17672-25-2Relevant academic research and scientific papers
1-(3′-[125I]iodophenyl)-3-methy-2-pyrazolin-5-one: Preparation, solution stability, and biodistribution in normal mice
Sano, Yuuhei,Motomura, Tomokazu,Yamamoto, Fumihiko,Fukuda, Miki,Mukai, Takahiro,Maeda, Minoru
experimental part, p. 1020 - 1025 (2010/11/04)
3-Methyl-1-phenyl-2-pyrazolin-5-one (edaravone, 1), known as a potent free radical scavenger, has been developed as a medical drug for the treatment of acute cerebral infarction. With the aim of developing radiotracers for imaging free radicals in vivo, 1-(3′-[125I]iodophenyl)-3-methy-2- pyrazolin-5-one (125I-2) was synthesized by two methods, via isotopic exchange and interhalogen exchange under solvent-free conditions, in which iodo- and bromo-derivatives were used as labeling precursors, respectively. After HPLC purification, 125I-2 was obtained in modest isolated radiochemical yields (ca. 20%) with high radiochemical purities by both methods. The former gave specific activities of 0.2-0.6 kBq/μmol, whereas the latter approach achieved specific activities of more than 0.14 GBq/μmol. On attempting to prepare an injectable formulation for 125I-2 with high specific activity, its radiochemical purities dropped to about 60-70%. Unlabeled analog 2 was found to have lipophilic and antioxidant properties similar to edaravone. Intravenous injection of 125I-2 with low specific radioactivity into normal mice showed signs of distribution profiles similar to reported results for 14C-labeled edaravone in normal rats.
Pyrazolones as inhibitors of 11B-hydroxysteroid dehydrogenase
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Page/Page column 20-21, (2008/06/13)
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, type II diabetes mellitus and metabolic syndrome.
