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 Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Naydenova ED,Zhivkova VI,Zamfirova RN,Vezenkov LT,Dobrinova YG,Mateeva PIdoi
10.1016/j.bmcl.2006.04.086subject
Has Abstractpub_date
2006-08-01 00:00:00pages
4071-4issue
15eissn
0960-894Xissn
1464-3405pii
S0960-894X(06)00525-7journal_volume
16pub_type
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