Tabel 1:
Summary of expression, function, related diseases and ligands of TRPM channels.
Name | Expression | Functions | Diseases | Ligands |
---|---|---|---|---|
TRPM1 | Retina ON bipolar cells; Skin melanocytes. | Depolarization of the bipolar cell; suppress melanoma metastasis. | Congenital stationary night blindness. |
Activation: pregnenolone sulphate Inhibition: Zn2+ |
TRPM2 | Central nervous system; Immune cells; Pancreatic β cells | Core body temperature sensation; Oxidative sensation; Insulin secretion; Immune response. | Bipolar disorder; Ischaemia-reperfusion injury; Alzheimer’s disease. |
Activation: ADPR, cADPR, 2′-deoxy-ADPR, 2′-P-ADPR, 3′-P-ADPR, 2-F-ADPR, AMPCPR, Ca2+ Inhibition: econazole, clotrimazole, flufenamic acid, N-(p-amylcinnamoyl)anthranilic acid, 2-APB, Scalardial, 3-MFA, 8-Br-cADPR, 8-Br-ADPR, 8-Ph-ADPR, 8-Ph-2′-deoxy-ADPR, 8-(3-acetylphenyl)-ADPR, 8-thiophenyl-ADPR, and more Other: PIP2 |
TRPM3 | Primary nociceptive neurons; Pancreatic beta-cell. Kidney | Glucose homeostasis; Heat sensation and inflammatory pain. | Visual epilepsy, retinal dystrophy. |
Activation: pregnenolone sulphate, CIM0216. Inhibition: primidone |
TRPM4 | Heart, liver | Regulation of calcium oscillations after T cell activation, prevention of cardiac conduction disorders, Regulating smooth muscle contraction. | Brugada syndrome, Cardiac conduction defect. |
Activation: Ca2+ Inhibition: ATP, ADP, AMP, DVT, 9-Phenanthrol. |
TRPM5 | Pancreatic beta-cells; tuft cells; solitary chemosensory cells. | Modulation of insulin secretion and sensory transduction in taste cells. | Beckwith-Wiedemann syndrome. |
Activation: Ca2+, PIP2, Steviol glycosides, Rutamarin. Inhibition: TPPO |
TRPM6 | Kidney, intestine | Magnesium uptake and homeostasis in kidney and intestine. | Hypomagnesemia. |
Activation: Mg2+ Inhibition: Ruthenium red |
TRPM7 | Ubiquitous. | Magnesium and Calcium homeostasis, cell viability. | Neuronal degenerative diseases. |
Activation: Mg2+-ATP, breakdown of PIP2, increase in cAMP concentrations Inhibition: Mg2+, spermine, 2-APB, MnTBAP |
TRPM8 | Sensory neurons, prostate. | Cold sensation. | Inflammatory/neuropathic pain; prostate cancer. |
Activation: menthol, icilin. Inhibition: WS-12, CPS-369. |