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Cyclopentadienyltricarbonylrheniumbenzazepines: synthesis and binding affinity
G Tamagnan1, R M Baldwin, N S Kula
1Yale University, School of Medicine, VA Connecticut HCS, West Haven 06516, USA. gilles.tamagnan@yale.edu
Bioorganic & Medicinal Chemistry Letters
|June 8, 2000
Abstract:
Analogues of the benzazepine dopamine D1 receptor antagonist SCH-23390 incorporating the cyclo-pentadienyltricarbonyl-rhenium (CPTR) moiety were synthesized and evaluated pharmacologically. The CPTR derivatives retained affinity (0.3-2.9 nM) and D1 selectivity of the parent compound, supporting their use as neuropharmacological surrogates for 99mTc-labeled SPECT radiopharmaceuticals.