title: Cyclopentadienyltricarbonylrheniumbenzazepines: synthesis and binding affinity.
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.
authors.affiliation: Yale University, School of Medicine, VA Connecticut HCS, West Haven 06516, USA. gilles.tamagnan@yale.edu
authors.forename: G
authors.initials: G
authors.lastname: Tamagnan
authors.forename: R M
authors.initials: RM
authors.lastname: Baldwin
authors.forename: N S
authors.initials: NS
authors.lastname: Kula
authors.forename: R J
authors.initials: RJ
authors.lastname: Baldessarini
authors.forename: R B
authors.initials: RB
authors.lastname: Innis
mesh_terms: D000818:Animals; D001552:Benzazepines / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism*; D051381:Rats; D044402:Receptor, Serotonin, 5-HT2A; D044405:Receptor, Serotonin, 5-HT2C; D017447:Receptors, Dopamine D1 / Q000378:metabolism*; D011985:Receptors, Serotonin / Q000378:metabolism; D012211:Rhenium / Q000737:chemistry; D013329:Structure-Activity Relationship; D013667:Technetium
chemical_list: C413738:2'-tricarbonylcyclopentadienylrhenium-SCH-23390; C413739:3'-tricarbonylcyclopentadienylrhenium-SCH-23390; D001552:Benzazepines; D009942:Organometallic Compounds; D019275:Radiopharmaceuticals; D044402:Receptor, Serotonin, 5-HT2A; D044405:Receptor, Serotonin, 5-HT2C; D017447:Receptors, Dopamine D1; D011985:Receptors, Serotonin; D012211:Rhenium; D013667:Technetium