SPECT imaging agents for serotonin transporters

    公开(公告)号:US06921840B1

    公开(公告)日:2005-07-26

    申请号:US09959581

    申请日:1999-04-30

    申请人: Hank F. Kung

    发明人: Hank F. Kung

    摘要: The present invention is directed to compounds of Formula (I) or pharmaceutically acceptable salts thereof; wherein X is hydrogen, Cl, Br, I, NO2, NR3R4 or —L—Ch; Y is hydrogen, —CH2OR5, —CH2NCH3R1, NO2, NR3R4 or —L—Ch; Y′ is hydrogen, —CH2OH5, —CH2NCH3R1, NO2, NR3R4 OR —L—Ch; provided that at least one of the Y or Y′ is —CH2NCH3R1; Z is S, O, NR6 CR7R8, C(O) or —C(═CR7R8)-; A is hydrogen, Cl, I, Br or —L—Ch; R1 is hydrogen, C1-C5 alkyl, C3-C8 cycloalkyl C1-5 alkylcarbonyl, (C3-C8 cycloalkyl) carbonyl, pnenyl, benzyl, naphthyl, naphthylmethyl or L—Ch; R2 is hydrogen or methyl; and R3-R8 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 affinity to SERT sites and show more high selectively for SERT over NET and DAT.

    Sulfide compounds and methods and compositions for treating depression
    19.
    发明授权
    Sulfide compounds and methods and compositions for treating depression 失效
    硫化合物和治疗抑郁症的方法和组合物

    公开(公告)号:US4123555A

    公开(公告)日:1978-10-31

    申请号:US741196

    申请日:1976-11-12

    摘要: Compounds, pharmaceutical preparations containing same, and method of treating depression in mammals, the compounds being of the formula I ##STR1## or an acid addition salt thereof, particularly a pharmacologically or pharmaceutically acceptable salt thereof, where R and R.sup.1 are the same or different and are each hydrogen or lower alkyl, or R and R.sup.1 taken together are (CH.sub.2).sub.X where X is 4 or 5, or NRR.sup.1 is ##STR2## where Y is 3 or 4 and R.sup.3 is hydrogen or lower alkyl, or NRR.sup.1 is ##STR3## where R.sup.2 is hydrogen or lower alkyl, in the above lower alkyl has 1 to 4 carbons and may be straight or branched and n and m are the same or different and are 1, 2, or 3.

    摘要翻译: 化合物,含有它们的药物制剂和治疗哺乳动物抑郁症的方法,式I化合物(I)或其酸加成盐,特别是其药理学或药学上可接受的盐,其中R和R 1是 相同或不同,各自为氢或低级烷基,或R和R1一起为(CH 2)X,其中X为4或5,或NRR1为Y,其中Y为3或4,R3为氢或低级烷基,或 NRR1是其中R 2是氢或低级烷基,其中上述低级烷基具有1至4个碳,并且可以是直链或支链,并且n和m相同或不同,并且是1,2或3。