EXPERIMENTAL EVALUATION OF TOXICOMETRIC INDICATORS AND ANALGESIC ACTIVITY OF KAPPA-OPIOID RECEPTOR AGONISTS

Мұқаба

Дәйексөз келтіру

Толық мәтін

Аннотация

Data on the biological activity of kappa-opioid receptor agonists - derivatives of three groups of compounds: 1,2-cyclohexylamine, 1,2,3,4-piperidine, 1,2,4-piperazine are presented. On the examples of 1,2-cyclohexylamine and 1,2,4-piperazine derivatives, it has been shown that a decrease in the length of the carbon chain in the phenylalkyl substituent at the nitrogen atom is accompanied by a decrease in the analgesic activity and toxicity of compounds. The replacement of chlorine atoms in the 3 and 4 positions of the phenyl ring with fluorine atoms, which are more electronegative, leads to an increase in the analgesic effect and a decrease in the toxicity of the compounds.

Авторлар туралы

S. Chepur

State Scientific Research Testing Institute of Military Medicine, Ministry of Defence of the Russian Federation

Хат алмасуға жауапты Автор.
Email: gniiivm_15@mil.ru

Chepur Sergei Viktorovich

195043, Saint Petersburg

Ресей

S. Galan

State Scientific Research Testing Institute of Military Medicine, Ministry of Defence of the Russian Federation

Email: gniiivm_15@mil.ru

Galan Sergei Evgenievich

195043, Saint Petersburg

Ресей

M. Vakhviayanen

State Scientific Research Testing Institute of Military Medicine, Ministry of Defence of the Russian Federation

Email: gniiivm_15@mil.ru

Vakhviayanen Maria Sergeevna

195043, Saint Petersburg

Ресей

R. Khromov

State Scientific Research Testing Institute of Military Medicine, Ministry of Defence of the Russian Federation

Email: gniiivm_15@mil.ru

Khromov Roman Nikolaevich

195043, Saint Petersburg

Ресей

A. Semenov

State Scientific Research Testing Institute of Military Medicine, Ministry of Defence of the Russian Federation

Email: gniiivm_15@mil.ru

Semenov Alexander Nikolaevich

195043, Saint Petersburg

Ресей

Әдебиет тізімі

  1. Litvinov R.A. Pharmacotoxicological properties of a new kappa-opioid agonist - benzimidazole derivative: Diss. cand. med. sciences, Volgograd; 2016, 26 p. (in Russian).
  2. Raschenko A.I. Pharmacological properties of a new analgesic benzimidazole derivative: Diss. cand. pharm. sciences, Volgograd; 2014 (in Russian).
  3. Sosnov A.V., Sadovnikov S.V., Semchenko F.M. et al. Strong non-narcotic analgesics as a direction of pharmaceutical development. Development and registration of medicines. 2016;1 (14): Pp. 196-206 (in Russian).
  4. Walsh S.L., Strain E.C., Abreu M.E., Bigelow G.E. Enadoline, aselectivekappaopioidagonist: comparison with butorphanol and hydromorphone in humans. Psychopharmacol. (Berl.). 2001. 157 (2): Pp. 151162.
  5. Ranganathan M., Schnakenberg A., Skosnik P.D. et al. Dose-related behavioral, subjective, endocrine and psychophysiological effects of the k opioid agonist Salvinorin A in humans. Biol. Psychiatry.2012. 72 (10): Pp.871–879.
  6. Kasatkin I.K. ,Nazarov G.V., Galan S.E. et al. Drug synthesis methods and manufacturing technology: new method for the synthesis of methyl-4-[(3,4-dichlorophenyl)acetyl]-3-[(1-pyrrolydinil) methyl]-1-[piperazinecarboxylate]. Pharm. Chem. J. 2009. 43 (2): Pp. 115117.
  7. Bykov V.N., Anokhin A.G., Chepur S.V. et al. Research of psycholeptic effects. Toxicological Review. 2011; 3 (108): Pp. 1316 (in Russian).
  8. Roux S., Sable E., Porsolt R.D. Primary observation (Irwin) test in rodents for assessing acute toxicity of a test agents and its effects on behavior and physiological function. Curr.Protoc. Pharmacol. 2004. 27 (1):10.10.1.–10.10.23.
  9. Mulla W.A., More S.D., Jamge S.B. et al. Evaluation of anti-inflammatory and analgesic activities of ethanolic extract of roots Adhatodavasica Linn. Int. J. Pharm. Te ch. Res. 2010. 2 (2): Pp. 13641368.
  10. Finney D.J. Probit analysis, 3d ed. New York: Cambridge University Press; 1971.
  11. Lei C., Sun X. Comparing lethal dose ratios probit regression with arbitrary slopes // BMC Pharmacology and Toxicology/ 2018/ 19:61. 10 p. https://doi.org/10.1186/s40360-018-0250-1.

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© Chepur S.V., Galan S.E., Vakhviayanen M.S., Khromov R.N., Semenov A.N., 2020



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