Beta-endorphin: opiate receptor binding activities of six naturally occurring beta-endorphin homologs studied by using tritiated human hormone and naloxone as primary ligands--effects of sodium ion.

摘要

Six naturally occurring homologs of beta-endorphin were tested for their potency in inhibiting the binding of [3H]naloxone and [3H]-beta h-endorphin either in the presence or in the absence of Na+. Sodium ion reduces inhibitory potency of these homologs against [3H]-beta h-endorphin and [3H]naloxone to about the same extent. The ratio of the IC50 obtained with Na+ to that obtained without Na+ is not highly correlated with analgesic potency. Very high (greater than 300) sodium ratios are observed with some homologs. A significant rank correlation was found between the ratio of the relative potency in displacing [3H]beta h-endorphin to the relative potency in analgesia and potency in inhibiting the binding of the pure antagonist naloxone.