Radioactive benzodiazepine derivatives

Organic compounds -- part of the class 532-570 series – Organic compounds – Unsubstituted hydrocarbyl chain between the ring and the -c-...

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424 11, C07D24312, A61K 4902

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active

052161471

ABSTRACT:
The present invention relates to a novel radioactive benzodiazepine derivative represented by the formula: ##STR1## wherein R is hydrogen or a lower alkyl; X* is radioactive iodine or bromine; Y is hydrogen or a halogen; and Z is a halogen or nitro group; and the salt thereof.
The compound of the present invention enables to non-invasively detect the presence of benzodiazepine receptors in human or animal brains, other organs or tissues. Additionally, it enables to dynamically trace the change in receptor concentration either. It is very useful as a radioactive diagnostic agent for nuclear medicine in vitro or in vivo or as a radiopharmaceutical.

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patent: 4280993 (1981-07-01), Braestrup et al.
patent: 4606908 (1986-08-01), Bassingthwaighte et al.
Int. J. Appl. Radiat. Isot. 35, 973-976 (1984).
Neuroscience Letters, 48, 115-120 (1984).
J. Psychiatric Res., 19, 609-622 (1985) No. 4.
The Journal of Nuclear Medicine (Abstract Book), vol. 28, No. 4, Apr. 1987 pp. 726-727, Abstract No. 719, New York, NY., US; M. E. VanDort et al.

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