Reagents for the determination of cerebral regional acetylcholinesterase activity

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United States of America Patent

PATENT NO 6509003
APP PUB NO 20020127180A1
SERIAL NO

09764263

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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The present invention relates to N-alkylpiperidine derivatives represented by general formula (1) or (2); ##STR1## wherein R.sup.1 represents optionally fluorinated lower alkyl; R.sup.2 represents lower alkyl; and R.sup.3 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 .gamma.-rays at an appropriate energy level. These characteristics make the compounds highly useful as tracers for SPECT in assaying the central AchE activity.

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Patent Owner(s)

  • DAIICHI PURE CHEMICALS CO., LTD.;DAIICHI RADIOISOTOPE LABORATORIES, LTD.

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Fukushi, Kiyoshi Funabashi, JP 3 2
Ikota, Nobuo Tokyo, JP 3 2
Irie, Toshiaki Yotsukaido, JP 12 20
Iyo, Masaomi Hamamatsu, JP 9 8
Nagatsuka, Shinichiro Ibaraki, JP 2 2
Namba, Hiroki Chiba, JP 2 2
Nishiura, Masaru Chiba, JP 2 2
Takatoku, Keizo Chiba, JP 2 2
Ueda, Takao Ibaraki, JP 11 91
Yomoda, Isamu Chiba, JP 2 2

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