A8</volume><issue>3</issue><spage>387</spage><epage>409</epage><pages>387-409</pages><issn>1064-1963</issn><issn>0730-0077</issn><eissn>1525-6006</eissn><coden>CEHADM</coden><abstract>The alpha-adrenoceptor blocking properties of the two enantiomers of idazoxan have been investigated in rats, dogs and chicks, as well as their agonistic effects in pithed rats. At peripheral sites, (+) idazoxan was equipotent for blocking both postsynaptic alpha-1 and alpha-2 adrenoceptors of the rat and revealed to be a potent antagonist at presynaptic sites of rats and dogs. (−) Idazoxan revealed to be selective for postsynaptic alpha-2 adrenoceptors with an apparent selectivity ratio of about 10. This selectivity of (−) idazoxan was greater in vitro (−) Idazoxan also antagonized presynaptic alpha-2 adrenoceptors of rats and dogs. At central sites, (+) and (−) idazoxan antagonized the hypotension, bradycardia, inhibition of sympathetic nerve activity induced by clonidine in rats and dogs and sedation induced by clonidine and azepexole in chicks. Although (+) idazoxan was more potent than (−) idazoxan, binding studies revealed (−) idazoxan to be more selective than (+) idazoxan at central sites. It is concluded that (+) idazoxan antagonizes both alpha-1 and alpha-2 adrenoceptors and (−) idazoxan is selective for alpha-2 adrenoceptors. 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| fulltext | fulltext |
| identifier | ISSN: 1064-1963 |
| ispartof | Clinical and experimental hypertension (1993), 1986, Vol.A8 (3), p.387-409 |
| issn | 1064-1963 0730-0077 1525-6006 |
| language | eng |
| recordid | cdi_crossref_primary_10_3109_10641968609039612 |
| source | MEDLINE; Taylor & Francis Journals Complete |
| subjects | Adrenergic alpha-Antagonists - pharmacology agonistic effects Animals Binding, Competitive Biological and medical sciences Blood Pressure - drug effects Cardiovascular system central alpha2 adrenoceptors Cerebral Cortex - drug effects Chickens Clonidine - pharmacology Decerebrate State Dioxanes - pharmacology Dioxins - pharmacology Dogs Electric Stimulation enantiomers Female Heart Rate - drug effects Hypnotics and Sedatives - pharmacology Idazoxan Isomerism Male Medical sciences Miscellaneous Neural Inhibition - drug effects peripheral alphal and alpha2 adrenoceptors Pharmacology. Drug treatments Rats Rats, Inbred Strains Receptors, Adrenergic, alpha - drug effects Synapses - physiology Tachycardia - chemically induced |
| title | Pharmacological Properties of the Enantiomers of Idazoxan: Possible Separation between their Alpha-Adrenoceptor Blocking Effects |
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