Nomenclature |
http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=499
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http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=500
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HGNC, UniProt |
https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:17994, http://www.uniprot.org/uniprot/Q96QT4
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https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:17961, http://www.uniprot.org/uniprot/Q7Z2W7
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EC number |
http://www.genome.jp/dbget‐bin/www_bget?ec:2.7.11.1
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Chemical activators |
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agonist activities are temperature dependent and potentiated by cooling |
Physical activators |
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depolarization (V½ +50 mV at 15°C), cooling (< 22‐26°C) |
Endogenous activators |
Extracellular http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2346 (Potentiation) |
– |
Activators |
http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2433 Concentration range: >1×10−3M [http://www.ncbi.nlm.nih.gov/pubmed/11385574?dopt=AbstractPlus] – Mouse, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=1640 [http://www.ncbi.nlm.nih.gov/pubmed/24633576?dopt=AbstractPlus] |
http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2429 (Agonist) (pEC50 6.7–6.9) [physiological voltage] [http://www.ncbi.nlm.nih.gov/pubmed/15190109?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/14757700?dopt=AbstractPlus] – Mouse, (‐)http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2430 (inhibited by intracellular Ca2+) (pEC50 4.6) [‐120mV – 160mV] [http://www.ncbi.nlm.nih.gov/pubmed/15306801?dopt=AbstractPlus] |
Selective activators |
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http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4343 (Full agonist) (pEC50 4.9) [physiological voltage] [http://www.ncbi.nlm.nih.gov/pubmed/18930858?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/20816009?dopt=AbstractPlus] – Rat |
Channel blockers |
http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=710 (Inhibition) (pK
i 5.6) [‐110mV – 80mV] [http://www.ncbi.nlm.nih.gov/pubmed/12149283?dopt=AbstractPlus] – Rat, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2433 (Inhibition) (pIC50 3.8) [‐100mV – 100mV] [http://www.ncbi.nlm.nih.gov/pubmed/16636202?dopt=AbstractPlus] – Mouse, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2497 (Inhibition) (pIC50 3.5) [‐100mV – 100mV] [http://www.ncbi.nlm.nih.gov/pubmed/19135721?dopt=AbstractPlus] – Mouse, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=708 (Antagonist) (pIC50 2.5) [80mV] [http://www.ncbi.nlm.nih.gov/pubmed/11385574?dopt=AbstractPlus] – Mouse, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2434 (Antagonist) Concentration range: 2×10−3M [‐100mV – 100mV] [http://www.ncbi.nlm.nih.gov/pubmed/11161216?dopt=AbstractPlus] – Mouse |
http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2460 (Antagonist) (pIC50 6.1) [physiological voltage] [http://www.ncbi.nlm.nih.gov/pubmed/14757700?dopt=AbstractPlus] – Mouse, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2433 (Antagonist) (pIC50 4.9–5.1) [100mV – ‐100mV] [http://www.ncbi.nlm.nih.gov/pubmed/15194687?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/21964764?dopt=AbstractPlus] – Mouse, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2461 (Antagonist) (pIC50 4.7) [physiological voltage] [http://www.ncbi.nlm.nih.gov/pubmed/14757700?dopt=AbstractPlus] – Mouse |
Selective channel blockers |
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http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=10300 (Antagonist) (pIC50 7) [voltage dependent] [http://www.ncbi.nlm.nih.gov/pubmed/25893043?dopt=AbstractPlus] |
Functional Characteristics |
γ = 40‐105 pS at negative and positive potentials respectively; conducts mono‐and di‐valent cations with a preference for monovalents (PCa/PNa = 0.34); conductance sequence Ni2+ > Zn2+ > Ba2+ = Mg2+ > Ca2+ = Mn2+ > Sr2+ > Cd2+; outward rectification, decreased by removal of extracellular divalent cations; inhibited by intracellular Mg2+, Ba2+, Sr2+, Zn2+, Mn2+ and Mg.ATP (disputed); activated by and intracellular alkalinization; sensitive to osmotic gradients |
γ = 40‐83 pS at positive potentials; conducts mono‐ and di‐valent cations non‐selectively (PCa/PNa = 1.0–3.3); pronounced outward rectification; demonstrates densensitization to chemical agonists and adaptation to a cold stimulus in the presence of Ca2+; modulated by lysophospholipids and PUFAs |
Comments |
http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2433 acts as a channel blocker in the μM range. Recent study shows cAMP inhibits TRPM7‐mediated Ca2+ influx [http://www.ncbi.nlm.nih.gov/pubmed/30615643?dopt=AbstractPlus]. Waixenicin‐A specifically inhibits TRPM7 [http://www.ncbi.nlm.nih.gov/pubmed/21926172?dopt=AbstractPlus]. |
http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4150 and http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2424 are examples of cannabinoid activators. TRPM8 is insensitive to http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2432. http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2429 requires intracellular Ca2+ for full agonist activity. |