Transient receptor potential vanilloid 4 (TRPV4) channel as a target of crotamiton and its bimodal effects

@article{Kittaka2017TransientRP,
  title={Transient receptor potential vanilloid 4 (TRPV4) channel as a target of crotamiton and its bimodal effects},
  author={Hiroki Kittaka and Y. Yamanoi and Makoto Tominaga},
  journal={Pfl{\"u}gers Archiv - European Journal of Physiology},
  year={2017},
  volume={469},
  pages={1313-1323}
}
The sensation of itching can be defined as “an unpleasant cutaneous sensation that provokes a desire to scratch.” The perception of itching is not critical for the maintenance of life, but persistent itching can be extremely irritating and decreases the quality of life. Crotamiton (N-ethyl-o-crotonotoluidide) has been used as an anti-itch agent for humans for around 70 years. In spite of the long use of crotamiton, its mechanism of action remains unknown. We hypothesized that crotamiton might… 
Identification of the molecular target of crotamiton, an anti–itch agent
TLDR
It is found that crotamiton strongly inhibits TRPV (vanilloid) 4 channel activity and inhibited itch–related behaviors induced by the TRpV4–selective agonist GSK1016790A.
Role of Transient Receptor Potential Vanilloid 4 Channel in Skin Physiology and Pathology
TLDR
There is substantial evidence implicating dysfunctional TRPV4 channel—in the form of either deficient or excessive channel activity—in pathological cutaneous conditions such as skin barrier compromise, pruritus, pain, skin inflammation and carcinogenesis.
Crotamiton, an Anti-Scabies Agent, Suppresses Histamine- and Chloroquine-Induced Itch Pathways in Sensory Neurons and Alleviates Scratching in Mice
TLDR
Overall, it was found that crotamiton has an anti-pruritic effect against non-scabietic itching by histamine and chloroquine, and may be used as a general anti- Pruritic agent, irrespective of the presence of scabies.
Physiological and Pathological Significance of Esophageal TRP Channels: Special Focus on TRPV4 in Esophageal Epithelial Cells
TLDR
This review focuses on the functional expression of TRPV4 in esophageal epithelium and its possible role in different esophagal diseases that would support TRpV4 as a candidate target for future therapeutic approaches to treat patients with these conditions.
TRPV4: A Physio and Pathophysiologically Significant Ion Channel
TLDR
Several lines of evidence derived from animal models and even clinical trials in humans highlight TRPV4 as a therapeutic target and as a protein that will receive even more attention in the near future, as will be reviewed here.
TRPing to the Point of Clarity: Understanding the Function of the Complex TRPV4 Ion Channel
TLDR
This review will highlight structural features of TRPV4, endogenous and exogenous activators of the channel, and discuss the reported roles of TRpV4 in health and disease.
Ca2+ Signaling by TRPV4 Channels in Respiratory Function and Disease
TLDR
The role of TRPV4 channels in lung fibroblasts, the lung endothelium, as well as the alveolar and bronchial epithelium is highlighted, during physiological and pathophysiological mechanisms.
Involvement of Neural Transient Receptor Potential Channels in Peripheral Inflammation
TLDR
The functional contribution of a subset of TRP channels (TRPV1, TRPV4, TRPM3, TRPA8, and TRPA1) that are involved in the body’s immune responses, particularly in relation to inflammation are discussed.
Potential therapeutic value of transient receptor potential channels in male urogenital system
TLDR
Developing safe and efficacious TRP channel modulators is warranted for male urogenital disorders in a clinical setting.
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TLDR
TRPV4 functions as a pruriceptor-TRP in skin keratinocytes in histaminergic itch, a novel basic concept with translational-medical relevance and is supported based on attenuated scratching behavior in response tohistaminergic pruritogens.
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TLDR
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