Nociceptin and Pilot Experiments to Detect Pharmacological Effects of its Short-Chain Analogues

Abstract

Nociceptin, or orphanin FQ, is an endogenous ligand for the nociceptin receptor (NOP, ORL-1). It is a potent antianalgesic agent. The receptor is widely distributed in brain structures. Peptidomimetics are short-chain molecules designed to mimic peptides and with typical pharmacokinetic properties. The aim of the study is to investigate the basic pharmacological and toxicological effects of two newly-synthesized neuropeptides (P1 and P2) in mice. Their activity on the CNS and their inf luence on the hexobarbital- induced narcosis as well were studied. The analgesic activity of these two compounds was examined by using acetic acid test. Dose-dependent effect of the analgesic activity of compound P2 was independently studied by means of the same method. It was established that P2 possessed antinociceptive properties which makes it suitable for further research in this direction

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