Editor-in-Chief İlkay Küçükgüzel Associate Editor Aslı Türe Online ISSN 2630-6344 Publisher Marmara University Frequency Bimonthly (Six issues / year) Abbreviation J.Res.Pharm. Former Name Marmara Pharmaceutical Journal
Journal of Research in Pharmacy 2020 , Vol 24 , Issue 2
The effect of 3,7-diazabicyclo[3.3.1]nonanes containing monoterpenoid moieties on the physical activity of mice
Anastasiya A. KOTLYAROVA3,Konstantin Yu. PONOMAREV1,Ekaterina A. MOROZOVA1,Dina V. KORCHAGINA2,Evgeniy V. SUSLOV1,Alla V. PAVLOVA1,Tatyana G. TOLSTIKOVA1,Konstantin P. VOLCHO1,Nariman F. SALAKHUTDINOV1
1Department of Medicinal Chemistry, Novosibirsk Institute of Organic Chemistry of Siberian Branch of Russian Academy of Sciences, Lavrentjev av. 9, 630090, Novosibirsk, Russia
2Department of Physical Organic Chemistry, Novosibirsk Institute of Organic Chemistry of Siberian Branch of Russian Academy of Sciences, Lavrentjev av. 9, 630090, Novosibirsk, Russia
3Department of Experimental Pharmacology, Research Institute of Clinical and Experimental Lymphology - a branch of the Institute of Cytology and Genetics of Siberian Branch of Russian Academy of Sciences, Acad. Timakova str., 2, 630060, Novosibirsk, Russia
DOI : 10.35333/jrp.2020.136 The aim of this work is to study the effect of agents combining fragments of monoterpenoids and 3,7-diazabicyclo[3.3.1]nonane (bispidine) on the performance of mice. Physical endurance was studied using two tests: exhaustive swimming with a load of 7% of body weight (after single dosing) and exhaustive treadmill running (after single dosing and a 7-day administration). It has been shown for the first time that derivatives of monoterpenoids with 3,7-diazabicyclo[3.3.1]nonane moiety containing methyl substituents at positions 1 and 5 have a stimulatory effect on the performance of mice, which exceeds the effect of the reference drug bromantane after single dosing. Compound K1-458, which contains (–)-myrtenal residues linked to a bispidine fragment via amino groups, is the most effective in increasing the duration of running and swimming at a dose of 100 mg/kg after single intragastric administration. It has been also established that the LD50 for these compounds exceeds 1,000 mg/kg. Keywords : Actoprotectors; treadmill; bromantane; monoterpenoids; bispidine
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