Opioid receptor binding properties of analgesic analogues of cholecystokinin oceapeptide

Jirina Slaninova, Richard J. Knapp, Jinji Wu, Fang Su-Nan, Thomas Kramer, Thomas F. Burks, Victor J. Hruby, Henry I. Yamamura

Research output: Contribution to journalArticle

33 Scopus citations

Abstract

Four analogues of cholecystokinin (CCK) octapeptide having analgesic activity after i.c.v. administration and high affinity for CCK-B receptors were studied for their ability to displace specific ligands,[3H]D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2. [3H]D-Pen2, 4'-Cl-Phe4,D-Pen5]enkephalin and [3H]U-69,593. for μ-, δ- and κ-opioid receptors, respectively. None of the analogues tested have high affinity for either μ- or κ-receptors (IC50 values > 0.7 μM), but their IC50 values for δ-receptors range from 29 to 1023 nM. The results suggest a relationship between the ligand requirements of CCK-B and δ-opioid receptors which further implies a possible structural relationship between these receptors.

Original languageEnglish (US)
Pages (from-to)195-198
Number of pages4
JournalEuropean Journal of Pharmacology
Volume200
Issue number1
DOIs
StatePublished - Jul 23 1991

Keywords

  • Analgesia
  • CCK analogues
  • CCK-B receptors
  • Cholecystokinin (CCK)
  • Opioid receptors
  • Radioligand binding

ASJC Scopus subject areas

  • Pharmacology

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    Slaninova, J., Knapp, R. J., Wu, J., Su-Nan, F., Kramer, T., Burks, T. F., Hruby, V. J., & Yamamura, H. I. (1991). Opioid receptor binding properties of analgesic analogues of cholecystokinin oceapeptide. European Journal of Pharmacology, 200(1), 195-198. https://doi.org/10.1016/0014-2999(91)90688-M