MEANS FOR REDUCTION OF GLYCOPROTEIN-P FUNCTIONAL ACTIVITY AND EXPRESSION Russian patent published in 2018 - IPC A61K31/5377 A61P43/00 

Abstract RU 2649134 C1

FIELD: pharmacology.

SUBSTANCE: application of afobazole (5-ethoxy-2-[2-(morpholino)ethylthio]benzylimidazole dihydrochloride) as an agent for reduction of functional activity and expression of glycoprotein-P is proposed. The technical result of the invention is expanded arsenal of agents with an ability to inhibit functional activity and expression of glycoprotein-P in order to increase the effectiveness of pharmacotherapy of CNS pathologies and oncological diseases with drug substances-substrates of this transporter protein; means suitable for prediction of drugs belonging to the substrates of the glycoprotein-P membrane transporter protein, and agents used as a positive control for reduced glycoprotein-P activity in the search for substances of a similar effect.

EFFECT: due to the low toxicity and economic availability of afobazole, its application with a view to inhibition of glycoprotein-P is rational and safe, improves the therapy without risk of enhanced toxicity and has additional benefits of anxiolytic and neuroprotective actions of the drug.

2 tbl

Similar patents RU2649134C1

Title Year Author Number
METHOD TO MODEL CONDITION OF INHIBITION OF FUNCTIONAL ACTIVITY OF GLYCOPROTEIN-P BY LYNESTRENOL IN TRIAL 2014
  • Kotljarova Anna Anatol'Evna
  • Jakusheva Elena Nikolaevna
RU2553362C1
METHOD OF DETERMINING FUNCTIONAL ACTIVITY OF GLYCOPROTEIN-P 2015
  • Yakusheva Elena Nikolaevna
  • Chernykh Ivan Vladimirovich
  • Shchulkin Aleksej Vladimirovich
RU2587780C1
HYDROLYZATE OF TANSY FLOWERS COMPLEX POLYSACCHARIDE COMPLEX AS A GLYCOPROTEIN-P TRANSPORTER PROTEIN INHIBITOR 2019
  • Yakusheva Elena Nikolaevna
  • Chernykh Ivan Vladimirovich
  • Esenina Anna Sergeevna
  • Shchulkin Aleksej Vladimirovich
  • Popova Natalya Mikhajlovna
  • Kirichenko Ekaterina Evgenevna
  • Grandinar Mariya Mikhajlovna
RU2699042C1
METHOD FOR EXPERIMENTAL FINASTERIDE SIMULATION OF INDUCTION OF FUNCTIONAL ACTIVITY OF GLYCOPROTEIN-P 2012
  • Chernykh Ivan Vladimirovich
  • Jakusheva Elena Nikolaevna
RU2504018C1
PROLONGED ACTION PHARMACEUTICAL COMPOSITION BASED ON 5-ETHOXY-2-[2-(MORPHOLINO)-ETHYLTHIO]BENZIMIDAZOLE DIHYDROCHLORIDE AND/OR BASE (APHOBAZOLUM) 2017
  • Seredenin Sergej Borisovich
  • Yarkova Milada Alnordovna
  • Alekseev Konstantin Viktorovich
  • Blynskaya Evgeniya Viktorovna
  • Zherdev Vladimir Pavlovich
  • Durnev Andrej Dmitrievich
  • Neznamov Grigorij Georgievich
RU2694837C2
METHOD FOR INHIBITION OF GLYCOPROTEIN-P IN AN IN VITRO EXPERIMENT 2021
  • Abalenikhina Yuliya Vladimirovna
  • Erokhina Pelageya Dmitrievna
  • Mylnikov Pavel Yurevich
  • Shchulkin Aleksej Vladimirovich
  • Yakusheva Elena Nikolaevna
  • Popova Natalya Mikhajlovna
RU2779177C1
METHOD FOR ASSESSING THE FUNCTIONAL ACTIVITY OF GLYCOPROTEIN-P IN THE BLOOD-BRAIN BARRIER 2018
  • Yakusheva Elena Nikolaevna
  • Chernykh Ivan Vladimirovich
  • Shchulkin Aleksej Vladimirovich
  • Popova Natalya Mikhajlovna
  • Mylnikov Pavel Yurevich
RU2677286C1
DRUG FOR PREVENTION AND TREATMENT OF DIABETES 2013
  • Seredenin Sergej Borisovich
  • Ostrovskaya Rita Usherovna
  • Voronina Tatyana Aleksandrovna
  • Zolotov Nikolaj Nikolaevich
  • Yarkova Milada Alnordovna
  • Durnev Andrej Dmitrievich
RU2597848C2
METHOD OF ABCB1 PROTEIN INHIBITION IN EXPERIMENT IN VITRO 2023
  • Chernykh Ivan Vladimirovich
  • Kopanitsa Mariia Andreevna
  • Mylnikov Pavel Iurevich
  • Shchulkin Aleksei Vladimirovich
  • Ershov Andrei Iurevich
  • Martynenkov Aleksandr Alekseevich
  • Lagoda Igor Viktorovich
  • Kukov Dmitrii Vladimirovich
  • Iakusheva Elena Nikolaevna
  • Popova Natalia Mikhailovna
RU2811993C1
AGENT FOR CORRECTING AUTISM SPECTRUM DISORDERS 2017
  • Seredenin Sergej Borisovich
  • Kapitsa Inga Gennadievna
  • Ivanova Elena Anatolevna
  • Voronina Tatyana Aleksandrovna
RU2666598C1

RU 2 649 134 C1

Authors

Yakusheva Elena Nikolaevna

Seredenin Sergej Borisovich

Yarkova Milada Alnordovna

Chernykh Ivan Vladimirovich

Shchulkin Aleksej Vladimirovich

Gatsanoga Mariya Valerievna

Dates

2018-03-29Published

2017-01-17Filed