Multidrug therapies become a standard of modern successful therapies in pain treatment in the clinic. However, the different pharmacodynamic profile of the drugs creates limits of using a mixture. Chimerization of tachykinin and opioid pharmacophores in one molecule is a new avenue for analgesic development. In our studies we have demonstrated  the relative balance of activities between tachykinin and opioid pharmacophores which will generally determine the net effect of the chimeric molecule as pro-nociceptive, antinociceptive, or neutral. The first combination of multiple active pharmacophores in one molecule which was performed on the SP scaffold showed high antinociceptive effect and was the starting point to design next chimeric peptide called AWL3106. The compound was a hybridized fragment of substance P(7-11) and dermorphin linked by spacer. This chimeric compound displayed analgesic effect without development of tolerance when applied iv and it in Wistar rats. The communication will present the way from an idea through synthesis to pharmacological studies and prospective application of the new chimeric compound called AWL3106 in pain therapy.

Acknowledgement: This work has been supported by 6FP STREP project “NORMOLIFE”

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