Pungency of TRPV1 agonists is directly correlated with kinetics of receptor activation and lipophilicity

D Ursu, K Knopp, RE Beattie, B Liu, E Sher - European journal of …, 2010 - Elsevier
TRPV1 (transient receptor potential vanilloid 1) is a ligand-gated ion channel expressed
predominantly in nociceptive primary afferents that plays a key role in pain processing. In …

Pharmacodynamics of TRPV1 agonists in a bioassay using human PC‐3 cells

D Alvarez-Berdugo, M Jiménez… - The Scientific World …, 2014 - Wiley Online Library
Purpose. TRPV1 is a multimodal channel mainly expressed in sensory neurons. We aimed
to explore the pharmacodynamics of the TRPV1 agonists, capsaicin, natural capsaicinoids …

Acidification of rat TRPV1 alters the kinetics of capsaicin responses

TR Neelands, MF Jarvis, P Han, CR Faltynek… - Molecular …, 2005 - journals.sagepub.com
TRPV1 (vanilloid receptor 1) receptors are activated by a variety of ligands such as
capsaicin, as well as by acidic conditions and temperatures above 42° C. These activators …

TRPV1 activation and induction of nociceptive response by a non-pungent capsaicin-like compound, capsiate

T Iida, T Moriyama, K Kobata, A Morita, N Murayama… - …, 2003 - Elsevier
Capsiate is a capsaicin-like ingredient of a non-pungent cultivar of red pepper, CH-19
sweet. To elucidate the mechanisms underlying the non-pungency of capsiate, we …

[HTML][HTML] A randomised trial evaluating the effects of the TRPV1 antagonist SB705498 on pruritus induced by histamine, and cowhage challenge in healthy volunteers

RA Gibson, J Robertson, H Mistry, S McCallum… - PLoS …, 2014 - journals.plos.org
Background Transient receptor potential vanilloid type 1 (TRPV1) is a non-selective cation
channel widely expressed in skin tissues, and peripheral sensory nerve fibres. Activation of …

TRPV1 agonist approaches for pain management

KR Bley - Vanilloid receptor TRPV1 in drug discovery: targeting …, 2010 - Wiley Online Library
Capsaicin and other naturally occurring pungent molecules have been used for centuries as
topical analgesics to treat a variety of painful conditions. However, only within the last 12 …

Vanilloid receptors take a TRP beyond the sensory afferent☆

MJ Caterina - Pain, 2003 - journals.lww.com
The capsaicin receptor, TRPV1,(transient receptor potential channel-vanilloid subfamily
member 1) is a cation channel subunit expressed by a subset of nociceptive neurons in …

Vanilloid receptor TRPV1 is not activated by vanilloids applied intracellularly

L Vyklický, A Lyfenko, DP Kuffler, V Vlachová - Neuroreport, 2003 - journals.lww.com
The vanilloid receptor TRPV1 is a ligand-gated cation channel that can be activated by
capsaicin, acids and noxious heat. For vanilloids, a stretch of 8 amino acids in the vicinity of …

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 …

N-palmitoyl-vanillamide (palvanil) is a non-pungent analogue of capsaicin with stronger desensitizing capability against the TRPV1 receptor and anti-hyperalgesic …

L De Petrocellis, F Guida, AS Moriello… - Pharmacological …, 2011 - Elsevier
N-acyl-vanillamide (NAVAM) analogues of the natural pungent principle of capsicum,
capsaicin, were developed several years ago as potential non-pungent analgesic …