Yadlovskyі O. The experimental and theoretical rationale for developing the potential of non-narcotic analgesics condensed derivatives of nitrogen heterocycles and their analogues.

The thesis devoted to the problem of search and development of new analgesics among of nitrogen heterocycles (pirrolo and imidazole derivatives). The PASS-prediction and its experimental verification revealed series of substances (derivatives polimetylenimydazol, 5H - pirrolo[1,3-а]imidazole) that in future investigations could to help find substances with analgesic and/or anti-inflammatory activity. The pharmacological activity of derivatives of 5H-pirrolo[1,3a]imidazole was study on the example of the most active substance of the series (Pirodazol). Substance showed anti-inflammatory and anti-pyrogenic actions, no effect to opioid system. Displaying monoaminergic component of its analgesic action associated with exposure to ?2-adrenergic CNS and ?-adrenergic receptors, and modulation of serotonin levels in the cerebral cortex and hypothalamus. Shown low probability of impact vanilloid receptor (TRPV1). The ability of agonists and antagonists of TRPV1 affect on non-opioid antinociceptive action of analgesics and NSAIDs.