G protein coupled receptors are the largest family of receptors in the organism. When the transmitter input is significantly changed in comparison to normal condition, the homologous or heterologous regulation can occur. Homologous regulation represents the situation in which the properties of the receptor system just influenced via extracellular signalling are changed. Heterologous regulation can manifest despite that the extracellular signalling influence the receptors. It is possible to comprehend such changes as one of the level of homeostasis. Both homologous and heterologous regulations play a role in physiological and pathophysiological processes. In the basic scheme this regulations are comprehend as phosphorylation-based events. We discuss other possible pathways of receptor regulation in this review.

        Key words: G protein-coupled receptors (GPCR), homologous regulation, heterologous regulation, phosphorylation, GPCR oligomerization