Drug intelligence / Profile preview

icilin

Development stage
Preclinical
Modality
Small Molecules
Administration
Intraperitoneal, Intrathecal, Intra-cisterna Magna, Subcutaneous, Intramuscular, Topical, Oral
01

Overview

Icilin is a synthetic small molecule that functions as a super-agonist of the transient receptor potential M8 (TRPM8) ion channel. It is known for producing an intense sensation of cold, being significantly more potent and efficacious than menthol. Beyond its primary action on TRPM8, icilin also acts as an inhibitor of the transient receptor potential V3 (TRPV3) channel and an agonist of the human epithelial Na+ channel (hENaC). Research indicates its potential involvement in various physiological processes and conditions, including migraine pathophysiology, autoimmune neuroinflammation, pruritus, colitis, and certain types of cancer, where it has shown effects such as attenuating inflammatory responses and inhibiting cancer cell motility.

Other names
AG 3-5AG3-5AG-3-5
02

Targets

ENaCTRPV3 (Transient receptor potential vanilloid subtype 3)TRPM4 (Calcium-activated non-selective cation channel TRPM4)

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