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: 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 …

The pharmacological challenge to tame the transient receptor potential vanilloid‐1 (TRPV1) nocisensor

P Holzer - British journal of pharmacology, 2008 - Wiley Online Library
The transient receptor potential vanilloid‐1 (TRPV1) cation channel is a receptor that is
activated by heat (> 42° C), acidosis (pH< 6) and a variety of chemicals among which …

Nociception and pain in humans lacking a functional TRPV1 channel

B Katz, R Zaguri, S Edvardson… - The Journal of …, 2023 - Am Soc Clin Investig
BACKGROUND Chronic pain is a debilitating illness with currently limited therapy, in part
due to difficulties in translating treatments derived from animal models to patients. The …

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 …

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 …

TRPV1 function in health and disease

J PM White, L Urban, I Nagy - Current pharmaceutical …, 2011 - ingentaconnect.com
The transient receptor potential vanilloid type 1 ion channel (TRPV1) was identified as a
receptor responsible for mediating the intense burning sensation following exposure to heat …

Modulation of transient receptor vanilloid 1 activity by transient receptor potential ankyrin 1

V Spahn, C Stein, C Zöllner - Molecular pharmacology, 2014 - ASPET
Transient receptor potential vanilloid 1 (TRPV1) is a nonselective ligand-gated cation
channel responding to noxious heat, protons, and chemicals such as capsaicin. TRPV1 is …

Clinical development of TRPV1 antagonists: targeting a pivotal point in the pain pathway

MJ Gunthorpe, BA Chizh - Drug discovery today, 2009 - Elsevier
TRPV1 is a noxious heat, capsaicin (vanilloid) and acid receptor for which the development
of antagonists represents a novel therapeutic approach for the treatment of pain. TRPV1 …

TRPV1: a therapeutic target for novel analgesic drugs?

A Szallasi, F Cruz, P Geppetti - Trends in molecular medicine, 2006 - cell.com
The vanilloid receptor TRPV1 is now recognized as a molecular integrator of painful stimuli
ranging from noxious heat to endovanilloids in inflammation. Pharmacological blockade of …