Synthesis and biological activity of nociceptin/orphanin FQ(1-13)NH2 analogues modified in 9 and/or 13 position.


:The purpose of the present study was the synthesis and the biological screening of new analogues of N/OFQ(1-13)NH2, the minimal sequence maintaining the same activity as the natural peptide nociceptin. In order to investigate the role of Lys, we substituted Lys at positions 9 and/or 13 by Orn, Dab (diaminobutanoic acid) or Dap (diaminopropanoic acid). The new N/OFQ(1-13)NH2 analogues exerted strong and naloxone-resistant inhibition of electrically evoked contractions of rat vas deferens. Lys replacement with Orn maintained or even enhanced the inhibitory activity, while replacements with Dab and Dap decreased inhibitory activity.


Bioorg Med Chem Lett


Naydenova ED,Zhivkova VI,Zamfirova RN,Vezenkov LT,Dobrinova YG,Mateeva PI




Has Abstract


2006-08-01 00:00:00














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