Preparation of tritium labeled dexamethasone phosphate and its application to assess the affinity of ligands to glucocorticoid receptors

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Resumo

The possibility of introducing tritium using the thermal activation method into dexamethasone and dexamethasone phosphate has been shown. Labeled compounds have been successfully used to assess the affinity of ligands to glucocorticoid receptors.

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Sobre autores

G. Badun

Moscow State University

Autor responsável pela correspondência
Email: badunga@my.msu.ru

Faculty of Chemistry

Rússia, Moscow, 119991

E. Zhidkova

Blokhin Russian Cancer Research Center, Ministry of Health of Russia

Email: badunga@my.msu.ru
Rússia, Moscow, 115478

M. Chernysheva

Moscow State University

Email: badunga@my.msu.ru

Faculty of Chemistry

Rússia, Moscow, 119991

A. Enikeev

Blokhin Russian Cancer Research Center, Ministry of Health of Russia

Email: badunga@my.msu.ru
Rússia, Moscow, 115478

M. Yakubovskaya

Blokhin Russian Cancer Research Center, Ministry of Health of Russia; Friendship University of Russia

Email: badunga@my.msu.ru
Rússia, Moscow, 115478; Moscow, 117198

E. Lesovaya

Blokhin Russian Cancer Research Center, Ministry of Health of Russia; Friendship University of Russia; Pavlov Ryazan State Medical University, Ministry of Health of Russia

Email: badunga@my.msu.ru
Rússia, Moscow, 115478; Moscow, 117198; Ryazan, 390026

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2. Scheme 1. Glucocorticoid receptor ligands used in the work: a – dexamethasone, b – dexamethasone phosphate, c – Compound A (CpdA).

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3. Fig. 1. Dependence of the specific radioactivity of [3H]dexamethasone on the mass of the drug applied to the walls of the reaction vessel from a methanol solution.

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4. Fig. 2. Dependence of the specific radioactivity of [3H]dexamethasone phosphate on the temperature of the atomizer when the substance is applied to smooth walls by lyophilization of an aqueous solution (1) and by evaporation of a methanol solution applied to rough walls of the reaction vessel (2).

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5. Fig. 3. Dependence of the signal level (in % of the maximum) on the incubation time with [3H]dexamethasone.

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6. Fig. 4. Change in the proportion of [3H]dexamethasone bound to GH at its concentration of 0.5, 1 and 2 μmol/l and different amounts of unlabeled dexamethasone phosphate. Incubation time 90 min.

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7. Fig. 5. Dependence of the proportion of GH-bound [3H]dexamethasone phosphate (0.5 μmol/L) on GH in the presence of unlabeled dexamethasone phosphate or CpdA. Incubation time is 90 min. Data are presented as % of the signal level in samples with [3H]dexamethasone.

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