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.
Keywords
About the Authors
Yi WangChina
Yi Wang, PhD, Professor
Institute of Pharmacy
Hangzhou
N. R. Bulatova
Jordan
Nailya R. Bulatova, PhD, MD, Professor of Pharmacology and Therapy
Institute of Pharmacy; Department of Biopharmacy and Clinical Pharmacology
Amman
E. E. Klen
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
Russian Federation
Galina A. Rozit, Head of the Laboratory
Laboratory of Small Targeted Molecules
Ufa
I. L. Nikitina
Russian Federation
Irina L. Nikitina, Doctor of Medical Sciences, Professor
Department of Pharmacology with a course of Clinical Pharmacology
Ufa
L. V. Startseva
Russian Federation
Lyudmila V. Startseva, Candidate of Pharmaceutical
Sciences, Associate Professor
Department of Pharmacology with a course of Clinical Pharmacology
Ufa
Yu. A. Bogdanova
Russian Federation
Yulia A. Bogdanova, Candidate of Pharmaceutical Sciences, Associate Professor
Department of Pharmacology with a course of Clinical Pharmacology
Ufa
V. S. Shchekin
Russian Federation
Vlas S. Shchekin, Head of the laboratory
scientific and morphological laboratory
Ufa
A. V. Samorodov
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