Research Article
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Year 2024, Volume: 49 Issue: 3, 465 - 480, 23.10.2024
https://doi.org/10.55262/fabadeczacilik.1417891

Abstract

Project Number

pharmacological part -grant 0122РКИ0052; synthetic (chemical) part - grants AP09057956, AP09057500

References

  • Yu, V. K., Sycheva, Y. S., Kairanbayeva, G. K., Dem- bitsky, V. M., Balabekova, M. K., Tokusheva, A. N., Seilkhanov, T. M., Zharkynbek, T. Y., Balapanova, A. K., & Tassibekov, K. S. (2023). Naphthalene- oxypropargyl-Containing Piperazine as a Regu- lator of Effector Immune Cell Populations upon an Aseptic Inflammation. Molecules (Basel, Swit- zerland), 28(20), 7023. https://doi.org/10.3390/ molecules28207023

The Local Anesthetic Activity of 4-(Naphthalen-1-yloxy)but-2-yn-1-yl)-containing Piperidine Derivatives in Experimental Animal Models

Year 2024, Volume: 49 Issue: 3, 465 - 480, 23.10.2024
https://doi.org/10.55262/fabadeczacilik.1417891

Abstract

Piperidine derivatives are of interest to researchers considering piperidines as an effective scaffold for the synthesis of new compounds. The aim of this research was to investigate the acute toxicity and local anesthetic activity of new synthesized 4-(Naphthalen-1-yloxy)but-2-yn-1-yl)-containing piperidine derivatives. Acute toxicity tests were performed on outbred laboratory mice by subcutaneous injection of increasing concentrations of the test solutions. An initial investigation of local anesthetic activity during infiltration anesthesia was performed on guinea pigs using the Bulbring & Wajda animal model. An in-depth study of the efficacy of the most active compound was performed on a model of infiltration anesthesia of the rabbit’s abdominal wall by determining the threshold of nociception during electrical stimulation. Studied new piperidine derivatives are low-toxic substances, which are confirmed by the results of an acute toxicity study. At the stage of the primary study of local anesthetic activity during infiltration anesthesia on the experimental Bulbring and Wajda model, the LAS-251 compound showed the greatest activity, surpassing the reference drugs in terms of anesthesia index, duration of full anesthesia and total duration of action. At the stage of in-depth study, despite a longer latency period, LAS-251 has a local anesthetic effect longer than procaine and is slightly inferior to lidocaine. Results of present study are promising because complex 1-(4-(naphthalen-1-yloxy)but-2-yn-1-yl)-4-phenylpiperidine (LAS-251) with cyclodextrin showed high local anesthetic activity. This new piperidine derivative is future-oriented for prospective studies of other types of anesthesia, as a potential medicinal substance for therapeutic use in the future.

Ethical Statement

The Protocol for this study has been approved and monitored by the Local Ethics Committee of Asfendiyarov Kazakh National Medical University (Protocol No.14(120), dated 10.28.2021, with the permission to extend the study - Protocol No.1(137), dated 01.31.2023).

Supporting Institution

Asfendiyarov Kazakh National Medical University (Almaty, Republic of Kazakhstan)

Project Number

pharmacological part -grant 0122РКИ0052; synthetic (chemical) part - grants AP09057956, AP09057500

References

  • Yu, V. K., Sycheva, Y. S., Kairanbayeva, G. K., Dem- bitsky, V. M., Balabekova, M. K., Tokusheva, A. N., Seilkhanov, T. M., Zharkynbek, T. Y., Balapanova, A. K., & Tassibekov, K. S. (2023). Naphthalene- oxypropargyl-Containing Piperazine as a Regu- lator of Effector Immune Cell Populations upon an Aseptic Inflammation. Molecules (Basel, Swit- zerland), 28(20), 7023. https://doi.org/10.3390/ molecules28207023
There are 1 citations in total.

Details

Primary Language English
Subjects Basic Pharmacology
Journal Section Research Article
Authors

Malika Khaiitova 0000-0001-6775-4358

Yelena Sycheva This is me 0000-0002-8409-2672

Vasılıy Trubachev This is me 0000-0002-8317-7914

Elmıra Satbayeva This is me 0000-0002-5521-5776

Valentına Yu This is me 0000-0001-6508-707X

Talgat Nurgozhın This is me 0000-0002-8036-604X

Edgaras Stankevıčıus This is me 0000-0003-2210-708X

Yeskendir Gassanov This is me 0000-0002-4184-4758

Zauresh Utelbayeva This is me 0000-0003-4312-9093

Khaıdar Tassıbekov This is me 0000-0002-1067-5162

Project Number pharmacological part -grant 0122РКИ0052; synthetic (chemical) part - grants AP09057956, AP09057500
Publication Date October 23, 2024
Submission Date January 20, 2024
Acceptance Date July 29, 2024
Published in Issue Year 2024 Volume: 49 Issue: 3

Cite

APA Khaiitova, M., Sycheva, Y., Trubachev, V., Satbayeva, E., et al. (2024). The Local Anesthetic Activity of 4-(Naphthalen-1-yloxy)but-2-yn-1-yl)-containing Piperidine Derivatives in Experimental Animal Models. Fabad Journal of Pharmaceutical Sciences, 49(3), 465-480. https://doi.org/10.55262/fabadeczacilik.1417891