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Efficacy of 4-(2-(4-nitrophenyl)-2-oxoethyl)-1-(thietane-3-yl)-1h-1,2,4-triazol-4 bromide in the rat model of inferior vena cava thrombosis

https://doi.org/10.18705/2311-4495-2024-11-1-19-27

EDN: AMKUTB

Abstract

   Introduction. According to WHO, acute disorders of cerebral circulation are anticipated to become a predominant contributor to the global disease burden by 2030. The comprehensive management of vascular depression entails not only the use of antidepressants but also fundamental interventions. The development of a novel molecule based on thietane-containing heterocycles, merging the attributes of an antidepressant and an antiplatelet agent, holds promise for enhancing therapeutic efficacy in patients with acute cerebrovascular accidents through multimodal action.

   Objective is to conduct a preclinical assessment of 4-(2-(4-nitrophenyl)-2-oxoethyl)-1-(thietane-3-yl)-1H-1,2,4-triazole-4-th bromide concerning model thrombosis in rats.

   Materials and Methods. The investigation involved the evaluation of thrombosis processes and the haemostasis system in rats subjected to complete occlusion of the inferior vena cava within 24 hours post-thrombosis induction. Techniques employed included thromboelastography, Born aggregometry, standard clotting assays to appraise the coagulation facet of haemostasis, and morphological examinations.

   Results. The results demonstrate that 4-(2-(4-nitrophenyl)-2-oxoethyl)-1-(thietane-3-yl)-1H-1,2,4-triazole-4-th bromide mitigates thrombosis mass, restores platelet hyper aggregation, and counters hypercoagulation observed in acute inferior vena cava thrombosis in rats. Comparative analysis with reference drugs substantiates the superior effectiveness of the chosen compound in thrombosis prevention.

   Conclusion. The preclinical investigation of 4-(2-(4-nitrophenyl)-2-oxoethyl)-1-(thietane-3-yl)-1H-1,2,4-triazole-4-th bromide unveils a fusion of established antidepressant and antithrombotic activities, laying groundwork for further drug development endeavours.

About the Authors

Yi Wang
Hangzhou Normal University
China

Yi Wang, PhD, Professor

Institute of Pharmacy

Hangzhou



N. R. Bulatova
The University of Jordan
Jordan

Nailya R. Bulatova, PhD, MD, Professor of Pharmacology and Therapy

Institute of Pharmacy; Department of Biopharmacy and Clinical Pharmacology

Amman



E. E. Klen
Bashkir State Medical University
Russian Federation

Elena E. Klen, Doctor of Pharmaceutical Sciences, Professor, Head of the Department

Department of Pharmaceutical Chemistry with a course in Analytical and Toxicological Chemistry

Ufa



G. A. Rozit
Bashkir State Medical University
Russian Federation

Galina A. Rozit, Head of the Laboratory

Laboratory of Small Targeted Molecules

Ufa



I. L. Nikitina
Bashkir State Medical University
Russian Federation

Irina L. Nikitina, Doctor of Medical Sciences, Professor

Department of Pharmacology with a course of Clinical Pharmacology

Ufa



L. V. Startseva
Bashkir State Medical University
Russian Federation

Lyudmila V. Startseva, Candidate of Pharmaceutical
Sciences, Associate Professor

Department of Pharmacology with a course of Clinical Pharmacology

Ufa



Yu. A. Bogdanova
Bashkir State Medical University
Russian Federation

Yulia A. Bogdanova, Candidate of Pharmaceutical Sciences, Associate Professor

Department of Pharmacology with a course of Clinical Pharmacology

Ufa



V. S. Shchekin
Bashkir State Medical University
Russian Federation

Vlas S. Shchekin, Head of the laboratory

scientific and morphological laboratory

Ufa



A. V. Samorodov
Bashkir State Medical University
Russian Federation

Aleksandr V. Samorodov, Doctor of Medical Sciences,
Head of the Department

Department of Pharmacology with a Course of Clinical Pharmacology

450008; Lenina str., 3; Ufa



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Review

For citations:


Wang Y., Bulatova N.R., Klen E.E., Rozit G.A., Nikitina I.L., Startseva L.V., Bogdanova Yu.A., Shchekin V.S., Samorodov A.V. Efficacy of 4-(2-(4-nitrophenyl)-2-oxoethyl)-1-(thietane-3-yl)-1h-1,2,4-triazol-4 bromide in the rat model of inferior vena cava thrombosis. Translational Medicine. 2024;11(1):19-27. https://doi.org/10.18705/2311-4495-2024-11-1-19-27. EDN: AMKUTB

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ISSN 2311-4495 (Print)
ISSN 2410-5155 (Online)