Table 4.
Vascular Transient Receptor Potential Channels and Their Pharmacology (259)
| Channel | Physiological activation | Selectivity [ratio] | Inhibitors/antagonists [IC50] | Activators/agonists [EC50] |
|---|---|---|---|---|
| TRPC1 | Gq signaling; SOCE with STIM1 (1078, 1238) | Ca2+:Na+ [~1:1] (1347) | La3+ [n.d.] (1347) | n.d. |
| Gd3+ [n.d.] (1655) | ||||
| TRPC3 | Diacylglycerols (612) | Ca2+:Na+ [1.6:1] (1654) | Gd3+ [0.1 µmol/L] (539) | OAG [n.d.] (612) |
| La3+ [4 µmol/L] (539) | ||||
| 2-APB [10 µmol/L] (874) | ||||
| BTP2 [0.3 µmol/L] (574) | ||||
| TRPC4 | Gi signaling; protons (693, 1279) | Ca2+:Na+ [1.1:1] (1258) | Niflumic acid [n.d.] (773) | (−)-englerin A [11.2 nmol/L] (25) |
| ML204 [3.2 µmol/L] (1002) | ||||
| TRPC5 | Gq/Gi/Go signaling; calpain cleavage (693, 721, 1258) | Ca2+:Na+ [1.8:1] (1258) | 2-APB [20 µmol/L] (1568) | rosiglitazone [32 µmol/L] (932) |
| KB-R7943 [1.3 µmol/L] (789) | Ca2+ [1 µmol/L] (507) | |||
| Mg2+ [500 µmol/L] (1101) | genistein [n.a.] (1543) | |||
| TRPC6 | Diacylglycerols; stretch (indirectly) (612, 1331) | Ca2+:Na+ [4.5:1] (647) | Gd3+ [1.9 µmol/L] (647) | OAG [n.d.] (612) |
| La3+ [3.9 µmol/L] (647) | SLG [n.d.] (612) | |||
| SKF96365 [3.9 µmol/L] (647) | SAG [n.d.] (612) | |||
| TRPV1 | Depolarization; heat; protons (206, 823) | Ca2+:Na+ [9.6:1] (206) | Capsazepine [40 nmol/L] (979) | capsaicin [30 nmol/L] (1481) |
| JNJ17203212 [16 nmol/L] (1365) | resiniferatoxin [4 nmol/L] (1310) | |||
| AMG517 [1 nmol/L] (143) | anandamide [1.3 µmol/L] (1309) | |||
| TRPV2 | Osmolarity/stretch; heat (rodent); IGF-1 (rodent) (205, 731, 1067) | Ca2+:Na+ [2.9:1] (205) | Tranilast [10 µmol/L] (1081) | probenecid [3.9 µmol/L] (83) |
| ruthenium red [0.6 µmol/L] (205) | Δ9-THC [16 µmol/L] (1181) | |||
| SKF96365 [n.d.] (720) | cannabidiol [79 µmol/L] (1181) | |||
| TRPV3 | Depolarization; heat (1566) | Ca2+:Na+ [12.1:1] (1566) | 17(R)-resolvin D1 [0.4 µmol/L] (84) | eugenol [2 mmol/L] (1562) |
| 2,2-di(phenyl)oxolane [8 µmol/L] (255) | carvacrol [4 µmol/L] (363) | |||
| 2-APB [25 µmol/L] (256) | ||||
| TRPV4 | Heat; mechanical stimuli; Gq signalling (994, 1345, 1501) | Ca2+:Na+ [6.9:1] (1482) | GSK2193874 [5 nmol/L] (1407) | 4α-PDD [0.2 µmol/L] (1499) |
| HC067047 [50 nmol/L] (392) | GSK1016790A [20 nmol/L] (1408) | |||
| RN1734 [2.5 µmol/L] (1480) | 5,6-EET [0.1 µmol/L] (1500) | |||
| TRPM4 | Intracellular Ca2+ (824) | Ca2+:Na+ [< 0.001:1] (1088) | 9-phenanthrol [20 µmol/L] (497) | BTP2 [8 nmol/L] (1378) |
| flufenamic acid [2.5 µmol/L] (1445) | decavanadate [2 µmol/L] (1089) | |||
| ATP [1 µmol/L] (1092) | PIP2 [5 µmol/L] (1085) | |||
| TRPM8 | Depolarization; cooling (1481) | Ca2+:Na+ [3.2:1] (980) | BCTC [0.8 µmol/L] (107) | Icilin [0.2 µmol/L] (48) |
| M8-B [0.8 µmol/L] (38) | menthol [16 µmol/L] (107) | |||
| PBMC [0.5 nmol/L] (767) | WS-12 [13 µmol/L] (1289) | |||
| TRPA1 | Chemosensation (129, 1490) | Ca2+:Na+ [0.84:1] (1046) | Resolvin D2 [2 nmol/L] (1137) | AITC [10 µmol/L] (714) |
| A967079 [63 nmol/L] (227) | acrolein [5 µmol/L] (97) | |||
| HC030031 [6.3 µmol/L] (983) | PF-4840154 [25 nmol/L] (1229) | |||
| TRPP1* | Cilial mechanosensation; Development (1278) | Ca2+:Na+ [6:1] (323) | SKF96365 [n.d.] (1148) | Calmidazolium [n.d.] (323) |
*
In this instance, “TRPP1” is used to describe the Pkd2 gene product. Prior to 2014, this same gene product is often referred to as “TRPP2” or “PKD2” in the literature. For further clarification, see the Section titled, “Polycystin (TRPP) Channels.”
n.d. = not determined.