Substituted 6-nitroquipazines, methods of preparation, and metho

Details Substituted 6-nitroquipazines, methods of preparation, and metho Substituted 6-nitroquipazines, methods of preparation, and metho

1992-12-22

1994-12-13

Stoll, Robert L.

Drug, bio-affecting and body treating compositions

Radionuclide or intended radionuclide containing; adjuvant...

In an organic compound

436504, 544363, A61K 4900, G01N 33567, C07D40100

Patent

active

053728130

ABSTRACT:
Disclosed is a substituted 6-nitroquipazine of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are each selected from the group consisting of H, Fl, CL, Br, I, CF.sub.3, CH.sub.2 CH.sub.2 F, CH.sub.3, CH.sub.2 CH.sub.3, and --CH(CH.sub.3).sub.2, and wherein one of R.sub.1, R.sub.2, R.sub.3, and R.sub.4 is other than H.
Also disclosed is a method for measurement of serotonin uptake sites in a sample, in which a radioligand is incubated with a sample and then the radioactivity of the radioligand bound to the sample is determined, utilizing a radio labeled substituted 6-nitroquipazine as the radioligand. Also disclosed is a method of manufacture and method of use.

REFERENCES:
patent: 3728351 (1973-04-01), Counsell et al.
patent: 3929907 (1975-12-01), Janzon et al.
patent: 4784958 (1988-11-01), Glossman
Mathis et al., "[125I]5-Iodo-2-nitro-2-piperazinylquinoline . . . ," European Journal of Pharmacology, 210(1), 103-4, 1992.

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