It depends on the receptor and ligand. In some cases, the binding is not strong and easily reversed. The ligand will bind and release over and over, and you'd need a high concentration of ligand to be effective. In other cases, the ligand binds and isn't released until after the ligand-receptor complex is internalized and either split up by an enzymatic reaction that allows the receptor to be recycled, or the whole ligand-receptor complex is metabolized.