RX77368

RX77368 is a potent and metabolically stable synthetic analog of thyrotropin-releasing hormone (TRH). Chemically structured as L-pyroglutamyl-L-histidyl-3,3-dimethylprolinamide, it acts as an agonist at TRH receptors. Unlike endogenous TRH, RX77368 is highly resistant to enzymatic degradation by TRH-degrading ectoenzyme, making it a critical tool in neuroscience and cardiovascular research for studying the central effects of TRH. Central administration of RX77368, typically via intracisternal or intrathecal injection, triggers intense sympathetic nervous system activation. This leads to significant physiological responses, including increased blood pressure, tachycardia, and stimulation of gastric acid secretion. In disease models, such as the Goto-Kakizaki (GK) rat model of type 2 diabetes, RX77368 has been used to demonstrate that overactivation of brainstem TRH-containing pathways contributes to cardiovascular morbidity and mortality through mechanisms involving peripheral oxidative stress and the renin-angiotensin system.

Other names

L-pyroglutamyl-L-histidyl-3,3-dimethylprolinamidepGlu-His-3,3'-dimethyl-Pro-NH2TRH analog RX77368