The clinical treatment of various types of pain relies upon opioid analgesic, however most of them produce, in addition to the analgesic effect, several side effects such as development of dependence and addiction as well as sedation, dysphoria, and constipation. One of the solutions to these problems are chimeric compounds in which opioid pharmacophore is hybridized with other type of synergically active antinociceptor. Neurotensin-induced antinociception is not mediated through the opioid system. Therefore, hybridizing neurotensin with opioid element results in a potent synergic antinociceptor.

Indeed, previously synthesized and examined an opioid-neurotensin hybrid peptide PK20 is a highly potent analgesic. Our in vivo studies have shown that PK20 treatment results in long-standing time-dependent antinociception while administered centrally as well as peripherally. This novel opioid-neurotensin hybrid peptide has a significantly intensified analgesic effect, when compared to morphine. The metabolic studies of PK20 indicated formation of quite stable N-terminal tetrapeptide. To evaluate its pharmacological profile the compound (metabolite) has been de novo synthesized and exposed to both in vitro and in vivo studies, which indicated that this compound expresses a high analgesic activity.

Fig. Degradation of PK20 in human plasma

Acknowledgement: This study has been supported by European 6^th  SPTRIP Grant

                                 Normolife (LSHC-CT-2006-037733)

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