Advertisement

Naunyn-Schmiedeberg's Archives of Pharmacology

, Volume 331, Issue 4, pp 351–354 | Cite as

Opioid activities of human β-casomorphins

  • Gertrud Koch
  • Klaus Wiedemann
  • Hansjörg Teschemacher
Article

Summary

Opioid activities of human β-casomorphin-4,-5,-7 and -8 and, for comparison, of the corresponding bovine β-casomorphins were studied in the guinea-pig ileum preparation. Binding parameters, i.e. K d -values and binding site concentrations, for the interaction of human and bovine β-casomorphins with opioid receptors in rat brain homogenates were determined in inhibition experiments, using [3H]-(d-Ala2, MePhe4, Gly-ol5)enkephalin, [3H]-(d-Ala2, d-Leu5)enkephalin and [3H]ethylketazocin as μ-, δ- and κ-opioid receptor ligands. Analysis of binding data was performed using a non-linear curve fitting program. All β-casomorphins examined displayed opioid activity. The affinity was highest for μ-receptors, less so for δ-receptors and lowest for κ-receptors. It is suggested that human β-casomorphins might play a role as “food hormones”.

Key words

Human β-casein Opioid peptides Opioid receptor ligands Human β-casomorphins Computerized binding data analysis 

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. Beubler E, Lembeck F (1979) Inhibition of stimulated fluid secretion in the rat small and large intestine by opiate agonists. Naunyn-Schmiedeberg's Arch Pharmacol 306:113–118Google Scholar
  2. Brantl V (1984) Novel opioid peptides derived from human β-caein: human β-casomorphins. Eur J Pharmacol 106:213–214Google Scholar
  3. Brantl V, Teschemacher H, Henschen A, Lottspeich F (1979) Novel opioid peptides derived from casein (β-casomorphins). Hoppe-Seyler's Z Physiol Chem 360:1211–1216Google Scholar
  4. Brantl V, Teschemacher H, Bläsig J, Henschen A, Lottspeich F (1981) Opioid activities of β-casomorphins. Life Sci 28:1903–1909Google Scholar
  5. Brantl V, Pfeiffer A, Herz A, Henschen A, Lottspeich F (1982) Antinociceptive potencies of β-casomorphin analogs as compared to their affinities towards μ- and δ-opiate receptor sites in brain and periphery. Peptides 3:793–797Google Scholar
  6. Chapman WP, Rowlands EN, Jones EM (1950) Multiple-balloon kymographic recording of the comparative action of DEMEROL, morphine and placebos on the motility of the upper small intestine in man. New Engl J Med 243:171–177Google Scholar
  7. Daniel EE, Sutherland WH, Bogoch A (and Kent JT [tech. asst.]) (1959) Effects of morphine and other drugs on motility of the terminal ileum. Gastroenterology 36:510–523Google Scholar
  8. Feldman H (1972) Mathematical theory of complex ligand-binding systems at equilibrium: some methods for parameter fitting. Anal Biochem 48:317–338Google Scholar
  9. Feldman H, Rodbard D, Levine D (1972) Mathematical theory of cross-reactive radioimmunoassay and ligand-binding systems at equilibrium. Anal Biochem 45:530–556Google Scholar
  10. Greenberg R, Groves ML, Dower HJ (1984) Human β-casein. Amino acid sequence and identification of phosphorylation sites. J Biol Chem 259:5132–5138Google Scholar
  11. Kosterlitz HW, Lyndon RJ, Watt AJ (1970) The effects of adrenaline, noradrenaline, and isoprenaline on inhibitory α- and β-adrenoceptors in the longitudinal muscle of the guinea-pig ileum. Br J Pharmacol 39:398–413Google Scholar
  12. Lutz RA, Cruciani RA, Costa T, Munson PJ, Rodbard D (1984) A very high affinity opioid binding site in rat brain: demonstration by computer modeling. Biochem Biophys Res Comm 122:265–269Google Scholar
  13. Magnan J, Paterson SJ, Tavani A, Kosterlitz W (1982) The binding spectrum of narcotic analgesic drugs with different agonist and antagonist properties. Naunyn-Schmiedeberg's Arch Pharmacol 319:197–205Google Scholar
  14. McIntosh JEA, McIntosh RP (1980) Mathematical modelling and computers in endocrinology. Springer-Verlag. Berlin Heidelberg New York, pp 250–260Google Scholar
  15. Morley JE (1982) Food peptides. A new class of hormones? JAMA 247:2379–2380Google Scholar
  16. Munson PJ, Rodbard D (1980) LIGAND: A versatile computerized approach for characterization of ligand-binding systems. Anal Biochem 107:220–239Google Scholar
  17. Paterson SJ, Robson LE, Kosterlitz HW (1983) Classification of opioid receptors. Br Med Bull 39:31–36Google Scholar
  18. Pert CB, Snyder SH (1973) Opiate receptor demonstration in nervous tissue. Science 179:1011–1014Google Scholar
  19. Schulz R, Goldstein A (1972) Inactivity of narcotic glucuronides as analgesics and on guinea-pig ileum. J Pharmacol Exp Ther 183:404–410Google Scholar
  20. Toll L, Keys C, Polgar W, Loew G (1984) The use of computer analysis in describing multiple opiate receptors. Neuropeptides 5:205–208Google Scholar
  21. Yoshikawa M, Yoshimura T, Chiba H (1984) Opioid peptides from human β-casein. Agric Biol Chem 48:3185–3187Google Scholar

Copyright information

© Springer-Verlag 1985

Authors and Affiliations

  • Gertrud Koch
    • 1
  • Klaus Wiedemann
    • 1
  • Hansjörg Teschemacher
    • 1
  1. 1.Rudolf-Buchheim-Institut für Pharmakologie der Justus-Liebig-Universität GießenGießenFederal Republic of Germany

Personalised recommendations