A-425619 [1-isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea], a novel transient receptor potential type V1 receptor antagonist, relieves pathophysiological pain …

P Honore, CT Wismer, J Mikusa, CZ Zhu… - … of Pharmacology and …, 2005 - ASPET
The vanilloid receptor 1 (VR1, TRPV1), which is a member of the transient receptor potential
(TRP) superfamily, is highly localized on peripheral and central processes of nociceptive …

A-425619 [1-isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea], a novel and selective transient receptor potential type V1 receptor antagonist, blocks channel …

R El Kouhen, CS Surowy, BR Bianchi… - … of Pharmacology and …, 2005 - ASPET
The vanilloid receptor transient receptor potential type V1 (TRPV1) integrates responses to
multiple stimuli, such as capsaicin, acid, heat, and endovanilloids and plays an important …

Antinociceptive pharmacology of N-(4-chlorobenzyl)-N′-(4-hydroxy-3-iodo-5-methoxybenzyl) thiourea, a high-affinity competitive antagonist of the transient receptor …

L Tang, Y Chen, Z Chen, PM Blumberg… - … of Pharmacology and …, 2007 - ASPET
The transient receptor potential vanilloid 1 receptor (TRPV1) is expressed predominantly in
a subset of primary afferent nociceptors. Due to its specific anatomical location and its …

Amelioration of neuropathic pain by novel transient receptor potential vanilloid 1 antagonist AS1928370 in rats without hyperthermic effect

T Watabiki, T Kiso, T Kuramochi, K Yonezawa… - … of Pharmacology and …, 2011 - ASPET
Transient receptor potential vanilloid 1 (TRPV1) is activated by a variety of stimulations, such
as endogenous ligands and low pH, and is believed to play a role in pain transmission …

Antihyperalgesic effects of (R, E)-N-(2-hydroxy-2, 3-dihydro-1H-inden-4-yl)-3-(2-(piperidin-1-yl)-4-(trifluoromethyl) phenyl)-acrylamide (AMG8562), a novel transient …

SG Lehto, R Tamir, H Deng, L Klionsky, R Kuang… - … of Pharmacology and …, 2008 - ASPET
Antagonists of the vanilloid receptor TRPV1 (transient receptor potential vanilloid type 1)
have been reported to produce antihyperalgesic effects in animal models of pain. These …

Design of Potent, Orally Available Antagonists of the Transient Receptor Potential Vanilloid 1. Structure−Activity Relationships of 2-Piperazin-1-yl-1H-benzimidazoles

VI Ognyanov, C Balan, AW Bannon, Y Bo… - Journal of medicinal …, 2006 - ACS Publications
The vanilloid receptor-1 (VR1 or TRPV1) is a membrane-bound, nonselective cation
channel that is predominantly expressed by peripheral neurons sensing painful stimuli …

Novel transient receptor potential vanilloid 1 receptor antagonists for the treatment of pain: structure− activity relationships for ureas with quinoline, isoquinoline …

A Gomtsyan, EK Bayburt, RG Schmidt… - Journal of medicinal …, 2005 - ACS Publications
Novel transient receptor potential vanilloid 1 (TRPV1) receptor antagonists with various
bicyclic heteroaromatic pharmacophores were synthesized, and their in vitro activity in …

AMG 9810 [(E)-3-(4-t-butylphenyl)-N-(2, 3-dihydrobenzo [b][1, 4] dioxin-6-yl) acrylamide], a novel vanilloid receptor 1 (TRPV1) antagonist with antihyperalgesic …

NR Gavva, R Tamir, Y Qu, L Klionsky, TJ Zhang… - … of Pharmacology and …, 2005 - ASPET
The vanilloid receptor 1 (VR1 or TRPV1) is a membrane-bound, nonselective cation channel
expressed by peripheral sensory neurons. TRPV1 antagonists produce antihyperalgesic …

Characterization of SB-705498, a potent and selective vanilloid receptor-1 (VR1/TRPV1) antagonist that inhibits the capsaicin-, acid-, and heat-mediated activation of …

MJ Gunthorpe, SL Hannan, D Smart, JC Jerman… - … of Pharmacology and …, 2007 - ASPET
Vanilloid receptor-1 (TRPV1) is a nonselective cation channel, predominantly expressed by
sensory neurons, which plays a key role in the detection of noxious painful stimuli such as …

Role of transient receptor potential vanilloid 1 in inflammation and autoimmune diseases

F Tsuji, H Aono - Pharmaceuticals, 2012 - mdpi.com
Transient receptor potential vanilloid 1 (TRPV1), a non-selective cation channel, is a
receptor activated by high temperatures and chemical agonists such as the vanilloids and …