Serotonergic dysfunction is mainly associated with neuropsychiatric and cardiovasculardisorders but has also been linked with many other pathological conditions. Serotonin (5-hydroxytryptamine, 5-HT) mediates numerous physiological functions in the brain and theperiphery by activating a variety of receptors. 5-HT receptors are divided into four classes,three of which belong to the G protein-coupled receptor family. This review provides anoverview of the recent pharmacological developments involving the Gq-coupled 5-HT2receptor subfamily as well as the pathological implications of this receptor subfamily withregard to fibrosis, the central nervous system, cardiovascular disorders and cancer. The finalsection highlights new therapeutic opportunities and emerging research revealing unexploredmedical opportunities for this class of 5-HT receptors. The development of biased 5-HT2receptor ligands appears to be an interesting topic in various areas. In light of recentdiscoveries, the need for the development of new and safer drugs should take into accountthe risk of cardiovascular side effects such as pulmonary hypertension and heart valvedisease.