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 Citations (Scopus)

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

Fingerprint

Cholecystokinin B Receptor
Cholecystokinin
Opioid Receptors
Inhibitory Concentration 50
Analgesics
Ligands
Sincalide
Ala(2)-enkephalinamide-met

Keywords

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

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

Cite this

Slaninova, J., Knapp, R. J., Wu, J., Su-Nan, F., Kramer, T., Burks, T. F., ... 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

Opioid receptor binding properties of analgesic analogues of cholecystokinin oceapeptide. / Slaninova, Jirina; Knapp, Richard J.; Wu, Jinji; Su-Nan, Fang; Kramer, Thomas; Burks, Thomas F.; Hruby, Victor J; Yamamura, Henry I.

In: European Journal of Pharmacology, Vol. 200, No. 1, 23.07.1991, p. 195-198.

Research output: Contribution to journalArticle

Slaninova, J, Knapp, RJ, Wu, J, Su-Nan, F, Kramer, T, Burks, TF, Hruby, VJ & Yamamura, HI 1991, 'Opioid receptor binding properties of analgesic analogues of cholecystokinin oceapeptide', European Journal of Pharmacology, vol. 200, no. 1, pp. 195-198. https://doi.org/10.1016/0014-2999(91)90688-M
Slaninova, Jirina ; Knapp, Richard J. ; Wu, Jinji ; Su-Nan, Fang ; Kramer, Thomas ; Burks, Thomas F. ; Hruby, Victor J ; Yamamura, Henry I. / Opioid receptor binding properties of analgesic analogues of cholecystokinin oceapeptide. In: European Journal of Pharmacology. 1991 ; Vol. 200, No. 1. pp. 195-198.
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