T2R1 Inibitori

I comuni inibitori del T2R1 includono, a titolo esemplificativo, il 6-propil-2-tiouracile CAS 51-52-5, la N-feniltiourea CAS 103-85-5, il Probenecid CAS 57-66-9, l'acesulfame di potassio CAS 55589-62-3 e la capsazepina CAS 138977-28-3.

Chemical inhibitors of T2R1 include a range of compounds that interact with the protein's receptor sites to prevent binding and recognition of bitter compounds. Propylthiouracil can inhibit T2R1 through competitive antagonism, in which it binds to receptor sites that respond to thiourea compounds. This binding prevents normal activation of T2R1 by its characteristic ligands. Phenylthiocarbamide operates by a similar mechanism, acting as a competitive inhibitor due to its structural similarity to natural ligands of T2R1, thus preventing activation of the receptor.

Probenecid also inhibits T2R1 by interacting with specific sulfonamide recognition sites on the receptor. This interaction hinders the binding of other bitter taste agents. Acesulfame potassium, a sweetener, can indirectly inhibit T2R1 by binding to sweet taste receptor sites, reducing the ability of T2R1 to detect and respond to bitter compounds. Capsazepine, on the other hand, can inhibit T2R1 by competing with molecules such as capsaicin for receptor binding sites, blocking the detection of some bitter substances. Finally, naringin and gymnemic acid bind to the bitter and sweet taste sites of T2R1, respectively. Naringin does so because of its intrinsic bitterness, while the occupancy of the sweet receptor site by gymnemic acid indirectly leads to a decrease in the interaction of T2R1 with bitter molecules.