T2R134 Activators

Chemical activators of T2R134 are diverse in structure yet united in their ability to elicit bitter taste perception through receptor activation. Denatonium Benzoate, known for its potent bitterness, directly engages T2R134 by binding to the receptor's ligand-binding domain, initiating a cascade of intracellular events that culminate in the sensation of bitterness. Similarly, the alkaloid Quinine, classically associated with the bitter flavor of tonic water, binds to and changes the conformation of T2R134. This interaction triggers the associated G-protein to initiate a bitter taste signal. Propylthiouracil (PTU), a compound used in genetic taste testing, also activates T2R134 by binding to the receptor, thereby leading to the intracellular response indicative of bitter taste.

Other sweet-tasting compounds, such as Saccharin and Acesulfame Potassium, paradoxically activate T2R134 as well. These sweeteners mimic the molecular interactions that typical bitter compounds have with the receptor, leading to its activation. Sucralose, another sweetener, can similarly activate T2R134, prompting the downstream signaling molecules involved in bitter taste perception. Phenylthiocarbamide (PTC), a substance that tastes bitter to some individuals based on genetic variance, activates T2R134 through its interaction with the receptor's taste-specific active site, signaling its characteristic bitter taste. The toxin Strychnine, though poisonous, serves as a direct activator of T2R134 by binding to the receptor and inducing the signaling pathway associated with bitterness. Additionally, compounds such as Aloin, Capsaicin, and Magnesium Sulfate, though varied in their typical taste profiles or uses, are capable of activating T2R134 by binding to specific sites on the receptor, which leads to the activation of the G-protein and the perception of bitterness. Lastly, Caffeine, known for its stimulant effects and bitter flavor, activates T2R134 by engaging with the receptor's ligand-binding domain, stimulating the signal transduction mechanisms that result in the sensation of bitterness.