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 …

Transient receptor potential vanilloid-1 antagonists: a survey of recent patent literature

EA Voight, ME Kort - Expert Opinion on Therapeutic Patents, 2010 - Taylor & Francis
Importance of the field: Transient receptor potential vanilloid-1 (TRPV1, vanilloid receptor-1)
is a nonspecific cation channel that can be activated by multiple endogenous stimuli and by …

Discovery of (S)–N-(3-isopropylphenyl)-2-(5-phenylthiazol-2-yl) pyrrolidine-1-carboxamide as potent and brain-penetrant TRPV1 antagonist

Y Qiao, Y Zhang, Z Qiao, W He, Y Chen, D Song… - European Journal of …, 2022 - Elsevier
Transient receptor potential vanilloid 1 (TRPV1) antagonists can inhibit the transmission of
nociceptive signals from the peripheral to the central nervous system (CNS), providing a …

A capsaicinoid-based soft drug, AG1529, for attenuating TRPV1-mediated histaminergic and inflammatory sensory neuron excitability

M Nikolaeva-Koleva, L Butron… - Scientific Reports, 2021 - nature.com
TRPV1, a member of the transient receptor potential (TRP) family, is a nonselective calcium
permeable ion channel gated by physical and chemical stimuli. In the skin, TRPV1 plays an …

Discovery of nonpungent transient receptor potential vanilloid 1 (TRPV1) agonist as strong topical analgesic

J Ann, HS Kim, SA Thorat, H Kim, HJ Ha… - Journal of medicinal …, 2019 - ACS Publications
Paradoxically, some TRPV1 agonists are, at the organismal level, both nonpungent and
clinically useful as topical analgesics. Here, we describe the scaled-up synthesis and …

Activation of the transient receptor potential vanilloid‐1 (TRPV1) channel opens the gate for pain relief

G Jancsó, M Dux, O Oszlács… - British Journal of …, 2008 - Wiley Online Library
Pharmacological modulation of the transient receptor potential vanilloid‐1 (TRPV1) receptor
function offers a promising means of producing pain relief at the level of the primary sensory …

Intrathecal administration of AS1928370, a transient receptor potential vanilloid 1 antagonist, attenuates mechanical allodynia in a mouse model of neuropathic pain

T Watabiki, T Kiso, M Tsukamoto, T Aoki… - Biological and …, 2011 - jstage.jst.go.jp
Transient receptor potential vanilloid 1 (TRPV1) is primarily expressed in central and
peripheral terminals of non-myelinated primary afferent neurons. We previously showed that …

Transient receptor potential vanilloid type 1 and pain development

E Palazzo, L Luongo, V de Novellis, F Rossi… - Current opinion in …, 2012 - Elsevier
Transient receptor potential vanilloid type 1 (TRPV1), a ligand-gated cation channel, is a
polymodal nocitransducer widely expressed within pain transmitting/modulating areas of the …

Mode-selective inhibitory effects of eugenol on the mouse TRPV1 channel

K Takahashi, T Yoshida, M Wakamori - Biochemical and Biophysical …, 2021 - Elsevier
The transient receptor potential vanilloid 1 (TRPV1) channel is a polymodal receptor in
sensory nerves and involved in pain sensation. TRPV1 has at least three distinct activation …

Pharmacology of the capsaicin receptor, transient receptor potential vanilloid type-1 ion channel

I Nagy, D Friston, JS Valente, JVT Perez… - Capsaicin as a …, 2014 - Springer
The capsaicin receptor, transient receptor potential vanilloid type 1 ion channel (TRPV1),
has been identified as a polymodal transducer molecule on a sub-set of primary sensory …