Diverse analgesic effects of novel benzimidazole derivatives
- 作者: Pridvorov G.V.1,2, Spasov A.A.1, Ganapolsky V.P.2,3, Dulimova A.D.1, Mukha O.Y.1
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隶属关系:
- Volgograd State Medical University
- Kirov Military Medical Academy
- North-Western State Medical University named after I.I. Mechnikov
- 期: 卷 16, 编号 1 (2025)
- 页面: 59-68
- 栏目: Original studies
- URL: https://journals.eco-vector.com/pediatr/article/view/681696
- DOI: https://doi.org/10.17816/PED16159-68
- EDN: https://elibrary.ru/IDVZUA
- ID: 681696
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BACKGROUND: The development of novel analgesics is a critical priority due to the high prevalence of pain-related pathologies and the limitations of current treatments, which are often associated with undesirable side effects.
AIM: This study aimed to evaluate the analgesic properties of new imidazobenzimidazole (BIF-70 and BIF-72) derivatives through in vivo testing, compare their efficacy with previously studied compounds, and assess potential aversive effects.
MATERIALS AND METHODS: Experiments were conducted on mature rats sourced from the Rappolovo nursery (Leningrad Region). Analgesic activity was assessed using models of somatic, inflammatory, and neurogenic pain, following guidelines for preclinical studies. The animals were divided into 3 groups. Analgesic efficacy was tested using the Plantar Test. Acute inflammation was induced via the formalin hyperalgesia model. Neurogenic pain was modeled through sciatic nerve injury. Aversive effects were evaluated using the conditioned place avoidance test. Statistical analysis was performed using two-factor ANOVA.
RESULTS: The compounds demonstrated high analgesic activity, comparable to morphine. BIF-70 exhibited activity in both phases of inflammation, surpassing butorphanol in the first phase. BIF-72 showed no activity in the first phase but outperformed butorphanol in the second phase. In the neurogenic pain model Both compounds were less effective than gabapentin but comparable to morphine. In addition, BIF-70 induced a euphoric effect, increasing the time spent in the chamber associated with its administration. In contrast, BIF-72 showed no aversive or rewarding effects.
CONCLUSIONS: The study identified new analgesics with efficacy comparable to classical drugs in certain models. Notably, these compounds lacked the aversive effects typically associated with kappa-opioid agonists, highlighting their potential as promising therapeutic candidates.
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作者简介
Gleb Pridvorov
Volgograd State Medical University; Kirov Military Medical Academy
Email: gleb.pridvorov@gmail.com
ORCID iD: 0000-0002-8070-693X
SPIN 代码: 7998-0743
Lecturer of the Department of Pharmacology, Kirov Military Medical Academy; assistant of the Department of Pharmacology and Bioinformatics, Volgograd State Medical University, Ministry of Health of the Russian Federation
俄罗斯联邦, Volgograd; Saint PetersburgAlexander Spasov
Volgograd State Medical University
Email: aspasov@mail.ru
ORCID iD: 0000-0002-7185-4826
SPIN 代码: 8777-1303
MD, Dr. Sci. (Medicine), Professor, Academician of the Russian Academy of Sciences, Head of the Department of Pharmacology and Bioinformatics
俄罗斯联邦, VolgogradVyacheslav Ganapolsky
Kirov Military Medical Academy; North-Western State Medical University named after I.I. Mechnikov
编辑信件的主要联系方式.
Email: ganvp@mail.ru
ORCID iD: 0000-0001-7685-5126
SPIN 代码: 9872-8841
MD, Dr. Sci. (Medicine), Associate Professor, Acting Head of the Department of Pharmacology, Kirov Military Medical Academy; Professor of the Department of Pharmacology nd Pharmacy, North-Western State Medical University named after I.I. Mechnikov, Ministry of Health of the Russian Federation
俄罗斯联邦, Saint Petersburg; Saint PetersburgAnastasiya Dulimova
Volgograd State Medical University
Email: bellochka0805@mail.ru
student
俄罗斯联邦, VolgogradOlga Mukha
Volgograd State Medical University
Email: olay.myha14@gmail.com
ORCID iD: 0000-0002-0429-905X
SPIN 代码: 2610-9280
Laboratory Technician of the Department of Pharmacology and Bioinformatics
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