Our group proposed to develop new chimeric analgesics in which opioid pharmacophores are covalently hybridized with other types of pharmacophores that positively modulate effects of the opioid part. Synergistic enhancement of opioid analgesia and/or decrease of unwanted side-effects should result from such hybridization.

It is generally accepted, that opioids and tachykinins are classified as functional antagonists. Therefore, hybridization of opioid agonist with tachykinin antagonist should result with very effective analgesics. Melanoma cancer cells overexpress tachykinin receptors. It has been already documented that tachykinin antagonists express antiproliferative properties of melanoma cells. Therefore chimeras of opioid agonists and tachykinin antagonists should express both analgesic and anticancer properties that make them ideal for cancer pain treatment.

Series of new opioid agonist-tachykinin antagonists conjugates have been developed, synthesized and tested. The affinities to opioid receptors mu and delta has been evaluated. The antiproliferative properties of new compounds has been evaluated in vitro in comparison to substance P antagonist aprepitant.

The new compounds express high affinity to opioid receptors as well as antiproliferative properties of melanoma cancer cells in vitro and they are good candidates for further studies as analgesics for cancer pain treatment.

Acknowledgement: This study has been supported by European 6^th STRIP Grant Normolife (LSHC-CT-2006-037733)

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