| 摘要 |
The present invention is directed to compounds of Formula (I) or pharmaceutically acceptable salts thereof; wherein X is hydrogen, C1, Br, I, NO2, NR<3>R<4> or -L-Ch; Y is hydrogen, -CH2OR<5>, -CH2NCH3R<1>, NO2, NR<3>R<4> or -L-Ch; Y' is hydrogen, -CH2OR<5>, -CH2NCH3R<1>, NO2, NR<3>R<4> OR -L-Ch; provided that at least one of the Y or Y' is -CH2NCH3R<1>; Z is S, O, NR<6>, CR<7>R<8>, C(O) or -C(=CR<7>R<8>)-; A is hydrogen, C1, I, Br or -L-Ch; R<1> is hydrogen, C1-C5 alkyl, C3-C8 cycloalkyl C1-5 alkylcarbonyl, (C3-C8 cycloalkyl) carbonyl, pnenyl, benzyl, naphthyl, naphthlymethyl or L-Ch; R<2> is hydrogen or methyl; and R<3>-R<8> are as defined herein. Radiolabeled compounds of the invention are useful as selective serotonin transporter (SERT) imaging agents for single photon emission tomography (SPECT). As such the compounds are useful for studying the underlying pharmacology and interaction of specific serotinin reuptake site inhibitors (SSRI), commonly used antidepressants, at the SERT sites in the human brain. Certain compounds of the invention, including IDAM (5-iodo-2[[2-2-[(dimethylamino)methyl]phenyl]thio]benzylalcohol) display ecxellent affinity to SERT sites and show more high selectively for SERT over NET and DAT. |
