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.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, Non-P.H.S.
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Benzazepines / analogs & derivatives*
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Benzazepines / chemical synthesis
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Benzazepines / chemistry
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Benzazepines / metabolism
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Organometallic Compounds / chemical synthesis
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Organometallic Compounds / chemistry*
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Organometallic Compounds / metabolism*
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Radiopharmaceuticals / chemical synthesis
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Radiopharmaceuticals / chemistry*
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Radiopharmaceuticals / metabolism*
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Rats
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Receptor, Serotonin, 5-HT2A
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Receptor, Serotonin, 5-HT2C
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Receptors, Dopamine D1 / metabolism*
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Receptors, Serotonin / metabolism
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Rhenium / chemistry
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Structure-Activity Relationship
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Technetium
Substances
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2'-tricarbonylcyclopentadienylrhenium-SCH-23390
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3'-tricarbonylcyclopentadienylrhenium-SCH-23390
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Benzazepines
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Organometallic Compounds
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Radiopharmaceuticals
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Receptor, Serotonin, 5-HT2A
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Receptor, Serotonin, 5-HT2C
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Receptors, Dopamine D1
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Receptors, Serotonin
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Rhenium
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Technetium