Synthesis and biological activity of novel small peptides with aminophosphonates moiety as NOP receptor ligands |
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| Authors: | Emilia D Naydenova Petar T Todorov Polina I Mateeva Rositza N Zamfirova Nikola D Pavlov Simeon B Todorov |
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| Institution: | (1) Department of Organic Chemistry, University of Chemical Technology and Metallurgy, 1756 Sofia, Bulgaria;(2) Institute of Neurobiology, Bulgarian Academy of Sciences, 1113 Sofia, Bulgaria |
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| Abstract: | The aim of the present study was the synthesis and the biological screening of new analogs of Ac-RYYRWK-NH2, modified at the N-terminal with 1-(methoxyphosphono)methylamino]cycloalkanecarboxylic acids. The four newly synthesized
ligands for the nociceptin/orphanin FQ (N/OFQ) receptor (NOP) have been prepared by solid-phase peptide synthesis—Fmoc-strategy.
These compounds were tested for agonistic activity in vitro on electrically stimulated smooth-muscle preparations isolated
from vas deferens of Wistar rats. Our data showed that substitution of Arg at position 1 with aminophosphonates moiety decreased
significantly the affinity of ligands to the NOP receptor. Furthermore, the enlargement of the cycle (with 5–8 carbon atoms)
additionally diminished both the activity and the selectivity for NOP-receptor. |
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