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Novel agonists for cold receptors on sensory neurons
Author(s) -
Wei E. T.
Publication year - 2004
Publication title -
experimental dermatology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.108
H-Index - 96
eISSN - 1600-0625
pISSN - 0906-6705
DOI - 10.1111/j.0906-6705.2004.0212am.x
Subject(s) - transient receptor potential channel , menthol , trpm8 , chemistry , receptor , pharmacology , capsaicin , odor , trpv1 , taste , calcium , extracellular , medicine , biochemistry , organic chemistry
An exciting research topic these past 2 years has been the identification of transient receptor potential (TRP) channel protein receptors on sensory neurons that are linked to thermosensation. Two compounds, menthol and icilin, were shown to activate the putative cold receptor, TRP‐M8 (CMR1, trp‐p8), in vitro . Here, some of the pharmacological properties of icilin are described and compared to menthol, summarized in the table below.Menthol Stimulates TRP‐M8 receptor, does not require extracellular calcium for activity, and does not stimulate the ANKTM1 receptor. Mint odor Irritant and harsh taste at high concentrations Duration of action less than15 min after topical application After systemic administration, lethal at high concentrations due to anesthetic activity Icilin Stimulates TRP‐M8 and ANKTM1 receptor and requires extracellular calcium for activity No odor No irritant activity on skin or mucous membranes Action on inflamed skin and mucous membranes (e.g. eyelids, lips, nasal, and anorectal) can last 4–8 h No anesthetic activity, and no lethality at doses of up to 1.5 g/kg intraperitoneally, but after systemic administration produces ‘wet dog shakes’ which are rapid, alternating contractions, and relaxations of the supination and pronation muscles about the spinal axis