Dose determination of haloperidol, risperidone and olanzapine using an in vivo dopamine D2-receptor occupancy method in the rat
The purpose of the present study was to determine antipsychotic doses that achieve 80% striatal dopamine D2-receptor occupancy for haloperidol, risperidone and olanzapine in rats. Wistar rats were treated with normal saline vehicle (controls), haloperidol (0.25 and 0.5 mg/kg/day), risperidone (3, 5...
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| Veröffentlicht in: | European journal of pharmacology 2006-07, Vol.540 (1-3), p.87-90 |
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| container_title | European journal of pharmacology |
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| creator | NAIKER, Dineshree V CARTS, Stanley V CATTS, Vibeke S BEDI, Kuldip S BRYAN-LLUKA, Lesley J |
| description | The purpose of the present study was to determine antipsychotic doses that achieve 80% striatal dopamine D2-receptor occupancy for haloperidol, risperidone and olanzapine in rats. Wistar rats were treated with normal saline vehicle (controls), haloperidol (0.25 and 0.5 mg/kg/day), risperidone (3, 5 and 6 mg/kg/day) and olanzapine (5 and 10 mg/kg/day) for 7 days via osmotic minipumps. Striatal and cerebellar tissue were collected and in vivo dopamine D2-receptor occupancies were determined using 3H-raclopride. The doses required to achieve dopamine D2-receptor occupancy of 80% in 11- and 24-week old rats were: haloperidol 0.25 mg/kg/day, risperidone 5 mg/kg/day and olanzapine 10 mg/kg/day. |
| doi_str_mv | 10.1016/j.ejphar.2006.04.048 |
| format | Article |
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Wistar rats were treated with normal saline vehicle (controls), haloperidol (0.25 and 0.5 mg/kg/day), risperidone (3, 5 and 6 mg/kg/day) and olanzapine (5 and 10 mg/kg/day) for 7 days via osmotic minipumps. Striatal and cerebellar tissue were collected and in vivo dopamine D2-receptor occupancies were determined using 3H-raclopride. 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Wistar rats were treated with normal saline vehicle (controls), haloperidol (0.25 and 0.5 mg/kg/day), risperidone (3, 5 and 6 mg/kg/day) and olanzapine (5 and 10 mg/kg/day) for 7 days via osmotic minipumps. Striatal and cerebellar tissue were collected and in vivo dopamine D2-receptor occupancies were determined using 3H-raclopride. The doses required to achieve dopamine D2-receptor occupancy of 80% in 11- and 24-week old rats were: haloperidol 0.25 mg/kg/day, risperidone 5 mg/kg/day and olanzapine 10 mg/kg/day.</description><subject>Algorithms</subject><subject>Analysis of Variance</subject><subject>Animals</subject><subject>Antipsychotic Agents - administration & dosage</subject><subject>Benzodiazepines - administration & dosage</subject><subject>Binding, Competitive - drug effects</subject><subject>Biological and medical sciences</subject><subject>Cerebellum - drug effects</subject><subject>Cerebellum - metabolism</subject><subject>Corpus Striatum - drug effects</subject><subject>Corpus Striatum - metabolism</subject><subject>Dose-Response Relationship, Drug</subject><subject>Haloperidol - administration & dosage</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Pharmacology. Drug treatments</subject><subject>Raclopride - metabolism</subject><subject>Radioligand Assay</subject><subject>Rats</subject><subject>Rats, Wistar</subject><subject>Receptors, Dopamine D2 - metabolism</subject><subject>Risperidone - administration & dosage</subject><subject>Tritium</subject><issn>0014-2999</issn><issn>1879-0712</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2006</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpFkE1r3DAQQEVpSDZp_kEIurSn2h3Jtj6OZdMmgUAu7Vlo5XFXi225kr2wveSvV8suBAY0M3ozMI-QOwYlAya-7UrcTVsbSw4gSqhzqA9kxZTUBUjGP5IVAKsLrrW-Itcp7QCg0by5JFdMyAqE1ivy9hAS0hZnjIMf7ezDSENHt7YPE0bfhv4rjT6d8hGpHVsaejv-s5PP5ZL8-Cc3qR_p3u8DbcNkh-PPAy8iOpzmEGlwbpns6A50wHkb2iM9b5FGO38iF53tE96e3xvy--ePX-un4uX18Xn9_aVwvIG5cBsBXIqO24ZbiwhaIOu0ki6nXEHtmG6Edlpx1aCWrQJXcdm1bAMVVKK6IV9Oe6cY_i6YZjP45LDPp2BYkhEKlNCCZ7A-gS6GlCJ2Zop-sPFgGJijeLMzJ_HmKN5AnUPlsfvz_mUzYPs-dDadgc9nwCZn-y5mHz69c1Ir1khe_QfI-o86</recordid><startdate>20060701</startdate><enddate>20060701</enddate><creator>NAIKER, Dineshree V</creator><creator>CARTS, Stanley V</creator><creator>CATTS, Vibeke S</creator><creator>BEDI, Kuldip S</creator><creator>BRYAN-LLUKA, Lesley J</creator><general>Elsevier</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>7X8</scope></search><sort><creationdate>20060701</creationdate><title>Dose determination of haloperidol, risperidone and olanzapine using an in vivo dopamine D2-receptor occupancy method in the rat</title><author>NAIKER, Dineshree V ; CARTS, Stanley V ; CATTS, Vibeke S ; BEDI, Kuldip S ; BRYAN-LLUKA, Lesley J</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c250t-cb60276f2a52aaee096e1f987ce092804c19569c98285e97d80c327fd1b030363</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2006</creationdate><topic>Algorithms</topic><topic>Analysis of Variance</topic><topic>Animals</topic><topic>Antipsychotic Agents - administration & dosage</topic><topic>Benzodiazepines - administration & dosage</topic><topic>Binding, Competitive - drug effects</topic><topic>Biological and medical sciences</topic><topic>Cerebellum - drug effects</topic><topic>Cerebellum - metabolism</topic><topic>Corpus Striatum - drug effects</topic><topic>Corpus Striatum - metabolism</topic><topic>Dose-Response Relationship, Drug</topic><topic>Haloperidol - administration & dosage</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Pharmacology. Drug treatments</topic><topic>Raclopride - metabolism</topic><topic>Radioligand Assay</topic><topic>Rats</topic><topic>Rats, Wistar</topic><topic>Receptors, Dopamine D2 - metabolism</topic><topic>Risperidone - administration & dosage</topic><topic>Tritium</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>NAIKER, Dineshree V</creatorcontrib><creatorcontrib>CARTS, Stanley V</creatorcontrib><creatorcontrib>CATTS, Vibeke S</creatorcontrib><creatorcontrib>BEDI, Kuldip S</creatorcontrib><creatorcontrib>BRYAN-LLUKA, Lesley J</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>MEDLINE - Academic</collection><jtitle>European journal of pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>NAIKER, Dineshree V</au><au>CARTS, Stanley V</au><au>CATTS, Vibeke S</au><au>BEDI, Kuldip S</au><au>BRYAN-LLUKA, Lesley J</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Dose determination of haloperidol, risperidone and olanzapine using an in vivo dopamine D2-receptor occupancy method in the rat</atitle><jtitle>European journal of pharmacology</jtitle><addtitle>Eur J Pharmacol</addtitle><date>2006-07-01</date><risdate>2006</risdate><volume>540</volume><issue>1-3</issue><spage>87</spage><epage>90</epage><pages>87-90</pages><issn>0014-2999</issn><eissn>1879-0712</eissn><coden>EJPHAZ</coden><abstract>The purpose of the present study was to determine antipsychotic doses that achieve 80% striatal dopamine D2-receptor occupancy for haloperidol, risperidone and olanzapine in rats. Wistar rats were treated with normal saline vehicle (controls), haloperidol (0.25 and 0.5 mg/kg/day), risperidone (3, 5 and 6 mg/kg/day) and olanzapine (5 and 10 mg/kg/day) for 7 days via osmotic minipumps. Striatal and cerebellar tissue were collected and in vivo dopamine D2-receptor occupancies were determined using 3H-raclopride. The doses required to achieve dopamine D2-receptor occupancy of 80% in 11- and 24-week old rats were: haloperidol 0.25 mg/kg/day, risperidone 5 mg/kg/day and olanzapine 10 mg/kg/day.</abstract><cop>Amsterdam</cop><pub>Elsevier</pub><pmid>16730699</pmid><doi>10.1016/j.ejphar.2006.04.048</doi><tpages>4</tpages></addata></record> |
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| subjects | Algorithms Analysis of Variance Animals Antipsychotic Agents - administration & dosage Benzodiazepines - administration & dosage Binding, Competitive - drug effects Biological and medical sciences Cerebellum - drug effects Cerebellum - metabolism Corpus Striatum - drug effects Corpus Striatum - metabolism Dose-Response Relationship, Drug Haloperidol - administration & dosage Male Medical sciences Pharmacology. Drug treatments Raclopride - metabolism Radioligand Assay Rats Rats, Wistar Receptors, Dopamine D2 - metabolism Risperidone - administration & dosage Tritium |
| title | Dose determination of haloperidol, risperidone and olanzapine using an in vivo dopamine D2-receptor occupancy method in the rat |
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