Table 2.
Small molecule modulators for TRPC channels (Agonists).
Agonists | Chemical Structure | TRPC Channel (EC50/IC50) | Characteristics | Reference |
---|---|---|---|---|
GSK1702934A |
![]() |
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 |
![]() |
TRPC6 (0.89–6.28 µm) TRPC3 (0.02–0.45 μm) |
Potency order: TRPC3 > TRPC7 > TRPC6 | [306] |
OptoDArG |
![]() |
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 |
![]() |
TRPC6 TRPC3 TRPC7 (10 and 30 μm were tested) |
Photoswitchable azobenzene analogue of GSK1702934 A; active in the cis-form | [307] |
PhoDAGs |
![]() |
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 |
![]() |
TRPC6 (1.26 μm) | A derivative of nonselective activator of TRPC3, TRPC6, and TRPC7 | [305] |
Artemisinin |
![]() |
TRPC3 (33 µm) | May inhibit TRPC6 | [309] |
(−)-Englerin A |
![]() |
TRPC4 (11.2 nm) and TRPC5 (7.6 nm) | Selective activator | [296] |