ICILIN

Description

Icilin (36945-98-9) is an activator of cold-sensitive TRP channels with 2.5-fold greater efficacy and 200-fold greater potency than menthol (EC50?= 0.36 μM for CRM1, rat orthologue of TRPM8).1 Activator at TRPM8 (EC50?= 0.2 μM)2?and ANKTM1(TRPA1)3. Activator effects require Ca2+?and are pH dependent.2,4?Icilin induced G1?arrest in PC-3 prostate cancer cells without cell death.5

The Uses of ICILIN

Icilin has been used as cooling agent in anterior ventromedial preoptic area (VMPO) neurons.

What are the applications of Application

Icilin is a potent agonist of the TRPM8 and ENaCδ ion channels

Definition

ChEBI: 3-(2-hydroxyphenyl)-6-(3-nitrophenyl)-1,4-dihydropyrimidin-2-one is a C-nitro compound.

General Description

Icilin is a synthetic cooling agent and modulates human transient receptor potential cation channel (TRPA1). Icilin inhibits transient receptor potential cation channel subfamily M member 8 (TRPM8) and modulates calcium release. Icilin also suppresses transient receptor potential vanilloid subtype 3 (TRPV3).

Biological Activity

Cooling agent that activates the novel cold receptors TRPM8 (CMR1) and TRPA1 (ANKTM1/TRPN1), members of the TRP ion channel family. Induces currents in CMR1-expressing HEK-293 cells (EC 50 = 0.36 μ M) more potently than menthol or low temperatures. Produces "wet shakes" in vivo .

Biochem/physiol Actions

Icilin is a potent agonist at the CMR1 cold- and menthol-sensitive receptor.

storage

Room temperature

References

1) McKemy?et al. (2002)?Identification of a cold receptor reveals a general role for TRP channels in thermosensation; Nature,?416?52 2) Andersson?et al. (2004)?TRPM8 activation by menthol, icilin and cold is differentially modulated by intracellular pH; J .Neurosci.,?24?5364 3) Story?et al. (2003)?ANKTM1, a TRP-like channel expressed in nociceptive neurons, is activated by cold temperatures; Cell,?112?819 4) Chuang?et al. (2004)?The super-cooling agent icilin reveals a mechanism of coincidence detection by a temperature-sensitive TRP channel; Neuron,?43?859 5) Kim?et al. (2011)?Icilin induces G1?arrest through activating JNK and p38 kinase in a TRPM8-independent manner; Biochem. Biophys. Res .Commun.,?406?30