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Osteoporosis is a chronic disease characterized by a pathological change in bone tissue, excessive fragility and a decrease in bone strength as a result of the predominance of bone resorption processes over the process of bone formation. This disease manifests in the form of low-traumatic fractures occurring in result of falling from a height of one’s height, or with little physical exertion. Osteoporosis could result in the fractures of the vertebral bodies and bones of the peripheral skeleton, causing a high level of disability. Of note, postmenopausal osteoporosis develops in women against the background of the cessation of the menstrual cycle. Here we overview the role of G-protein-associated membrane receptors (GPCR family) in the pathogenesis of this disease and the prospects for finding targets among these receptors for the diagnosis and treatment of osteoporosis. Malformations in the genes encoding GPCR lead to impaired bone tissue remodeling. Exploring the functions of GPCR family members is critical to the search for predisposition markers of bone tissue dysfunction and could improve the early diagnosis of osteoporosis. Studies on a model of osteoblasts differentiated from hIPSCs obtained from patients with osteoporosis associated with mutations in the genes of the GPCR family will allow a deeper understanding of the molecular nature of osteoporosis and the identification of new targets for osteoporosis treatment.