A new synthesis is described for the production of the positron emitting radiopharmaceutical R-(+)-7-chloro-8-hydroxy-2,3,4,5-tetrahydro-3-N-[11C]methyl-1-phenyl-1H- 3-benzazepine (SCH 23390, 2a). This novel method involves reductive carboxylation, in which [11C]CO2 is reacted with the trimethylsily
Synthesis of [11C]SCH 23390 for dopamine D1 receptor studies
β Scribed by O.T. DeJesus; G.J.C. Van Moffaert; A.M. Friedman
- Publisher
- Elsevier Science
- Year
- 1987
- Weight
- 365 KB
- Volume
- 38
- Category
- Article
- ISSN
- 0883-2889
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β¦ Synopsis
The optimal conditions for the synthesis of 11C-labelled SCH 23390 by radio-methylation of its desmethyl precursor, SCH 24518, with [11C]iodomethane are described. Isocratic reversed phase HPLC was used for the purification of [11C]SCH 23390. The specific activity range in 30 runs was 10-235 Ci/mmol and average radiochemical yield was 72% based on [11C]iodomethane. Mean synthesis time was 40-60 min from the end of bombardment. Preliminary animal studies indicate that [11C]SCH 23390 would be useful in visualizing D1 receptors in a living brain by positron tomography.
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The dopamine D-1 receptor antagonist, SCH 23390 ((R)-(+)-8-chloro-2,3,4,5-tetrahydro-3-methyl-5-phenyl-1H-3- benzazepin-7-ol), was labelled by alkylation of the desmethyl compound SCH 24518 ((R)-(+)-8-chloro-2,3,4,5-tetrahydro-5-phenyl-1H-3-benzazepin-7- ol) with [11C]methyl iodide. A multivariate o
A r a d i o b r o d n a t e d analog of SCH 23390, a s e l e c t i v e dopamine D1/DAI a n t a g o n i s t was prepared. were obtained w i t h i n 15 minutes r e a c t i o n a t r o m temperature. The s y n t h e s i s was v a l i d a t e d by performing both p h y s i c a l (MR and mass spectroscop
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