Urotensin-2 receptor (UTS2R)

The **Urotensin-2 receptor** (UTS2R) is a class A, rhodopsin family G protein-coupled receptor predominantly expressed in peripheral vasculature, heart, kidney, brainstem, and other tissues[1][3][4]. It binds the neuropeptide **urotensin II** as its principal endogenous ligand, resulting in extremely potent vasoconstrictive effects—the strongest known among endogenous peptides[1]. The receptor mediates its effect via Gq/11 proteins, activating phosphoinositide and calcium second messenger pathways, which regulate vascular tone and influence neuromuscular physiology[1][3]. UTS2R signaling also affects neuroendocrine responses and REM sleep by regulating stress hormones and cholinergic neuron activity[1]. Dysregulation or overactivation of the urotensin-2 receptor has been associated with a range of cardiovascular, metabolic, neurological, and oncological disorders, making it a researched therapeutic target for antagonists aiming to mitigate its pathological signaling[2][3][5].

Other names

GPR14Urotensin II receptorUR-2-RUR-II-RUTRUTR2SenrU-II

Agonists: Bind and activate Urotensin-2 receptor, causing vasoconstriction via Gq/11 protein pathway (phosphatidylinositol-calcium second messenger system, increasing intracellular calcium)[1][3][5]. Antagonists: Block Urotensin-2 receptor activation, inhibiting downstream vasoconstriction or cellular response[5].