METHOD OF PRODUCING AN ACTIVE PHARMACEUTICAL SUBSTANCE FOR SYNTHESIS OF A RADIOPHARMACEUTICAL PREPARATION TROPIC TO CELLS OF EHRLICH CARCINOMA

摘要

FIELD: pharmaceutics.;SUBSTANCE: invention refers to chemical-pharmaceutical industry and concerns preparing an active pharmaceutical substance based on DNA-aptamers for synthesis of a radiopharmaceutical preparation tropic to Ehrlich's carcinoma cells. Method comprises a step of introducing a radioactive label, which is selected as an ultralow-living radionuclide with positron type of decay – ¹¹C into molecule – DNA-oligonucleotide, wherein radioactive label is introduced into primer molecule (5'-/5ThioMC6-D/GGC TTC TGG ACT ACC TAT GC3'), complementary to 20 nucleotide section by 3'-end of aptamer AS14, primer is pre-activated – subjected to treatment for disruption of disulphide bonds and nucleophilic substitution reaction, obtained 3'-thiomodified primer is heated in a closed reaction vessel with methyl iodide in DMSO medium, and obtained from methylation reaction 3'-11CH₃S-primer is mixed with preheated aptamer AS14 with subsequent cooling of finished mixture and obtaining complex 3'-11CH₃S-primer with AS14 aptamer used as an active pharmaceutical substance.;EFFECT: method enables to obtain an active pharmaceutical substance for synthesis of a radiopharmaceutical with high degree of DNA-oligonucleotide binding to radionuclide ¹¹C and high tropism to cells of ascitic Ehrlich's carcinoma.;4 cl, 2 dwg, 2 tbl, 2 ex