title: Carrier effect on radiolabeling the polynuclear pentavalent rhenium-186 complex of dimercaptosuccinic acid at alkaline pH: 186Re(V)-DMS.
abstract: Radiolabeling with rhenium (Re-186, Re-188), a tumor agent to resemble the pentavalent polynuclear technetium complex of dimercaptosuccinic acid (99mTc[V]-DMS) has been reported for radiotherapeutical use. Nevertheless, despite the periodic analogies between both radiometals, differences in the redox potential and the carrier concentration have made the radiolabeling of the rhenium counterpart difficult. In the present study, the effect of the carrier contained in the reactor-produced Re-186 was estimated as an important factor relevant to the Re-186 radiolabeling of DMS at an alkaline pH. Great effect of the carrier Re with an inverse correlation with the stannous ion was an interesting phenomenon relevant for an assumption on the Sn participation in the complex. Under strict control of various labeling parameters, the 186Re(V)-DMS was made available with high yield (93-97%) at an alkaline pH and at room temperature. The great effect of carrier offers support to the polymeric or polynuclear nature of the rhenium complex of DMS as depicted in the drug design basis of its parent Tc(V)-DMS. The biodistribution studies of Re(V)-DMS showed mimetic characteristics with its parent Tc(V)-DMS drug.
authors.affiliation: Department of Pathofunctional Bioanalysis, Graduate School of Pharmaceutical Sciences, Faculty of Pharmaceutical Sciences, Kyoto University, Japan. shkazuko@pharm.kyoto-u.ac.jp
authors.forename: K
authors.initials: K
authors.lastname: Horiuchi
authors.forename: H
authors.initials: H
authors.lastname: Saji
authors.forename: A
authors.initials: A
authors.lastname: Yokoyama
mesh_terms: D000818:Animals; D002286:Carcinoma, Ehrlich Tumor / Q000532:radiotherapy; D002614:Chelating Agents / Q000737:chemistry*; D006863:Hydrogen-Ion Concentration; D007553:Isotope Labeling / Q000379:methods; D051379:Mice; D009942:Organometallic Compounds / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000627:therapeutic use; D011868:Radioisotopes / Q000737:chemistry / Q000627:therapeutic use; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000627:therapeutic use; D019163:Reducing Agents / Q000737:chemistry; D012211:Rhenium / Q000737:chemistry* / Q000627:therapeutic use; D004113:Succimer / Q000138:chemical synthesis* / Q000737:chemistry* / Q000493:pharmacokinetics / Q000627:therapeutic use; D013696:Temperature; D017971:Tin Compounds / Q000737:chemistry; D014018:Tissue Distribution
chemical_list: D002614:Chelating Agents; D009942:Organometallic Compounds; D011868:Radioisotopes; D019275:Radiopharmaceuticals; D019163:Reducing Agents; D017971:Tin Compounds; C069609:rhenium(V)dimercaptosuccinic acid; C023599:stannous chloride; D012211:Rhenium; D004113:Succimer