On the relationship between incorporation of32P into phospholipids and binding of beta-adrenoceptor blocking drugs to isolated mast cells

The lipophilic beta-adrenoceptor blocking drugs exaprolol and propranolol significantly decreased the incorporation of³²P into phosphatidylethanolamine, phosphatidylcholine and phosphatidylinositol of isolated rat mast cells. In contrast, the hydrophilic drugs metipranolol, practolol and atenolol increased the incorporation of³²P into phosphatidylethanolamine, phosphatidylserine and phosphatidylinositol. The inhibition of³²P incorporation by lipophilic drugs correlated with the high binding of these drugs to mast cells.