;wherein R1 represents optionally fluorinated lower alkyl; R2 represents lower alkyl; and R3 represents alkenyl substituted at the 1-position with hydroxy, lower alkoxy, lower alkoxyalkyloxy, lower alkoxyalkyloxyalkyloxy, or lower alkanoyloxy and substituted at the end with radioactive iodine, or alkenyloxymethyl substituted at the end with a radioactive iodine reagent containing the same for assaying central local AchE activity; a method for assaying the central local AchE activity; and labeled precursors of the above compounds. After easily passing through the blood-brain barrier, these compounds are hydrolyzed specifically by AchE in the brain into alcohols, which are then captured by the brain. In contrast, alcohols formed outside the brain do not migrate into the brain. The compounds of the invention emit &ggr;-rays at an appropriate energy level. These characteristics make the compounds highly useful as tracers for SPECT in assaying the central AchE activity."/>
公开/公告号US6509003B2
专利类型
公开/公告日2003-01-21
原文格式PDF
申请/专利号US20010764263
发明设计人 HIROKI NAMBA;MASARU NISHIURA;KEIZO TAKATOKU;NOBUO IKOTA;TOSHIAKI IRIE;ISAMU YOMODA;MASAOMI IYO;SHINICHIRO NAGATSUKA;KIYOSHI FUKUSHI;TAKAO UEDA;
申请日2001-01-19
分类号A61K510/40;A61K314/45;A61K491/00;C07D2114/00;
国家 US
入库时间 2022-08-22 00:05:41