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

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.