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. 2020 Aug 28;9(9):1983. doi: 10.3390/cells9091983

Table 2.

Small molecule modulators for TRPC channels (Agonists).

Agonists Chemical Structure TRPC Channel (EC50/IC50) Characteristics Reference
GSK1702934A graphic file with name cells-09-01983-i001.jpg TRPC3 (0.08 μm)
TRPC6 (0.44 μm)
No effect on TRPV4, TRPA1, TRPM1, TRPM4, CaV1.2, hERG, NaV1.5, or CXCR5 receptors at a concentration of 10 μmol/L [305]
Pyrazolo-pyrimidines graphic file with name cells-09-01983-i002.jpg TRPC6 (0.89–6.28 µm)
TRPC3 (0.02–0.45 μm)
Potency order: TRPC3 > TRPC7 > TRPC6 [306]
OptoDArG graphic file with name cells-09-01983-i003.jpg TRPC6
TRPC3
(30 μm was tested)
Photoswitchable DAG analogue containing two azobenzene photoswitchable moieties; active in cis-form at 365 nm and inactive at 430 nm [50]
OptoBI-1 graphic file with name cells-09-01983-i004.jpg TRPC6
TRPC3
TRPC7
(10 and 30 μm were tested)
Photoswitchable azobenzene analogue of GSK1702934 A; active in the cis-form [307]
PhoDAGs graphic file with name cells-09-01983-i005.jpg TRPC6
TRPC2
(5 and 50 μm were tested)
Photoswitchable DAG analogues; contain one photoswitchable moiety; active in cis-form at 370 nM and inactive at 460 nm [308]
Hyp9 graphic file with name cells-09-01983-i006.jpg TRPC6 (1.26 μm) A derivative of nonselective activator of TRPC3, TRPC6, and TRPC7 [305]
Artemisinin graphic file with name cells-09-01983-i007.jpg TRPC3 (33 µm) May inhibit TRPC6 [309]
(−)-Englerin A graphic file with name cells-09-01983-i008.jpg TRPC4 (11.2 nm) and TRPC5 (7.6 nm) Selective activator [296]