Results 131 to 140 of about 6,833 (180)

TRPM8 Channels and Dry Eye [PDF]

open access: yesPharmaceuticals, 2018
Transient receptor potential (TRP) channels transduce signals of chemical irritation and temperature change from the ocular surface to the brain. Dry eye disease (DED) is a multifactorial disorder wherein the eyes react to trivial stimuli with abnormal sensations, such as dryness, blurring, presence of foreign body, discomfort, irritation, and pain ...
Jee Myung Yang   +2 more
exaly   +6 more sources

Recent Progress in TRPM8 Modulation: An Update [PDF]

open access: yesInternational Journal of Molecular Sciences, 2019
The transient receptor potential melastatin subtype 8 (TRPM8) is a nonselective, multimodal ion channel, activated by low temperatures (<28 °C), pressure, and cooling compounds (menthol, icilin). Experimental evidences indicated a role of TRPM8 in cold thermal transduction, different life-threatening tumors, and other pathologies, including migraine,
Isabel Gomez-Monterrey   +2 more
exaly   +5 more sources
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5-Benzyloxytryptamine as an antagonist of TRPM8

Bioorganic and Medicinal Chemistry Letters, 2010
5-Benzyloxytryptamine 19 was found to act as an antagonist of the TRPM8 ion-channel. For example, 19 had an IC(50) of 0.34 μM when menthol was used as the stimulating agonist. Related commercially-available tryptamine derivatives showed diminished, or no antagonist activity at TRPM8.
Matthew A J Duncton
exaly   +3 more sources

TRPM8

2014
Transient receptor potential melastatin 8 (TRPM8) was originally cloned from prostate tissue. Shortly thereafter, the protein was identified as a cold- and menthol-activated ion channel in peripheral sensory neurons, where it plays a critical role in cold temperature detection.
Laura, Almaraz   +3 more
openaire   +2 more sources

Regulation of TRPM8 channel activity [PDF]

open access: yesMolecular and Cellular Endocrinology, 2012
Transient Receptor Potential Melastatin 8 (TRPM8) is a Ca(2+) permeable non-selective cation channel directly activated by cold temperatures and chemical agonists such as menthol. It is a well established sensor of environmental cold temperatures, found in peripheral sensory neurons, where its activation evokes depolarization and action potentials. The
Yevgen Yudin, Tibor Rohacs
exaly   +3 more sources

TRPM8

2007
Originally cloned as a prostate-specific protein, TRPM8 is now best known as a cold- and menthol-activated channel implicated in thermosensation. In this chapter we provide a brief review of current knowledge concerning the biophysical properties, gating mechanisms, pharmacology and (patho)physiology of this TRP channel.
T, Voets, G, Owsianik, B, Nilius
openaire   +2 more sources

TRPM8 ligand modification

Bulletin Physiology and Pathology of Respiration, 2022
Introduction.In silico methods make it possible to detect low molecular weight ligands with a high affinity for a protein, but cannot answer the question of whether the ligand is its agonist or antagonist.Aim.Use of a virtual modification of the TRPM8 agonist menthol to solve this problem.Materials and methods.The structure of menthol was modified ...
P. D. Timkin   +2 more
openaire   +1 more source

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