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Study in vitro and in vivo of nociceptin/orphanin FQ(1-13)NH2 analogues substituting N-Me-Gly for Gly2 or Gly3.

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Date
2004-08
Authors
Chen, Li-xiang
Fang, Quan
Chen, Qiang
Guo, Jia
Wang, Zhuan-zi
Chen, Yong
Wang, Rui
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Abstract
In the present study, two analogues containing N-Me-Gly (Sarcosine, Sar) were synthesized to further investigate the structural-activity relationships of orphanin FQ/nociceptin (OFQ/NC, NC). The replacement of Gly(2) or Gly(3) with Sar increased the flexibility and decreased the hydrophobicity of the N-terminal tetrapeptide. The activity of the analogues was investigated in a series of assays in vivo and in vitro. [Sar(2)]NC(1-13)NH(2) was found to (1) produce dose-dependent inhibition of the electrically induced contraction in MVD assay (pEC(50) = 6.14); (2) produce significant hyperalgesia effects in a dose-dependent manner when intracerebroventricularly (i.c.v.) injected in mice. The inhibitive effects of [Sar(2)]NC(1-13)NH(2) in MVD assay could be significantly antagonized by [Nphe(1)]NC(1-13)NH(2), and partially antagonized by naloxone; the hyperalgesic effect of [Sar(2)]NC(1-13)NH(2) could be significantly antagonized by naloxone, and partially antagonized by [Nphe(1)]NC(1-13)NH(2). On the contrary, [Sar(3)]NC(1-13)NH(2) showed no effects in these assays. All the findings suggest that the flexibility of the peptide bond between Phe(1) and Gly(2) and between Gly(2) and Gly(3) play an important role in NC-OP(4) receptor interaction, and the hydrophobicity of the N-terminal tetrapeptide showed no significant effect on this interaction. The present work also helps to provide a novel method to elucidate structural and conformational requirements of the opioid peptide-receptor interaction.
Type
Journal article
Subject
Amino Acid Substitution
Animals
Glycine
Male
Mice
Oligopeptides
Opioid Peptides
Pain Measurement
Sarcosine
Structure-Activity Relationship
Vas Deferens
Permalink
https://hdl.handle.net/10161/13664
Published Version (Please cite this version)
10.1016/j.peptides.2004.05.012
Publication Info
Chen, Li-xiang; Fang, Quan; Chen, Qiang; Guo, Jia; Wang, Zhuan-zi; Chen, Yong; & Wang, Rui (2004). Study in vitro and in vivo of nociceptin/orphanin FQ(1-13)NH2 analogues substituting N-Me-Gly for Gly2 or Gly3. Peptides, 25(8). pp. 1349-1354. 10.1016/j.peptides.2004.05.012. Retrieved from https://hdl.handle.net/10161/13664.
This is constructed from limited available data and may be imprecise. To cite this article, please review & use the official citation provided by the journal.
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Scholars@Duke

Chen

Yong Chen

Associate Professor in Neurology
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