Cyclopentadienyltricarbonylrheniumbenzazepines: synthesis and binding affinity

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 thei...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2000-05, Vol.10 (10), p.1113-1115
Main Authors: Tamagnan, G, Baldwin, R M, Kula, N S, Baldessarini, R J, Innis, R B
Format: Article
Language:English
Subjects:
Animals
Benzazepines - analogs & derivatives
Benzazepines - chemical synthesis
Benzazepines - chemistry
Benzazepines - metabolism
Organometallic Compounds - chemical synthesis
Organometallic Compounds - chemistry
Organometallic Compounds - metabolism
Radiopharmaceuticals - chemical synthesis
Radiopharmaceuticals - chemistry
Radiopharmaceuticals - metabolism
Rats
Receptor, Serotonin, 5-HT2A
Receptor, Serotonin, 5-HT2C
Receptors, Dopamine D1 - metabolism
Receptors, Serotonin - metabolism
Rhenium - chemistry
Structure-Activity Relationship
Technetium
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Summary: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.
ISSN:0960-894X
DOI:10.1016/S0960-894X(00)00185-2