T1R3 Inhibitors
T1R3 inhibitors encompass a diverse group of chemicals that attenuate the signaling or function of the T1R3 receptor, a G-protein-coupled receptor (GPCR) implicated in sweet and umami taste perceptions. These inhibitors operate through a variety of mechanisms, some directly targeting the T1R3 receptor and its associated signaling pathways, while others exert their effects indirectly by influencing related cellular processes. Direct inhibitors like gymnemic acid and lactisole exhibit their inhibitory action by binding to the T1R3 receptor, impeding its ability to recognize sweet molecules, which can disrupt the typical conformational changes required for signal transduction. Gymnemic acid achieves this by attaching to the sugar-binding sites on the sweet taste receptors, nullifying the activation signal typically transmitted by sweet substances. Lactisole similarly inhibits the T1R3 receptor function by directly interacting with the receptor complex, blocking the activation cascade that normally results in the perception of sweetness.
On the other hand, several indirect inhibitors modulate the T1R3 receptor activity without directly binding to the receptor. Compounds such as amiloride, known for its primary action on sodium channels, can modify the ionic environment pivotal for receptor activation and thereby indirectly influence T1R3 activity. Amiloride's effect on T1R3 highlights the complexity of taste receptor modulation, as changes in ion channel activity can lead to significant alterations in taste perception. Other agents, such as alloxan and probenecid, may exert their inhibitory influence on T1R3 through changes in cellular metabolism or ion transport, respectively. Alloxan can indirectly inhibit T1R3 by altering cellular redox states, modifying GPCR function, while probenecid's inhibition of anion transporters and channels can lead to a reduced T1R3 receptor activity. Methyl-β-cyclodextrin demonstrates its effect by extracting cholesterol from cell membranes, disrupting lipid rafts that are essential for the structural and functional integrity of GPCRs, including T1R3. The interference with lipid rafts can lead to diminished T1R3 activity and, consequently, impaired taste perception.
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Amiloride | 2609-46-3 | sc-337527 | 1 g | $290.00 | 7 | |
Amiloride is a known inhibitor of epithelial sodium channels but has also been reported to modulate taste receptor function. It can alter T1R3-related signaling by modifying the ionic environment necessary for receptor activation, particularly in response to sweet and umami tastes. | ||||||
Alloxan monohydrate | 2244-11-3 | sc-254940 | 10 g | $53.00 | ||
Alloxan targets beta cells in the pancreas but may also interact with GPCRs, potentially leading to an indirect inhibition of the T1R3 receptor by altering the cellular redox state, which is known to affect GPCR function. | ||||||
Probenecid | 57-66-9 | sc-202773 sc-202773A sc-202773B sc-202773C | 1 g 5 g 25 g 100 g | $27.00 $38.00 $98.00 $272.00 | 28 | |
Probenecid is known to inhibit a variety of anion transporters and channels, and through these effects, it could indirectly affect the signaling pathways associated with T1R3, leading to a reduced taste receptor activity, particularly in the perception of umami taste. | ||||||
Denatonium benzoate | 3734-33-6 | sc-234525 sc-234525A sc-234525B sc-234525C sc-234525D | 1 g 5 g 25 g 100 g 250 g | $31.00 $46.00 $138.00 $464.00 $903.00 | ||
Denatonium benzoate is considered the most bitter-tasting compound and is known to affect taste receptor function. While its primary action is on bitter taste receptors, it can indirectly influence T1R3 activity by altering taste receptor function and signaling pathways. | ||||||
Phloretin | 60-82-2 | sc-3548 sc-3548A | 200 mg 1 g | $63.00 $250.00 | 13 | |
Phloretin is a dihydrochalcone found in apple tree leaves, which inhibits various glucose transporters. Its action on glucose transport can indirectly affect glucose availability and, subsequently, glucose-induced T1R3 + TAS1R2 receptor activation for sweet taste perception. | ||||||
Adenosine phosphate(Vitamin B8) | 61-19-8 | sc-278678 sc-278678A | 50 g 100 g | $160.00 $240.00 | ||
AMP is known to competitively inhibit cyclic AMP (cAMP) signaling. Since cAMP is a secondary messenger in taste receptor signaling, AMP can indirectly decrease T1R3-mediated sweet taste signaling by attenuating the cAMP-dependent pathway. | ||||||
Quinine hydrochloride dihydrate | 6119-47-7 | sc-212619 sc-212619A | 5 g 25 g | $63.00 $210.00 | ||
Quinine hydrochloride, while primarily known as a bitter compound, can affect other taste receptors including T1R3. It can indirectly inhibit T1R3 by interfering with GPCR signaling pathways and by altering the taste receptor cells' signal processing. | ||||||
Methyl-β-cyclodextrin | 128446-36-6 | sc-215379A sc-215379 sc-215379C sc-215379B | 100 mg 1 g 10 g 5 g | $25.00 $65.00 $170.00 $110.00 | 19 | |
Methyl-β-cyclodextrin extracts cholesterol from cell membranes, which can disrupt lipid rafts. These rafts are important for the proper functioning of GPCRs, including T1R3, and their disruption can lead to reduced receptor activity and impaired taste perception. | ||||||