Synthesis and autoradiographic localization of the dopamine D-1 agonists [11C]SKF 75670 and [11C]SKF 82957 as potential PET radioligands
Identifieur interne : 003D31 ( Main/Exploration ); précédent : 003D30; suivant : 003D32Synthesis and autoradiographic localization of the dopamine D-1 agonists [11C]SKF 75670 and [11C]SKF 82957 as potential PET radioligands
Auteurs : Jean N. Dasilva [Canada] ; Alan A. Wilson [Canada] ; Jose N. Nobrega [Canada] ; Dilshad Jiwa [Canada] ; Sylvain Houle [Canada]Source :
- Applied Radiation and Isotopes [ 0969-8043 ] ; 1996.
Abstract
The high affinity benzazepine D1 agonists SKF 75670 and SKF 82957 were labeled with 11C by N-[11C]methylation of SKF 38393 and SKF 81297, respectuvely, using [11C]methyl iodide in the presence of N-ethyldiisopropylamide. Both radiotracers were purified using a semi-preparative cation exchange HPLC column. Radiochemical yields of 20–75% were obtained (from [11C]methyl iodine, decay-corrected) with a synthesis time of 30–35 min from EOB. The specific activities wer e 700–2500 Ci/mmol (25.9–92.5 GBq/μmol) at EOS, and the radiochemical purities were > 99%. Autoradiographic studies showed selective binding for both tracers in rat brain regions rich in D1 receptors such as the caudata-putamen, nucleus accumbens, olfactory tubercles and substantia nigra. [11C]SKF 75670 and [11C]SKF 82957 are thus potential PET radioligands for the functional high-affinity state of D1 receptors.
Url:
DOI: 10.1016/0969-8043(95)00306-1
Affiliations:
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Nobrega</name><affiliation wicri:level="4"><country>Canada</country><wicri:regionArea>Neuroimaging Research Section, Clarke Institute of Psychiatry, Department of Psychiatry, University of Toronto, 250 College St., Toronto, Ontario</wicri:regionArea><orgName type="university">Université de Toronto</orgName><placeName><settlement type="city">Toronto</settlement><region type="state">Ontario</region></placeName></affiliation></author><author><name sortKey="Jiwa, Dilshad" sort="Jiwa, Dilshad" uniqKey="Jiwa D" first="Dilshad" last="Jiwa">Dilshad Jiwa</name><affiliation wicri:level="4"><country>Canada</country><wicri:regionArea>Neuroimaging Research Section, Clarke Institute of Psychiatry, Department of Psychiatry, University of Toronto, 250 College St., Toronto, Ontario</wicri:regionArea><orgName type="university">Université de Toronto</orgName><placeName><settlement type="city">Toronto</settlement><region type="state">Ontario</region></placeName></affiliation></author><author><name sortKey="Houle, Sylvain" sort="Houle, Sylvain" uniqKey="Houle S" first="Sylvain" last="Houle">Sylvain Houle</name><affiliation wicri:level="4"><country>Canada</country><wicri:regionArea>PET Centre, Clarke Institute of Psychiatry, Department of Psychiatry, University of Toronto, 250 College St., Toronto, Ontario</wicri:regionArea><orgName type="university">Université de Toronto</orgName><placeName><settlement type="city">Toronto</settlement><region type="state">Ontario</region></placeName></affiliation></author></analytic><monogr></monogr><series><title level="j">Applied Radiation and Isotopes</title><title level="j" type="abbrev">ARI</title><idno type="ISSN">0969-8043</idno><imprint><publisher>ELSEVIER</publisher><date type="published" when="1996">1996</date><biblScope unit="volume">47</biblScope><biblScope unit="issue">3</biblScope><biblScope unit="page" from="279">279</biblScope><biblScope unit="page" to="284">284</biblScope></imprint><idno type="ISSN">0969-8043</idno></series></biblStruct></sourceDesc><seriesStmt><idno type="ISSN">0969-8043</idno></seriesStmt></fileDesc><profileDesc><textClass></textClass><langUsage><language ident="en">en</language></langUsage></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">The high affinity benzazepine D1 agonists SKF 75670 and SKF 82957 were labeled with 11C by N-[11C]methylation of SKF 38393 and SKF 81297, respectuvely, using [11C]methyl iodide in the presence of N-ethyldiisopropylamide. Both radiotracers were purified using a semi-preparative cation exchange HPLC column. Radiochemical yields of 20–75% were obtained (from [11C]methyl iodine, decay-corrected) with a synthesis time of 30–35 min from EOB. The specific activities wer e 700–2500 Ci/mmol (25.9–92.5 GBq/μmol) at EOS, and the radiochemical purities were > 99%. Autoradiographic studies showed selective binding for both tracers in rat brain regions rich in D1 receptors such as the caudata-putamen, nucleus accumbens, olfactory tubercles and substantia nigra. [11C]SKF 75670 and [11C]SKF 82957 are thus potential PET radioligands for the functional high-affinity state of D1 receptors.</div></front></TEI><affiliations><list><country><li>Canada</li></country><region><li>Ontario</li></region><settlement><li>Toronto</li></settlement><orgName><li>Université de Toronto</li></orgName></list><tree><country name="Canada"><region name="Ontario"><name sortKey="Dasilva, Jean N" sort="Dasilva, Jean N" uniqKey="Dasilva J" first="Jean N." last="Dasilva">Jean N. Dasilva</name></region><name sortKey="Houle, Sylvain" sort="Houle, Sylvain" uniqKey="Houle S" first="Sylvain" last="Houle">Sylvain Houle</name><name sortKey="Jiwa, Dilshad" sort="Jiwa, Dilshad" uniqKey="Jiwa D" first="Dilshad" last="Jiwa">Dilshad Jiwa</name><name sortKey="Nobrega, Jose N" sort="Nobrega, Jose N" uniqKey="Nobrega J" first="Jose N." last="Nobrega">Jose N. Nobrega</name><name sortKey="Wilson, Alan A" sort="Wilson, Alan A" uniqKey="Wilson A" first="Alan A." last="Wilson">Alan A. 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