Opioid activities of human beta-casomorphins

Opioid activities of human beta-casomorphin-4, -5, -7 and -8 and, for comparison, of the corresponding bovine beta-casomorphins were studied in the guinea-pig ileum preparation. Binding parameters, i.e. KD-values and binding site concentrations, for the interaction of human and bovine beta-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 mu-, delta- and kappa-opioid receptor ligands. Analysis of binding data was performed using a non-linear curve fitting program. All beta-casomorphins examined displayed opioid activity. The affinity was highest for mu-receptors, less so for delta-receptors and lowest for kappa-receptors. It is suggested that human beta-casomorphins might play a role as "food hormones".