The luteinizing and follicle-stimulating hormones and human chorionic gonadotropin are the most important regulators of the reproductive system that regulate the sexual behavior, the reproduction and many other physiological functions. In the recent years, there has been a real progress in deciphering the unique structure and mechanisms of action of gonadotropins, and their great diversity has been found, due to the high variability of N-glycosylation. The pattern of N-glycosylation changes both during the day and in ontogenesis, determining the fertility and sexual behavior. Until recently, it was believed that the production of gonadotropins is controlled by the hypothalamic factor gonadoliberin, but currently more than 20 regulators have been added to it, such as adipokines, kisspeptin, gonadotropin-inhibiting hormone, and follistatin. The interest in the extraordinary properties of gonadotropins is so great because they are indispensable in such an important area of medicine as reproduction. But their use in the clinic is associated with a number of adverse side effects, which is associated with a wide spectrum of their action. This leads to the search for their effective “substitutes”, among which the most suitable are low molecular weight agonists of the gonadotropin receptors. These and other interesting questions will be the subject of a lecture.