Some criteria for the evaluation of the functional importance of endogenous analogues of pharmacological drugs are proposed. For endogenous regulators, these include opposite changes in their content in opposite (patho)physiological states, accompanied by corresponding changes in the functional activity of enzymes sensitive to changes in their level; regulation of target enzymes by physiological concentrations of such endogenous compounds. The applicability of these criteria has been demonstrated using tribulin, the endogenous family of inhibitors of monoamine oxidases.