The therapeutic potential of Convolvulus prostratus Forssk (C. prostratus) has been valued in traditional medicine for years, and its immense pharmacological properties have recently been revealed. Phytochemicals such as Ayapanin, Scopoletin, Scopolin, Convolamine, Convolidine, etc., are present in C. prostratus and possess interesting medicinal properties, including memory enhancement and neuroprotective abilities. This article provides a brief overview of the biological activities of each phytochemical present in the plant, based on existing information in public databases. This review also delves into the diverse therapeutic potential of C. prostratus, especially related to neuropharmacological properties, by referencing existing preclinical in vitro and in vivo studies. This data not only provide the ground knowledge of the therapeutic potential of the plant but also reinforce the need for further preclinical and clinical studies to explore the full spectrum of the plant’s medicinal activities.