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

Abstract:

: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.

journal_name

Bioorg Med Chem Lett

authors

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

doi

10.1016/j.bmcl.2006.04.086

subject

Has Abstract

pub_date

2006-08-01 00:00:00

pages

4071-4

issue

15

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(06)00525-7

journal_volume

16

pub_type

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