Study of analgesic and myotropic spasmolytic activity of alkylcarb




alkylamides of dihydroquinoline-3-carboxylic acid, non-narcotic analgesics, antispasmodics, alkylcarb


The work is devoted to the search for new biologically active substances in a series of alkylamides of dihydroquinoline-3-carboxylic acid. Analgesic properties of 30 newly synthesized substances were studied, which made it possible to identify the leader compound (provisional name alkylcarb) and recommend its effectiveness for further research as an antispasmodic agent for pain relief. It has been established experimentally, that the substance alkylcarb exhibits concentration-dependent vasodilatory properties in vitro on segments of the thoracic aorta of rats. The data, obtained in the work, justify the prospect of using the leader substance as a new analgesic and antispasmodic drug. The research expands and deepens knowledge about the pharmacological properties of alkylamide derivatives of dihydroquinoline-3-carboxylic acid.

The aim of the work was to conduct screening studies to establish the analgesic activity of a newly synthesized series of chemical compounds among alkylamides of dihydroquinoline-3-carboxylic acid and to study the myotropic spasmolytic activity of the leader substance.

Materials and methods. Analgesic properties of alkylamides of dihydroquinoline-3-carboxylic acid were studied on outbred white mice in the "acetic acid convulsions" test. During the experiment, the animals were treated in accordance with the International Principles of the European Convention for the Protection of Vertebrate Animals Used for Experiments and Other Scientific Purposes (Strasbourg, March 18, 1986). The studied substances were administered intragastrically to experimental animals at a dose of 10 mg/kg in the form of a finely dispersed aqueous suspension, stabilized with Tween-80. Voltaren at a dose of 8 mg/kg, recommended for preclinical studies, and analgin at a dose of 50 mg/kg were chosen as reference drugs.

The studies of the contractile activity of smooth muscle vessels were carried out on segments of the thoracic aorta of rats of both sexes weighing 180-200 g. The studies of dilator reactions were carried out against the background of preliminary contraction with phenylephrine at a concentration of 10-6 mol/l. The antispasmodic efficiency of the new compound was determined in comparison with the classic antispasmodic drotaverine.

The statistical processing of the results was carried out using the package of statistical analysis of electronic spreadsheets Exel, with the help of the program "Statgraphics Plus v. 3.0.” and the standard package of statistical programs "Statistica, V. 6.0". We used the Student's test, a non-parametric analog of univariate variance analysis - the Kruskal-Wallis test, and the Mann-Whitney test. Differences were considered statistically significant at p<0.05.

Results. The study of the analgesic activity of substances АO1-АO30 in the "acetic acid convulsion" test in mice showed that a compound АO26 (provisional name alkylcarb) has the most pronounced analgesic activity when administered intragastrically. In the "acetic acid convulsion" test, alkylcarb (10 mg/kg, per os) probably reduces the number of convulsions, caused by acetic acid. The level of activity of this compound is comparable to the activity of diclofenac (8 mg/kg, per os) and exceeds analgin (50 mg/kg, per os). The substance alkylcarb relieved vasospasm at the level of the comparison drug drotaverine in in vitro experiments on a model of an isolated fragment of the thoracic aorta of rats against the background of previous constriction with phenylephrine.

Conclusion. Today, the search for new highly effective non-opioid analgesics is an urgent problem of modern pharmacology, since painkillers used in clinical practice do not meet the requirements of efficiency and safety. In this regard, in recent years, scientists of the National Pharmaceutical University have been intensively searching for new, highly effective substances with antinociceptive, anti-inflammatory and antipyretic effects among alkylamides of dihydroquinoline-3-carboxylic acid.

Author Biographies

Olga Naboka, National University of Pharmacy

Doctor of Biological Sciences, Professor

Department of Biochemistry

Alla Kotvitska, National University of Pharmacy

Doctor of Pharmaceutical Sciences, Professor, Rector

Alina Volkova, National University of Pharmacy

PhD, Associated Professor, Head of Department

Departments of Social Pharmacy

Oksana Tkachenko, National University of Pharmacy

PhD, Assistant

Department of Biological Chemistry

Yuliya Voronina-Tuzovskykh , T. H. Shevchenko National University «Chernihiv Colehium»


Department of Chemistry, Technology and Pharmacy

Olga Filiptsova, National University of Pharmacy

Doctor of Biological Sciences, Professor

Department of Cosmetology and Aromology


  1. Dmytriiev, D. V., Dmytriieva, K. Yu., Semenenko, A. I., Moravska, O. A. (2017). Multimodal analgesia as a method of removal of post–operation intra–abdominal hypertension in children. Klinicheskaia Khirurgiia, 8, 59. doi:
  2. Imanaeva, A. Ia., Zalialiutdinova, L. N., Tcyplakov, D. E. (2013). Izuchenie protivovospalitelnoi aktivnosti lipoevoi kisloty na modeli adiuvantindutcirovannogo artrita krys. Biologicals ciences. Fundamental research, 6, 596.
  3. WHO Collaborating Centre for Drug Statistics Methodology. Available at:
  4. Derzhavnyi reiestr likarskykh zasobiv Ukrainy. Available at:
  5. Valeeva, I. Kh., Zaganshina, L. E., Khaziakhmetova, V. N., Titarenko, A. F. (2011). Dimefosfon proiavliaet protivovospalitelnuiu i antioksidantnuiu aktivnost na modeli khronicheskogo autoimmunnogo vospaleniia. Eksperimentalnaia i klinicheskaia farmakologiia, 3, 13–16.
  6. Jiang, B., Huang, X., Yao, H., Jiang, J., Wu, X., Jiang, S., Wang, Q., Lu, T., Xu, J. (2014). Discovery of potential anti-inflammatory drugs: diaryl-1,2,4-triazoles bearing N-hydroxyurea moiety as dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase. Organic & Biomolecular Chemistry, 12 (13), 2114–2127. doi:
  7. Pattan, S., Gadhave, P., Tambe, V. et al. (2012). Synthesis and evaluation of some novel 1,2,4-triazole derivatives for antimcrobial, antitubercular and antiinflamatory activities. Indian Journal of Chemistry, 51B, 297–301.
  8. Ukrainetc, I. V., Sidorenko, L. V., Davidenko, A. A., Iarosh, A. K. (2010). Gidrokhloridy alkilamino-alkilamidov 1-allil-4-gidroksi-6,7-dimetoksi-2-okso-1,2-digidrokhinolin-3-karbonovoi kisloty – novyi klass antagonistov opioidnykh retceptorov. Khimiia geterotciklicheskikh soedinenii, 4, 560–568.
  9. Ukrainetc, I. V., Berezniakova, N. L., Davidenko, A. A., Slobodzian, S. V. (2009). Issledovanie reaktcii etilovykh efirov 1-alkilzameshchennykh 4-gidroksi-2-okso-1,2-digidrokhinolin-3-karbonovykh kislot s fosfora oksitrikhloridom. Khimiia geterotciklicheskikh soedinenii, 8, 1198–1203.
  10. Stefanov, A. V. (Ed.) (2001). Metodychni vkazivky po doklinichnomu vyvchenniu likarskykh zasobiv. Kyiv, 567.
  11. Kim, J., Lee, Y. R., Lee, C.-H., Choi, W.-H., Lee, C.-K., Kim, J. et al. (2005). Mitogen-activated protein kinase contributes to elevated basal tone in aortic smooth muscle from hypertensive rats. European Journal of Pharmacology, 514 (2-3), 209–215. doi:
  12. Rebrova, O. Iu. (2002). Statisticheskii analiz meditcinskikh dannykh. Primenenie paketa prikladnykh programm STATISTICA. Moscow: MediaS-fera, 312.
  13. Lapach, S. N., Chubenko, A. V., Babich, P. N. (2001). Statisticheskie metody v mediko-biologicheskikh issledovaniiakh s ispolzovaniem Excel. Kyiv: Morion, 408.
  14. Vakhnina, N. H. (2016). Research of relationship «structure – anti-inflammatory effect» and «structure– analgesic effect» among amide derivatives of malonic and oxalic acids. Pharmaceutical Review, 4, 5–10. doi:
  15. Сhaparro, M., Gisbert, J. P. (2015). New molecules in the treatment of inflammatory bowel disease. Gastroenterol Hepatol, 26, 210–215.
  16. Seyed Mirzaei, S. M., Zahedi, M. J., Shafiei Pour, S. (2015). Non-Steroidal Antiinflammatory Drug Related Peptic Ulcer Disease in Patients Referred to Afzalipour Hospital. Middle East Journal of Digestive Diseases, 7 (4), 241–244.




How to Cite

Naboka, O., Kotvitska, A., Volkova, A., Tkachenko, O., Voronina-Tuzovskykh , Y., Filiptsova, O., & Pasynchuk, I. (2023). Study of analgesic and myotropic spasmolytic activity of alkylcarb. ScienceRise: Biological Science, (2(35), 4–11.



Biological research