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. 2019 Oct 2;10:1267. doi: 10.3389/fphys.2019.01267

TABLE 1.

Compounds selected for functional studies with regard to their ability to act as agonists (or not) of the 25 TAS2R receptors identified in humans to date.

hTAS2R 1 3 4 5 7 8 9 10 13 14 16 19 20 30 31 38 39 40 41 42 43 45 46 50 60
Promiscuous agonists:
Diphenidol 100 100 10 and 675 ± 186 30 30 10 100 100 100 3 100 100 30 30 30
Quinine 10 and 838 ± 24∗∗ 10 and 983 ± 257 10 10 10 10 10 10 10
Denatonium 300 1000 3 and 120 ± 56 30 0.03 and 0.27 ± 0.06 100 300 30 and 240 ± 192
Partly selective agonists:
Colchicine 100 and 1025 ± 1219 3000 300 and 1580 ± 170
Chloroquine 10 and 172 ± 29 +/0 10000 100
Dapsone 100 100 30
Strychnine +/1000 3 and 21.8 ± 7.5 0.1 and 0.43 ± 0.02
Saccharin + 170 ± 10 and 1700 ± 20 80 ± 60 and 1100 ± 10
Sodium cromoglycate 3000 and 4500 ± 1600 10 and 45 ± 25 3000
Selective agonists:
Ofloxacin EC50 ≈ 200
Phenanthroline 100
Erythromycin 300
Carisoprodol 100

The most recent nomenclature was adopted (Andres-Barquin and Conte, 2004; Sainz et al., 2007; Dotson et al., 2008; Meyerhof et al., 2010; Alexander et al., 2011; Soares et al., 2013). Unless otherwise stated, single values (i.e., lacking ± SEM) represent the threshold concentration (i.e., the lowest concentration (μM) to have elicited a calcium response in transfected HEK-293T cells), whereas values presented as the mean ± SEM represent the EC50 (μM) (Meyerhof et al., 2010). When both a threshold concentration and the EC50 were available, both values were reported (in that order). When no quantitative indicators were available, the symbol “+” indicates agonism. The TAS2R numbers in bold type and those underlined correspond to the TAS2Rs found to be expressed in human LMs. The TAS2R numbers in italics correspond those not expressed in human LMs. The TAS2R numbers in standard type correspond to the receptors not assessed in RT-qPCR assays. values from Liu et al. (2018) and ∗∗ values from Jaggupilli et al. (2019).