New evidence for the selective, long-lasting central effects of the brain-targeted estradiol, Estredox
The present study examined the dose- and time-dependent central effects of an estradiol chemical delivery system cyclodextrin complex (E 2-CDS–CD) on the reestablishment of copulatory behavior of castrated male and ovariectomized female rats with concomitant determination of the blood luteinizing ho...
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| Veröffentlicht in: | Pharmacology, biochemistry and behavior biochemistry and behavior, 2004-03, Vol.77 (3), p.423-429 |
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| container_title | Pharmacology, biochemistry and behavior |
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| creator | Tapfer, Mariann K Sebestyen, Laszlo Kurucz, Istvan Horvath, Katalin Szelenyi, Istvan Bodor, Nicholas |
| description | The present study examined the dose- and time-dependent central effects of an estradiol chemical delivery system cyclodextrin complex (E
2-CDS–CD) on the reestablishment of copulatory behavior of castrated male and ovariectomized female rats with concomitant determination of the blood luteinizing hormone (LH) and E
2 levels. In orchidectomized males, Estredox, after single doses of 0.3 and 3.0 mg/kg iv, reestablished the mounting and intromission up to 4 weeks. The LH suppressive effect lasted to Day 7 and 28, respectively. After repeated administration for 10 days at a dose of 0.01mg/kg iv, significant effect was obtained by Day 14.
Ovariectomized females were treated iv daily for 5 days either with E
2-CDS–CD, estradiol benzoate (EB) or vehicle, and the lordosis quotient was determined. At a dose of 0.03 mg/kg the duration of EB's effect was 10 days shorter and only one-third of that of E
2-CDS–CD. The LH suppression lasted to Day 18. On the other hand, after EB treatment there was no significant decrease in LH levels. The low plasma E
2 levels indicated fast rate of peripheral elimination in both males and females.
The brain-targeting E
2 indicates better efficacy and increased safety in replacement therapies because of the reduced peripheral side effects. |
| doi_str_mv | 10.1016/j.pbb.2003.11.005 |
| format | Article |
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2-CDS–CD) on the reestablishment of copulatory behavior of castrated male and ovariectomized female rats with concomitant determination of the blood luteinizing hormone (LH) and E
2 levels. In orchidectomized males, Estredox, after single doses of 0.3 and 3.0 mg/kg iv, reestablished the mounting and intromission up to 4 weeks. The LH suppressive effect lasted to Day 7 and 28, respectively. After repeated administration for 10 days at a dose of 0.01mg/kg iv, significant effect was obtained by Day 14.
Ovariectomized females were treated iv daily for 5 days either with E
2-CDS–CD, estradiol benzoate (EB) or vehicle, and the lordosis quotient was determined. At a dose of 0.03 mg/kg the duration of EB's effect was 10 days shorter and only one-third of that of E
2-CDS–CD. The LH suppression lasted to Day 18. On the other hand, after EB treatment there was no significant decrease in LH levels. The low plasma E
2 levels indicated fast rate of peripheral elimination in both males and females.
The brain-targeting E
2 indicates better efficacy and increased safety in replacement therapies because of the reduced peripheral side effects.</description><identifier>ISSN: 0091-3057</identifier><identifier>EISSN: 1873-5177</identifier><identifier>DOI: 10.1016/j.pbb.2003.11.005</identifier><identifier>PMID: 15006452</identifier><identifier>CODEN: PBBHAU</identifier><language>eng</language><publisher>New York, NY: Elsevier Inc</publisher><subject>Animals ; Biological and medical sciences ; Brain - drug effects ; Brain - metabolism ; Brain targeting ; Castration ; Central vs. peripheral effect ; Copulatory behavior ; Dose-Response Relationship, Drug ; Estradiol ; Estradiol - analogs & derivatives ; Estradiol - pharmacology ; Female ; Fundamental and applied biological sciences. Psychology ; Lordosis behavior ; Luteinizing Hormone - blood ; Male ; Medical sciences ; Neuropharmacology ; Orchiectomy ; Ovariectomy ; Pharmacology. Drug treatments ; Psychology. Psychoanalysis. Psychiatry ; Psychology. Psychophysiology ; Rats ; Rats, Sprague-Dawley ; Sexual Behavior, Animal - drug effects ; Sexual Behavior, Animal - physiology ; Time</subject><ispartof>Pharmacology, biochemistry and behavior, 2004-03, Vol.77 (3), p.423-429</ispartof><rights>2003</rights><rights>2004 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c410t-50af614b82b796d65bc4393b94bed956915ec05622198e3d03fac567511959293</citedby><cites>FETCH-LOGICAL-c410t-50af614b82b796d65bc4393b94bed956915ec05622198e3d03fac567511959293</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.pbb.2003.11.005$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>315,782,786,3552,27931,27932,46002</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=16008981$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/15006452$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Tapfer, Mariann K</creatorcontrib><creatorcontrib>Sebestyen, Laszlo</creatorcontrib><creatorcontrib>Kurucz, Istvan</creatorcontrib><creatorcontrib>Horvath, Katalin</creatorcontrib><creatorcontrib>Szelenyi, Istvan</creatorcontrib><creatorcontrib>Bodor, Nicholas</creatorcontrib><title>New evidence for the selective, long-lasting central effects of the brain-targeted estradiol, Estredox</title><title>Pharmacology, biochemistry and behavior</title><addtitle>Pharmacol Biochem Behav</addtitle><description>The present study examined the dose- and time-dependent central effects of an estradiol chemical delivery system cyclodextrin complex (E
2-CDS–CD) on the reestablishment of copulatory behavior of castrated male and ovariectomized female rats with concomitant determination of the blood luteinizing hormone (LH) and E
2 levels. In orchidectomized males, Estredox, after single doses of 0.3 and 3.0 mg/kg iv, reestablished the mounting and intromission up to 4 weeks. The LH suppressive effect lasted to Day 7 and 28, respectively. After repeated administration for 10 days at a dose of 0.01mg/kg iv, significant effect was obtained by Day 14.
Ovariectomized females were treated iv daily for 5 days either with E
2-CDS–CD, estradiol benzoate (EB) or vehicle, and the lordosis quotient was determined. At a dose of 0.03 mg/kg the duration of EB's effect was 10 days shorter and only one-third of that of E
2-CDS–CD. The LH suppression lasted to Day 18. On the other hand, after EB treatment there was no significant decrease in LH levels. The low plasma E
2 levels indicated fast rate of peripheral elimination in both males and females.
The brain-targeting E
2 indicates better efficacy and increased safety in replacement therapies because of the reduced peripheral side effects.</description><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Brain - drug effects</subject><subject>Brain - metabolism</subject><subject>Brain targeting</subject><subject>Castration</subject><subject>Central vs. peripheral effect</subject><subject>Copulatory behavior</subject><subject>Dose-Response Relationship, Drug</subject><subject>Estradiol</subject><subject>Estradiol - analogs & derivatives</subject><subject>Estradiol - pharmacology</subject><subject>Female</subject><subject>Fundamental and applied biological sciences. Psychology</subject><subject>Lordosis behavior</subject><subject>Luteinizing Hormone - blood</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Neuropharmacology</subject><subject>Orchiectomy</subject><subject>Ovariectomy</subject><subject>Pharmacology. Drug treatments</subject><subject>Psychology. Psychoanalysis. Psychiatry</subject><subject>Psychology. Psychophysiology</subject><subject>Rats</subject><subject>Rats, Sprague-Dawley</subject><subject>Sexual Behavior, Animal - drug effects</subject><subject>Sexual Behavior, Animal - physiology</subject><subject>Time</subject><issn>0091-3057</issn><issn>1873-5177</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2004</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkU2P0zAQQC0EYrsLP4AL8gVOmzCTxHYsTqvVsiCt4AJny7HHxVWaFDst8O9xaaW9wWlGmjcfmsfYK4QaAeW7Tb0bhroBaGvEGkA8YSvsVVsJVOopWwForFoQ6oJd5rwBgK6R6jm7QAEgO9GsWPhMPzkdoqfJEQ9z4st34plGcks80DUf52ldjTYvcVpzR9OS7MgphFLPfA5_8SHZOFWLTWtayHPKBfJxHq_5XUnJz79esGfBjplenuMV-_bh7uvtx-rhy_2n25uHynUISyXABond0DeD0tJLMbiu1e2gu4G8FlKjIAdCNg3qnloPbbBOSCUQtdCNbq_Y29PcXZp_7MshZhuzo3G0E837bBQqbDTCf0FUfa91jwXEE-jSnHOiYHYpbm36bRDM0YLZmGLBHC0YRFMslJ7X5-H7YUv-seP89gK8OQM2OzuGZCcX8yMnAfrT8vcnjsrPDpGSyS4eTfmYigDj5_iPM_4A8nOjsA</recordid><startdate>20040301</startdate><enddate>20040301</enddate><creator>Tapfer, Mariann K</creator><creator>Sebestyen, Laszlo</creator><creator>Kurucz, Istvan</creator><creator>Horvath, Katalin</creator><creator>Szelenyi, Istvan</creator><creator>Bodor, Nicholas</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>7X8</scope></search><sort><creationdate>20040301</creationdate><title>New evidence for the selective, long-lasting central effects of the brain-targeted estradiol, Estredox</title><author>Tapfer, Mariann K ; Sebestyen, Laszlo ; Kurucz, Istvan ; Horvath, Katalin ; Szelenyi, Istvan ; Bodor, Nicholas</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c410t-50af614b82b796d65bc4393b94bed956915ec05622198e3d03fac567511959293</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2004</creationdate><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Brain - drug effects</topic><topic>Brain - metabolism</topic><topic>Brain targeting</topic><topic>Castration</topic><topic>Central vs. peripheral effect</topic><topic>Copulatory behavior</topic><topic>Dose-Response Relationship, Drug</topic><topic>Estradiol</topic><topic>Estradiol - analogs & derivatives</topic><topic>Estradiol - pharmacology</topic><topic>Female</topic><topic>Fundamental and applied biological sciences. Psychology</topic><topic>Lordosis behavior</topic><topic>Luteinizing Hormone - blood</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Neuropharmacology</topic><topic>Orchiectomy</topic><topic>Ovariectomy</topic><topic>Pharmacology. Drug treatments</topic><topic>Psychology. Psychoanalysis. Psychiatry</topic><topic>Psychology. Psychophysiology</topic><topic>Rats</topic><topic>Rats, Sprague-Dawley</topic><topic>Sexual Behavior, Animal - drug effects</topic><topic>Sexual Behavior, Animal - physiology</topic><topic>Time</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Tapfer, Mariann K</creatorcontrib><creatorcontrib>Sebestyen, Laszlo</creatorcontrib><creatorcontrib>Kurucz, Istvan</creatorcontrib><creatorcontrib>Horvath, Katalin</creatorcontrib><creatorcontrib>Szelenyi, Istvan</creatorcontrib><creatorcontrib>Bodor, Nicholas</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>MEDLINE - Academic</collection><jtitle>Pharmacology, biochemistry and behavior</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Tapfer, Mariann K</au><au>Sebestyen, Laszlo</au><au>Kurucz, Istvan</au><au>Horvath, Katalin</au><au>Szelenyi, Istvan</au><au>Bodor, Nicholas</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>New evidence for the selective, long-lasting central effects of the brain-targeted estradiol, Estredox</atitle><jtitle>Pharmacology, biochemistry and behavior</jtitle><addtitle>Pharmacol Biochem Behav</addtitle><date>2004-03-01</date><risdate>2004</risdate><volume>77</volume><issue>3</issue><spage>423</spage><epage>429</epage><pages>423-429</pages><issn>0091-3057</issn><eissn>1873-5177</eissn><coden>PBBHAU</coden><abstract>The present study examined the dose- and time-dependent central effects of an estradiol chemical delivery system cyclodextrin complex (E
2-CDS–CD) on the reestablishment of copulatory behavior of castrated male and ovariectomized female rats with concomitant determination of the blood luteinizing hormone (LH) and E
2 levels. In orchidectomized males, Estredox, after single doses of 0.3 and 3.0 mg/kg iv, reestablished the mounting and intromission up to 4 weeks. The LH suppressive effect lasted to Day 7 and 28, respectively. After repeated administration for 10 days at a dose of 0.01mg/kg iv, significant effect was obtained by Day 14.
Ovariectomized females were treated iv daily for 5 days either with E
2-CDS–CD, estradiol benzoate (EB) or vehicle, and the lordosis quotient was determined. At a dose of 0.03 mg/kg the duration of EB's effect was 10 days shorter and only one-third of that of E
2-CDS–CD. The LH suppression lasted to Day 18. On the other hand, after EB treatment there was no significant decrease in LH levels. The low plasma E
2 levels indicated fast rate of peripheral elimination in both males and females.
The brain-targeting E
2 indicates better efficacy and increased safety in replacement therapies because of the reduced peripheral side effects.</abstract><cop>New York, NY</cop><pub>Elsevier Inc</pub><pmid>15006452</pmid><doi>10.1016/j.pbb.2003.11.005</doi><tpages>7</tpages></addata></record> |
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| ispartof | Pharmacology, biochemistry and behavior, 2004-03, Vol.77 (3), p.423-429 |
| issn | 0091-3057 1873-5177 |
| language | eng |
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| source | MEDLINE; Access via ScienceDirect (Elsevier) |
| subjects | Animals Biological and medical sciences Brain - drug effects Brain - metabolism Brain targeting Castration Central vs. peripheral effect Copulatory behavior Dose-Response Relationship, Drug Estradiol Estradiol - analogs & derivatives Estradiol - pharmacology Female Fundamental and applied biological sciences. Psychology Lordosis behavior Luteinizing Hormone - blood Male Medical sciences Neuropharmacology Orchiectomy Ovariectomy Pharmacology. Drug treatments Psychology. Psychoanalysis. Psychiatry Psychology. Psychophysiology Rats Rats, Sprague-Dawley Sexual Behavior, Animal - drug effects Sexual Behavior, Animal - physiology Time |
| title | New evidence for the selective, long-lasting central effects of the brain-targeted estradiol, Estredox |
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