In vitro characterization of the thermoneutral transient receptor potential vanilloid-1 (TRPV1) inhibitor GRTE16523

N Damann, G Bahrenberg, H Stockhausen… - European Journal of …, 2020 - Elsevier
The TRPV1 ion channel is a neuronal sensor that plays an important role in nociception and
neuropathic as well as inflammatory pain. In clinical trials, hyperthermia and thermo …

Clinical and preclinical experience with TRPV1 antagonists as potential analgesic agents

A Gomtsyan, JD Brederson - TRP Channels as Therapeutic Targets, 2015 - Elsevier
Identification of novel antagonists targeting the transient receptor potential vanilloid type 1
(TRPV1) protein has been at the forefront of pain research in the pharmaceutical industry for …

Triazine-based vanilloid 1 receptor open channel blockers: Design, synthesis, evaluation, and SAR analysis

M Vidal-Mosquera, A Fernández-Carvajal… - Journal of medicinal …, 2011 - ACS Publications
The thermosensory transient receptor potential vanilloid 1 channel (TRPV1) is a polymodal
receptor activated by physical and chemical stimuli. TRPV1 activity is drastically potentiated …

Therapeutic targeting of TRP channels-the TR (i) P to pain relief

SR Eid - Current topics in medicinal chemistry, 2011 - ingentaconnect.com
Following the cloning and characterization of the transient receptor potential vanilloid 1
(TRPV1), a growing body of research has identified the important role of TRPV1 and related …

A patent review of transient receptor potential vanilloid type 1 modulators (2014–present)

M Gao, Y Wang, L Liu, Z Qiao, L Yan - Expert Opinion on …, 2021 - Taylor & Francis
Introduction: Transient receptor potential vanilloid 1 (TRPV1) is a nonselective cation
channel with high permeability to calcium, which is widely expressed in the central nervous …

[图书][B] Vanilloid (TRPV1) and other transient receptor potential channels

M Trevisani, A Szallasi - 2009 - books.google.com
The neuropathic pain market in the United States is expected to nearly double from today's
$2.6 billion to $5 billion by 2018 according to a recent report by the market research firm …

Editorial [Hot Topic: New Developments in the Medicinal Chemistry of Vanilloid TRPV1 and Related Receptors (Guest Editor: Arpad Szallasi)]

A Szallasi - Current Topics in Medicinal Chemistry, 2011 - ingentaconnect.com
With 462 reviews over the past decade, Transient Receptor Potential (TRP) channels
arguably represent one of today's most extensively reviewed pharmacological targets. The …

TRPV1 ligands with hyperthermic, hypothermic and no temperature effects in rats

A Gomtsyan, HA McDonald, RG Schmidt, JF Daanen… - Temperature, 2015 - Taylor & Francis
Transient receptor potential vanilloid 1 (TRPV1) is a multifunctional ion channel playing
important roles in a numerous biological processes including the regulation of body …

Transient receptor potential vanilloid type 1 antagonists: a patent review (2011–2014)

Y Lee, S Hong, M Cui, PK Sharma, J Lee… - Expert opinion on …, 2015 - Taylor & Francis
Introduction: Transient receptor potential vanilloid type 1 (TRPV1) is a nonselective cation
channel that can be activated by noxious heat, low pH and vanilloid compounds such as …

TRPV1 analgesics disturb core body temperature via a biased allosteric mechanism involving conformations distinct from that for nociception

YZ Huang, JX Ma, YJ Bian, QR Bai, YH Gao, SK Di… - Neuron, 2024 - cell.com
Efforts on developing transient receptor potential vanilloid 1 (TRPV1) drugs for pain
management have been hampered by deleterious hypo-or hyperthermia caused by TRPV1 …