Investigation of the Antihypoxic Properties of New Nicotinic Acid Derivatives

Yasnetsov, Vik.V.; Kaurova, Diana E.; Bersenev, E.Yu.; Skachilova, S. Ya.

doi:10.21687/0233-528x-2020-54-5-73-76

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“…The choice of doses of the studied compounds was dictated by the results of previous experiments, in particular, to study their antihypoxic activity (Yasnetsov et al 2020).…”

Section: Experimental Methodsmentioning

confidence: 99%

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Antiamnestic effect of new nicotinic acid derivatives

Yasnetsov¹,

Kaurova²,

Skachilova³

et al. 2021

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Introduction: The search for new drugs for the prevention and treatment of vascular cognitive disorders continues to be a relevant task of pharmacology. In this regard, the aim of this work is to study the antiamnestic effect of five new nicotinic acid derivatives in comparison with the well-known drug mexidol (ethylmethylhydroxypyridine succinate) in animals. Materials and methods: The experiments were carried out on white male mice using conditioned passive avoidance reflex (CPAR). Electroconvulsive shock (ECS), scopolamine administration, and acute hypoxia in a hermetic chamber were used as amnesic effects. Testing for the safety of CPAR was performed 24 h after amnesic exposure. The new substances, reference drug mexidol, and a 0.9% sodium chloride solution (control group) were administered once intraperitoneally 60 min before mice training. Results and discussion: Three of the five new nicotinic acid derivatives, LKhT 4-19 (100 mg/kg), LKhT 6-19 (25, 50, and 100 mg/kg), and LKhT 7-19 (100 mg/kg), have antiamnestic properties on models of amnesia in mice induced by ESC, scopolamine, and acute hypoxia in a hermetic chamber. At the same time, the most efficient substance – LKhT 6-19 – exceeds the reference drug mexidol on all three models used. In addition, this compound is also more efficient than two other new compounds, LKhT 4-19 and LKhT 7-19, on the model of ESC-induced amnesia and LKhT 7-19 on the scopolamine-induced amnesia model. Conclusion: Compound LKhT 6-19 is promising for further advanced preclinical studies as a potential drug with antiamnestic activity. Graphical abstract:

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“…The choice of doses of the studied compounds was dictated by the results of previous experiments, in particular, to study their antihypoxic activity (Yasnetsov et al 2020).…”

Section: Experimental Methodsmentioning

confidence: 99%

“…We have previously shown that one of the five new nicotinic acid derivatives, LKhT 6-19, was the most efficient on a model of acute hypoxia in a hermetic chamber in mice. This derivative provided an action depending on the dose, surpassing the severity of the effect of the wellknown domestic drug mexidol (Yasnetsov et al 2020).…”

Section: Introductionmentioning

confidence: 99%