Transient Receptor Potential

The largest group of receptors that function as noxious stimuli detectors in nociceptors is the transient receptor potential (TRP) channel family. TRPs have been subclassified into the C, V, M, A, P, and ML subfamilies. The members are principal transducers of thermal stimuli that depolarize nerve terminals to the action potential threshold. A role of TRP channels specifically in pain and thermosensation was first suggested by the finding that mammalian TRPV1 is activated by both noxious heat and capsaicin, the active ingredient of chilli peppers. Although there is little amino-acid conservation among distant TRP channels, they share a similar architecture of six-transmembrane domains with cytoplasmic amino and carboxy termini. TRP channels are thought to function as tetramers, mostly as homomers. Six of the 28 TRP channels from the three distinct TRP family subtypes are activated by temperature (TRPV1–4, TRPM8 and TRPA1). Three other TRP channels (TRPM2, TRPM4 and TRPM5) are strongly modulated by warm temperatures as well; however, the lack of expression in nociceptor neurons argues against a role in nociception[1].

[1] A. Patapoutian et al. Transient receptor potential channels: targeting pain at the source. Nat Rev Drug Discov. 2009 Jan;8(1):55-68.

17 Item(s)

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Axon ID Name Description From price
1816 A 784168 TRPV1 receptor antagonist €95.00
1504 ABT 102 TRPV1 antagonist €90.00
3026 AC1903 Selective TRPC5 inhibitor €95.00
3356 AMG 9810 Potent and selective vanilloid receptor-1 (TRPV1) antagonist €90.00
3036 BI 749327 Potent, selective and orally bioavailable TRPC6 inhibitor €160.00
2458 Clemizole Inhibitor of the transient receptor potential channel TRPC5 €75.00
2742 GSK 2193874 Orally active TRPV4 antagonist €120.00
3726 JT010 Potent and selective TRPA1 agonist €90.00
2423 M8-B hydrochloride Selective and potent antagonist of the TRPM8 channel €115.00
2980 ML2-SA1 Potent and selective activator of TRPML2 €105.00
3349 NMDAR-TRPM4 blocker C19 dihydrochloride NMDAR/TRPM4 interaction interface inhibitor €130.00
3348 NMDAR-TRPM4 blocker C8 dihydrochloride NMDAR/TRPM4 interaction interface inhibitor €120.00
3633 Ononetin Potent and selective TRPM3 antagonist €60.00
2374 Optovin Reversible photoactivated TRPA1 agonist €85.00
2483 PF 05105679 TRPM8 inhibitor with >100-fold selectivity and in vivo activity in humans €95.00
2498 RQ 00203078 Selective, potent, and orally active TRPM8 antagonist with in vivo activity €125.00
3287 SET2 Potent and selective TRPV2 inhibitor €100.00

17 Item(s)

per page
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