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

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Abstract

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.

About the authors

S. V. Chepur

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

Author for correspondence.
Email: gniiivm_15@mil.ru

Chepur Sergei Viktorovich

195043, Saint Petersburg

Russian Federation

S. E. 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

Russian Federation

M. S. 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

Russian Federation

R. N. 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

Russian Federation

A. N. 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

Russian Federation

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Copyright (c) 2020 Chepur S.V., Galan S.E., Vakhviayanen M.S., Khromov R.N., Semenov A.N.



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