Discovery of a Potent (4R,5S)-4-Fluoro-5-methylproline Sulfonamide Transient Receptor Potential Ankyrin 1 Antagonist and Its Methylene Phosphate Prodrug …

H Chen, M Volgraf, S Do, A Kolesnikov… - Journal of Medicinal …, 2018 - ACS Publications
Transient receptor potential ankyrin 1 (TRPA1) is a non-selective cation channel expressed
in sensory neurons where it functions as an irritant sensor for a plethora of electrophilic …

Tetrahydrofuran-based transient receptor potential ankyrin 1 (TRPA1) antagonists: ligand-based discovery, activity in a rodent asthma model, and mechanism-of …

JA Terrett, H Chen, DG Shore, E Villemure… - Journal of Medicinal …, 2021 - ACS Publications
Transient receptor potential ankyrin 1 (TRPA1) is a nonselective calcium-permeable ion
channel highly expressed in the primary sensory neurons functioning as a polymodal sensor …

Discovery of BAY-390, a selective CNS penetrant chemical probe as transient receptor potential ankyrin 1 (TRPA1) antagonist

S Mesch, D Walter, A Laux-Biehlmann… - Journal of Medicinal …, 2023 - ACS Publications
Transient receptor potential ankyrin 1 (TRPA1) is a voltage-dependent, ligand-gated ion
channel, and activation thereof is linked to a variety of painful conditions. Preclinical studies …

Transient receptor potential ankyrin 1 (TRPA1) antagonists: a patent review (2015–2019)

H Chen, JA Terrett - Expert Opinion on Therapeutic Patents, 2020 - Taylor & Francis
Introduction TRPA1 is a non-selective cation channel predominantly expressed in sensory
neurons, and functions as an irritant sensor for a plethora of noxious external stimuli and …

Transient receptor potential ankyrin 1 (TRPA1) modulators: Recent update and future perspective

Z Hu, Y Zhang, W Yu, J Li, J Yao, J Zhang… - European Journal of …, 2023 - Elsevier
The transient receptor potential ankyrin 1 (TRPA1) channel is a non-selective cation channel
that senses irritant chemicals. Its activation is closely associated with pain, inflammation, and …

TRPA1 modulation by piperidine carboxamides suggests an evolutionarily conserved binding site and gating mechanism

T Chernov-Rogan, E Gianti, C Liu… - Proceedings of the …, 2019 - National Acad Sciences
The transient receptor potential ankyrin 1 (TRPA1) channel functions as an irritant sensor
and is a therapeutic target for treating pain, itch, and respiratory diseases. As a ligand-gated …

Development of novel azabenzofuran TRPA1 antagonists as in vivo tools

KW Copeland, AA Boezio, E Cheung, J Lee… - Bioorganic & Medicinal …, 2014 - Elsevier
The transient receptor potential ankyrin 1 (TRPA1) channel is activated by noxious stimuli
including chemical irritants and endogenous inflammatory mediators. Antagonists of this …

[HTML][HTML] TRPA1 as a drug target—promise and challenges

J Chen, DH Hackos - Naunyn-Schmiedeberg's archives of pharmacology, 2015 - Springer
The transient receptor potential ankyrin 1 (TRPA1) channel is a nonselective cation channel
belonging to the superfamily of transient receptor potential (TRP) channels. It is …

Transient receptor potential ankyrin 1 (TRPA1) channel as emerging target for novel analgesics and anti-inflammatory agents

PG Baraldi, D Preti, S Materazzi… - Journal of medicinal …, 2010 - ACS Publications
1. Introduction 1. a. TRP Channels and TRPA1. The identification of the first transient
receptor potential (TRPa) channel originated from the observation that, in contrast to the …

Transient receptor potential ankyrin 1 (TRPA1) antagonists

D Preti, G Saponaro, A Szallasi - Pharmaceutical patent analyst, 2015 - Future Science
The transient receptor potential ankyrin 1 (TRPA1) channel is an irritant sensor highly
expressed on nociceptive neurons. The clinical use of TRPA1 antagonists is based on the …