Exchange yielding R u t h e n o c e n o y l -g l y c i n e -D e r i v a t i v e s react i o n of Ferrocen oy 1 -9 1 y c i net hy 1 ester w i t h 03RuC 1 Summary: Ruthenocenoyl-glycine derivatives labelled with radioactive ruthenium (g7Ru, lo3Ru). showing a clearance similar t o Hippuran, are potential r a d i o p h a r m a c e u t i c a l s . S y n t h e s i s , reaction mechanism and identification o f r u t h e n o c e n o y l -1 . 1 ' -d i g l y c i n e derivatives are described. Einleitung: Ruthenocenoy mi t radioakt -glycin (Ruppuran) und -diglycin kann man leicht vem Ruthenium als Zentralatom markieren. Beide Ruthenocen-Derivate haben interessante biochemische Eigenschaften: Sie werden ahnlich w i e das Radiopharmakon o-clod-Hippursaure (Hippuran) primar von der Niere akkumuliert und eden (1,2). D a diese werden u n d im Urin sie z u r Bestimmung anschliei3end extrem schnell renal ausgesch Ruthenocen-Verbindungen nicht metabolisier nur die Ausgangs-Produkte erscheinen, sind der Nieren-Funktion gut geeignet.
The ruthenocene derivatives of different biogenic amines labelled with 103RU in the ruthenocene moity were synthesized. In a first step the central atom of ferrocene was exchanged with 103RuCl3 yielding [103RU]‐ruthenocene, by vilsmeier‐formylation the radioactive ruthenocene aldehyde was synthesized which was condensed with the desired amine to the Schiff'sche base, followed by the reduction of the CN double bond by NaBH4.
Ruthenocenoyl-glycine (ruppuran) is a metallocene analog of iodo-labeled hippuran. After injection of 103Ru-labeled ruppuran and ruthenocenoyl-1,1'-diglycine in rabbits, measurement with external detectors revealed a very rapid accumulation in the kidneys followed by rapid excretion of the 103Ru activity. By measurement of the radioactivity concentration in plasma and urine samples collected 1-60 min after IV injection, the plasma clearance was calculated and compared with the clearance of 125I-labeled hippuran injected simultaneously. The clearance of ruppuran and ruthenocenoyl-diglycine in rabbits was found to be somewhat higher than that of hippuran. Extrapolating to man (1.73 m3), plasma clearance with both ruthenocene derivatives was approximately 500-600 ml/min. Biochemical data as well as the nuclear properties of 97Ru indicate the usefulness of 97Ru-labeled ruthenocenoyl-glycine as a radiopharmaceutical for kidney function studies.
The cytostatic drugs Chlorambucil and Bleomycin were labeled with 131I and with 57Co, respectively: Ruthenocenealdehyde-(N-methyl-N-beta-chlorethyl)-hydrazone and Ruthenocene-3-phenyl-prop.1-en-3-one were labeled with the gamma emitter 103Ru. In tumor-bearing mice the elimination and organ distribution of these radioactive substances were tested after intravenous (i.v.) and intratumoral (i.t.) injection of the drugs. The organ load showed lower values after i.t. than after i.v. application, while the radioactivity concentrations in the tumor were considerably increased after i.t. injection. The integrals of the concentration-time curves showed 10--80 times higher concentrations in the tumor after i.t. compared to i.v. injection of the drugs.
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