TRPM8 agon 
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  • ||||||||||  isunakinra (EBI-005) / Sesen Bio, tivanisiran (SYL1001) / PharmaMar
    Review, Journal:  Experimental Pharmacotherapy for Dry Eye Disease: A Review. (Pubmed Central) -  Apr 2, 2021   
    Moreover, the most advanced experimental strategies in the pipeline for DED, tivanisiran, IL-1R antagonist EBI-005 and SkQ1, are being tested in Phase III clinical trials, still ongoing. Nevertheless, although promising results, further studies are still needed to confirm efficacy and safety of the new emerging therapies for DED.
  • ||||||||||  Tectin (tetrodotoxin) / WEX
    Journal:  TRPM8 Channel Activation Reduces the Spontaneous Contractions in Human Distal Colon. (Pubmed Central) -  Feb 20, 2021   
    Moreover, iberiotoxin, a blocker of the large-conductance Ca-dependent K-channels, but not apamin, a blocker of small-conductance Ca-dependent K channels, significantly reduced the inhibitory DIPA 1-8 actions. The results of the present study demonstrated that TRPM8 receptors are also expressed in human distal colon in healthy conditions and that ligand-dependent TRPM8 activation is able to reduce the colonic spontaneous motility, probably by the opening of the large-conductance Ca-dependent K-channels.
  • ||||||||||  Journal:  Agonists of Orally Expressed TRP Channels Stimulate Salivary Secretion and Modify the Salivary Proteome. (Pubmed Central) -  Jan 17, 2021   
    In the case of nonivamide, these changes were attributed to functional shifts in the WMS secreted, primarily the over representation of salivary and nonsalivary cystatins which was confirmed by immunoassay. This study provides new evidence of the impact of TRP channel agonists on the salivary proteome and the stimulation of salivary secretion by a TRPM8 channel agonist, which suggests that TRP channel agonists are potential candidates for developing treatments for sufferers of xerostomia.
  • ||||||||||  Clinical, Journal:  Topical TRPM8 Agonist for Relieving Neuropathic Ocular Pain in Patients with Dry Eye: A Pilot Study. (Pubmed Central) -  Jan 16, 2021   
    This study provides new evidence of the impact of TRP channel agonists on the salivary proteome and the stimulation of salivary secretion by a TRPM8 channel agonist, which suggests that TRP channel agonists are potential candidates for developing treatments for sufferers of xerostomia. TRPM8 agonist (C3) could be a novel agent for treating patients with DE-associated NOP who are unresponsive to conventional treatments.
  • ||||||||||  Tectin (tetrodotoxin) / WEX
    [VIRTUAL] IMPROVING THE EFFECT OF HYPERTONIC SALINE TREATMENT BY ACTIVATION OF SENSORY NEURONS IN SWINE AIRWAY () -  Oct 7, 2020 - Abstract #NACFC2020NACFC_445;    
    Our results show that inhibiting the nervous system with tetrodotoxin blocked HTS-triggered increase in MCC...Our findings suggest that concomitantly modulating the airway nervous system with TRPV1 and TRPM8 agonists could improve nebulized HTS treatment in CF patients, and may be a new target for the development of improved longer-lasting and more efficacious therapies for CF lung disease. Supported by Cystic Fibrosis Canada and Canadian Institutes of Health Research.
  • ||||||||||  Journal, PD(L)-1 Biomarker, IO Biomarker:  TRPM8 facilitates proliferation and immune evasion of esophageal cancer cells. (Pubmed Central) -  Sep 30, 2020   
    Finally, we explored the mechanism and found that calcineurin-NFATc3 pathway contributed to the expression of PD-L1 induced by TRPM8 overexpression and TRPM8 agonist, which might lead to immune evasion of esophageal cancer cells. These findings uncovered the crucial role of TRPM8 in the pathogenesis of esophageal cancer.
  • ||||||||||  Journal:  Evidence for the involvement of peripheral cold-sensitive TRPM8 channels in human cutaneous hygrosensation. (Pubmed Central) -  Jul 19, 2020   
    Our results indicated that: 1) independently of contact with moisture, a cold-dry stimulus in the TRPM8-range of activation induced wetness perceptions across 12 different body regions, and those wetness perceptions varied across the body following regional differences in cold sensitivity; 2) independently of skin cooling, menthol-induced stimulation of TRPM8 triggered wetness perceptions that were greater than those induced by physical dry cooling and by contact with an aqueous cream containing actual moisture. For the first time, we show that the cutaneous cold-sensing TRPM8 channel plays the dual role of cold and wetness sensor in human skin and that this ion channel is a peripheral mediator of human skin wetness perception.
  • ||||||||||  Journal:  Drug Discovery for Soft Drugs on TRPV1 and TRPM8 Channels Using the Passerini Reaction. (Pubmed Central) -  Jan 27, 2020   
    On the other hand, an overlooked possibility with the Passerini products is to exploit the presence of an ester group in the design and synthesis of soft drugs. We started to fill this gap, designing and synthesizing a series of TRPV1 and TRPM8 agonists able to act as soft drugs by using the Passerini reaction.
  • ||||||||||  Review, Journal:  Recent Progress in TRPM8 Modulation: An Update. (Pubmed Central) -  Nov 14, 2019   
    This short review will cover recent progress on the TRPM8 agonists and antagonists, describing newly reported chemotypes, and their application in the pharmacological characterization of TRPM8 in health and disease. The recently described structures of the TRPM8 channel alone or complexed with known agonists and PIP are also discussed.
  • ||||||||||  Journal:  TRPM8, ASIC1, and ASIC3 localization and expression in the human oropharynx. (Pubmed Central) -  Oct 25, 2019   
    TRPM8 and ASIC3 are found on submucosal sensory nerves in the human oropharynx. Our study lays the basis to use oropharyngeal TRPM8 and ASIC3 receptors as therapeutic targets to develop new active pharmacological treatments for OD patients.