taste receptor

Aspartame (SC-18862), an artificial, non-carbohydrate sweetener, is aspartyl-phenylalanine-1-methyl ester.

Lactisole (na-PMP) is an inhibitor of the glucose-sensing receptor

Denatonium benzoate (THS-839) , a quaternary ammonium cation, is a compound of a salt with an inert anion like saccharide or benzoate. Its structure is involved in the local anesthetic lidocaine which difference only is the addition of a benzyl group to the amino nitrogen.

Neotame (HSDB 7965) is a white-colored, dipeptide methyl ester, which is found to be a highly potent and non-nutritive sweetener or flavour enhancer and hence finds applications in a variety of foods.

6-Methoxyflavanone (6-MeOF) is a positive allosteric modulator of the GABA response in human recombinant GABA A receptors, exhibiting antianxiety and anti-inflammatory properties, and is used to alleviate cisplatin-induced neuropathic pain.

Adenosine 5'-succinate is a compound closely related to adenosine monophosphate (AMP) that demonstrates strong inhibitory properties against taste receptor activation of transducin caused by Denatonium benzoate.

GIV3727, a bitter taste receptor hTAS2R antagonist, inhibits the activation of hTAS2R31 by saccharin and acesulfame potassium, effectively diminishing the bitter taste in foods, beverages, and pharmaceuticals [1].

Alitame hydrate is a non-nutritive sweetener that is 2000 times sweeter than sucrose. It is formed from aspartic acid, alanine & an amide.

Epiquinidine, an analogue of quinine, serves as an agonist for ggTas2r1, exhibiting activation at concentrations of 10 μM or higher.

S6821 is a TAS2R8 antagonist. S6821 was not found to be mutagenic or clastogenic in vitro, and did not induce micronuclei in bone marrow polychromatic erythrocytes in vivo.

Lysine-N,N-diacetic acid (BCML) is a highly efficient TAS2R4 inhibitor, blocking the human TAS2R4-mediated response to quinine.

Compound 28.1, also known as TAS2R14 agonist-2, is a potent and selective inhibitor of TAS2R14, exhibiting an EC50 of 72 nM [1].

TAS2R14 agonist is a potent partial agonist of TAS2R14, displaying an EC50 value of 116.6 ± 23.6 nM [1].

FEMA 4774 (S9632) is a positive allosteric modulator of T1R2/T1R3. FEMA4774 shows obvious enhancement of the sweetness of sucrose in sensory evaluation tests

Dulcoside A, isolated from Stevia rebaudiana, is a sweetener with antioxidant activity.

Perillartine (DL-Perillartine) is a sweetener. Perillartine activates the taste receptor type 1 member 2 (Tas1r2) subunit in a species-dependent manner.

P2X3 antagonist 34, a potent, selective, and orally active antagonist, targets the P2X3 homotrimeric receptor, exhibiting IC50s of 25 nM, 92 nM, and 126 nM for human, rat, and guinea pig P2X3 receptors respectively. It shows reduced activity against P2X2/3 heterotrimeric receptors across human, rat, and guinea pig models. Notably, this compound demonstrates a significant anti-tussive effect without altering taste[1].

RO5166017 is an orally active, potent and selective trace amine-associated receptor 1 (TAAR1) agonist for the study of conditioned taste aversion frontal nerve disorders.

Lactisole free acid acts as a typical antagonist of sweet taste receptors, selectively targeting the T1R3 subunit. T1R3 functions as a glucose-sensing receptor. Additionally, Lactisole free acid inhibits insulin secretion induced by glucose in mouse islets.

Cyclo(L-Leu-L-Trp) is a diketopiperazine metabolite initially derived from Penicillium, exhibiting antibacterial (MICs = 125-1000 µg/ml) and antifungal activities (MICs = 8-64 µg/ml). It also demonstrates antioxidant properties by reducing the production of hydroxy radicals, as evidenced in an electron spin resonance (ESR) spectroscopy assay (IC50 = 1.8 µM). Additionally, Cyclo(L-Leu-L-Trp) has been identified as a bitter compound capable of quickly crossing rat taste cell membranes ex vivo at a 1 mM concentration. Furthermore, it acts as a melatonin receptor agonist in X. laevis melanophores, suppressing cAMP accumulation at a 20 µM concentration, with this effect being negated by the melatonin receptor antagonist luzindole.