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Table 1 Multimodal gating in mammalian somatosensory channels

From: Molecular and cellular limits to somatosensory specificity

Channel

Thermal

Mechanical

Chemical

Blockers

TRPV1

T>42°C

hyper-osmolarity (N-terminal variant), modulates mechanosensitivity

protons, capsaicin, resiniferatoxin, camphor, eugeneol, anandamide, lypooxygenases, 2-APB, clotrimazole, hydroxy-alpha-sanshool

Ruthenium Red (RR), capsazepine, BCTC, DD01050, iodo-resiniferatoxin, SB-452533, Cu:phenantroline

TRPV2

T>52°C

hypo-osmolarity

2-APB, Δ9-THC, probenecid

RR, SKF96365

TRPV3

T>30–39°C

 

camphor, 6-tert-butyl-m-cresol, carvacrol, eugenol, dihydrocarveol, thymol, carveol and (+)-borneol, 2-APB, arachidonic acid (AA); diphenylboronic anhydride

diphenyltetrahydrofuran, RR,

TRPV4

T>25–35°C

mechanical (sheer stress), hypo-osmolarity

4α-PDD, anandamide, epoxyeicosatrienoic acids, bisandrographolide A

RR

TRPM8

T<23–28°C

membrane tension

menthol, eucalyptol, icilin, WS23, LPC

BCTC, SKF96365, clotrimazole, Cu:phenantroline, intracellular acidification, 2-APB

TRPA1

T<18°C

mechanical

icilin, cinnamaldehyde, mustard oil, allicin, BCTC, 2-APB, 4-hydroxynonenal, hydroxy-alpha-sanshool, acetaldehyde, Δ9-THC, formaldehyde, trinitrophenol, GsMTx-4, methyl p-hydroxybenzoate, menthol, Ca2+

camphor, Gd3+, RR, gentamicin, amiloride, HC-030031, menthol, clorpromazine, AP18

TRPC1

 

mechanical

 

Gd3+, La3+, 2-APB

TRPC6

 

hypo-osmolarity

1-oleolyl-2-acetyl-sn-glycerol

2-APB

ASIC1

cold (positive modulator)

mechanical?

Protons

amiloride, aspirin, Psalmotoxin, A-317567

ASIC2

 

mechanical

Protons

amiloride, aspirin, A-317567

ASIC3

cold (positive modulator)

mechanical

protons, lactic acid

amiloride, aspirin, APETx2, A-317567

P2X2

 

mechanical (modulates ATP release)

ATP, UTP

suramin

P2X3

 

mechanical (modulates ATP release)

ATP, α,β-meATP

suramin, A-317491, TNP-ATP

TREK1

heat

mechanical

AA, LPC, protons, riluzole, inhalation anesthetics, flufenamic acid

clorpromazine, diltiazem, bupivacaine, fluoxetine, sipatrigine

TREK2

heat

mechanical

AA, LPC, protons, riluzole, inhalation anesthetics, Zn2+, flufenamic acid

Pb2+, diltiazem

TASK1

  

inhalation anesthetics

protons, Zn2+, hypoxia, anandamide, Gα q

TASK3

  

inhalation anesthetics

protons. Zn2+, Ba2+, RR, anandamide, Gα q

  1. The list of agonists and antagonists cited is extensive but not comprehensive, merely illustrating the degree of polymodality observed in different channels.
  2. Notes:
  3. Agonists for TRPV2 show marked species differences (Neeper et al., 2007).
  4. In the case of TREK and TASK channels, blockers produce an augmentation of excitability while activators reduce it.
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Molecular Pain

ISSN: 1744-8069

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