Table 2.
Overview of the Biophysical and Pharmacological Properties of Endothelial TRP Channels
| TRP | Unitary conductance | PCa:PNa | Physiological activators | Pharmacological agonists (EC50) | Pharmacological antagonists (IC50) |
|---|---|---|---|---|---|
| TRPA1 | ~98ps(192) | 7.9(135) | H2O2, 4-HNE, 4-ONE (10, 286), noxious cold <17°C (257)) | Allyl isothiocyanate (rat 11 μmol/L, mouse 22 μmol/L) (19, 131), cinnamaldehyde (mouse 61 μmol/L) (19) | HC-030031 (human 0.7 μmol/L) (180) |
| TRPV1 | 35 pS at −60mV and 77 pS at +60mV (42) | 9.6 (42) | Noxious heat >43°C (42), protons (12) | Capsaicin (mouse 9.1 nmol/L) (56) | Capsazepine (human 39 nmol/L, rat 0.22 μmol/L, mouse 1.4 μmol/L) (56, 179) |
| TRPV3 | ~150–200 pS (51) | ~12 (320) | Heat 23–39°C (320), depolarization (67) | Carvacrol, eugenol, thymol (319) | Ruthenium red (211), isopentenyl pyrophosphate (239 nmol/L) (20) |
| TRPV4 | ~30–60 pS at −60mV and ~88–100 pS at +60mV (258,301,303) | ~6 (258) | Heat 25–43°C (303), mechanical stimuli (164), EETs(302) | 4α-PDD (11.7nM) (318), GSK1016790A (mouse 18 nmol/L, human 2.1 nmol/L) (279) | HC-067047 (human 48 nmol/L, rat 133nmol, mouse 17 nmol/L) (84), RN-1734 (human 2.3 μmol/L, rat 3.2 μmol/L, mouse 4 μmol/L) (293), GSK2193874 (278) |
| TRPC1 | ~5 pS (in combination with TRPC5) (260) | 0.95 (in combination with TRPC5) (260) | Nitric oxide (330), stretch (176) | Gd3+ (340), La3+ (260), Pico 145 (human 200pmol/L, and in combination with TRPC5) (225) | |
| TRPC3 | ~60 pS (134) | 1.6(134) | Diacylglycerol (119) | OAG (119) | Pyr3 (mouse 0.7 μmol/L) (139), Gd3+ (human 20 nmol/L), La3+ (human 20 nmol/L) (105) |
| TRPC4 | 42 pS (232) | 1.1–7.7 (25,232) | Nitric oxide (330) | (−)-Englerin A (human 11.2 nmol/L) (7), La3+ (μmol/L range) (132,232) | ML204 (mouse 0.96 μmol/L) (185), Picol45 (human 0.35 nmol/L) (225), La3+ (mmol/L range) (132,232) |
| TRPC5 | 40–66 pS (133,232) | 1.8–9.5 (132,202, 232) | Nitric oxide, H2O2 (330), protons (238), stretch (99) | (−)-Englerin A (human 7.6 nmol/L) (7), La3+ (μmol/L range) (132,232) | ML204 (mouse <10 μmol/L) (185), Picol 45 (human 1.3 nmol/L) (225), La3+ (mmol/L range) (132) |
| TRPC6 | ~30 pS (119,126,154) | ~5 (119, 126,154) | Diacylglycerol (119), stretch (255) | OAG (119), hyperforin(155) | Gd3+(mouse 1.9 μmol/L), La3+ (mouse 4 μmol/L) (126), SH045 (104) |
| TRPM2 | 58 pS at negative membrane potentials and 76 pS at positive potentials (230) | ~0.7–0.9 (230,317) | Heat 35°C (252), adenosine diphosphate ribose (213,230), arachidonic acid (107), H2O2 (145), nicotinic acid adenine dinucleotide phosphate (24) | Clotrimazole, econazole (115) | |
| TRPP1 | 97 pS (140) | 3.92 (140) | Intracellular Ca2+ (146), stretch (241) | Gd3+, La3+, Cd2+, Ni2+ (212) |
Note. Further details can be found at the International Union of Basic and Clinical Pharmacology (IUPHAR) database (http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=78).