Medicinal chemistry, pharmacology, and clinical implications of TRPV1 receptor antagonists

M Aghazadeh Tabrizi, PG Baraldi… - Medicinal research …, 2017 - Wiley Online Library
Transient receptor potential vanilloid 1 (TRPV1) is an ion channel expressed on sensory
neurons triggering an influx of cations. TRPV1 receptors function as homotetramers …

TRPV1: a potential drug target for treating various diseases

R Brito, S Sheth, D Mukherjea, LP Rybak, V Ramkumar - Cells, 2014 - mdpi.com
Transient receptor potential vanilloid 1 (TRPV1) is an ion channel present on sensory
neurons which is activated by heat, protons, capsaicin and a variety of endogenous lipids …

Progress in the development of TRPV1 small-molecule antagonists: Novel Strategies for pain management

K Zhu, L Wang, TT Liao, W Li, J Zhou, Y You… - European journal of …, 2023 - Elsevier
Transient receptor potential vanilloid 1 (TRPV1) channels are widely distributed in sensory
nerve endings, the central nervous system, and other tissues, functioning as ion channel …

Modulation of the TRPV1 channel: current clinical trials and recent patents with focus on neurological conditions

L De Petrocellis, AS Moriello - Recent Patents on CNS Drug …, 2013 - ingentaconnect.com
The transient receptor potential vanilloid-1 cat ion channel (TRPV1) is a nonspecific cation
channel that can be activated by multiple endogenous stimuli and is expressed …

TRPV1: a target for next generation analgesics

LS Premkumar, P Sikand - Current neuropharmacology, 2008 - ingentaconnect.com
Transient Receptor Potential Vanilloid 1 (TRPV1) is a Ca2+ permeant non-selective cation
channel expressed in a subpopulation of primary afferent neurons. TRPV1 is activated by …

TRPV1: a target for rational drug design

V Carnevale, T Rohacs - Pharmaceuticals, 2016 - mdpi.com
Transient Receptor Potential Vanilloid 1 (TRPV1) is a non-selective, Ca2+ permeable cation
channel activated by noxious heat, and chemical ligands, such as capsaicin and …

TRPV1-targeted drugs in development for human pain conditions

M Iftinca, M Defaye, C Altier - Drugs, 2021 - Springer
The transient receptor potential vanilloid-1 (TRPV1) is a non-specific cation channel known
for its sensitivity to pungent vanilloid compound (ie capsaicin) and noxious stimuli, including …

TRPV1 antagonists as a potential treatment for hyperalgesia

LA Roberts, M Connor - Recent Patents on CNS Drug …, 2006 - ingentaconnect.com
The vanilloid receptor (TRPV1) is a member of the transient receptor potential family of ion
channels that is highly expressed in nociceptive primary afferent sensory neurons. TRPV1 is …

Modulation of the TRPV4 ion channel as a therapeutic target for disease

MS Grace, SJ Bonvini, MG Belvisi, P McIntyre - Pharmacology & …, 2017 - Elsevier
Abstract Transient Receptor Potential Vanilloid 4 (TRPV4) is a broadly expressed,
polymodally gated ion channel that plays an important role in many physiological and …

Recent progress in the development of selective TRPV1 antagonists for pain

LM Broad, SJ Keding, MJ Blanco - Current topics in medicinal …, 2008 - ingentaconnect.com
As last year marked the tenth anniversary of the cloning of TRPV1, no attenuation has been
observed in the intense interest surrounding this ion channel by both academic labs and …