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”.
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References
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 306:113–118
Brantl V (1984) Novel opioid peptides derived from human β-caein: human β-casomorphins. Eur J Pharmacol 106:213–214
Brantl V, Teschemacher H, Henschen A, Lottspeich F (1979) Novel opioid peptides derived from casein (β-casomorphins). Hoppe-Seyler's Z Physiol Chem 360:1211–1216
Brantl V, Teschemacher H, Bläsig J, Henschen A, Lottspeich F (1981) Opioid activities of β-casomorphins. Life Sci 28:1903–1909
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 3:793–797
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 243:171–177
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 36:510–523
Feldman H (1972) Mathematical theory of complex ligand-binding systems at equilibrium: some methods for parameter fitting. Anal Biochem 48:317–338
Feldman H, Rodbard D, Levine D (1972) Mathematical theory of cross-reactive radioimmunoassay and ligand-binding systems at equilibrium. Anal Biochem 45:530–556
Greenberg R, Groves ML, Dower HJ (1984) Human β-casein. Amino acid sequence and identification of phosphorylation sites. J Biol Chem 259:5132–5138
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 39:398–413
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 122:265–269
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 319:197–205
McIntosh JEA, McIntosh RP (1980) Mathematical modelling and computers in endocrinology. Springer-Verlag. Berlin Heidelberg New York, pp 250–260
Morley JE (1982) Food peptides. A new class of hormones? JAMA 247:2379–2380
Munson PJ, Rodbard D (1980) LIGAND: A versatile computerized approach for characterization of ligand-binding systems. Anal Biochem 107:220–239
Paterson SJ, Robson LE, Kosterlitz HW (1983) Classification of opioid receptors. Br Med Bull 39:31–36
Pert CB, Snyder SH (1973) Opiate receptor demonstration in nervous tissue. Science 179:1011–1014
Schulz R, Goldstein A (1972) Inactivity of narcotic glucuronides as analgesics and on guinea-pig ileum. J Pharmacol Exp Ther 183:404–410
Toll L, Keys C, Polgar W, Loew G (1984) The use of computer analysis in describing multiple opiate receptors. Neuropeptides 5:205–208
Yoshikawa M, Yoshimura T, Chiba H (1984) Opioid peptides from human β-casein. Agric Biol Chem 48:3185–3187
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Koch, G., Wiedemann, K. & Teschemacher, H. Opioid activities of human β-casomorphins. Naunyn-Schmiedeberg's Arch. Pharmacol. 331, 351–354 (1985). https://doi.org/10.1007/BF00500818
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DOI: https://doi.org/10.1007/BF00500818