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Designing of an orally active complement C3a agonist peptide with anti-analgesic and anti-amnesic activity.

Abstract
Complement C3a is an anti-opioid peptide, having anti-analgesic and anti-amnesic effects after intracerebroventricular administration. However, the peptide is inactive after oral administration. Orally active C3a agonist peptide was designed based on the structure of oryzatensin, a C3a agonist peptide derived from rice albumin. Tyr-Pro-Leu-Pro-Arg, a pentapeptide at the carboxyl terminus of oryzatensin is the minimally essential structure for exerting C3a activity. Due to the affinity for mu-opioid receptor, both oryzatensin and Tyr-Pro-Leu-Pro-Arg showed analgesia after intracerebroventricular administration in mice which was blocked by the opioid antagonist naloxone. Tyr-Pro-Leu-Pro-Arg lost opioid activity by substitution the amino terminus tyrosine with other hydrophobic residues. Among the newly designed peptides, Trp-Pro-Leu-Pro-Arg was found to possess the strongest C3a activity. The peptide antagonized morphine-induced analgesia at 300 mg/kg after oral administration and also improved scopolamine- and ischemia-induced amnesia in a step-through passive avoidance test.
AuthorsY Jinsmaa, Y Takenaka, M Yoshikawa
JournalPeptides (Peptides) Vol. 22 Issue 1 Pg. 25-32 (Jan 2001) ISSN: 0196-9781 [Print] United States
PMID11179594 (Publication Type: Journal Article)
Chemical References
  • Analgesics
  • Complement C3
  • Peptides
Topics
  • Administration, Oral
  • Amnesia (drug therapy)
  • Analgesia
  • Analgesics (antagonists & inhibitors)
  • Animals
  • Complement C3 (agonists)
  • Guinea Pigs
  • Male
  • Mice
  • Peptides (chemistry, pharmacology)

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