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 their use as neuropharmacological surrogates for 99mTc-labeled SPECT radiopharmaceuticals.
Tamagnan
G
G
Yale University, School of Medicine, VA Connecticut HCS, West Haven 06516, USA. gilles.tamagnan@yale.edu
Baldwin
R M
RM
Kula
N S
NS
Baldessarini
R J
RJ
Innis
R B
RB
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
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