Despite the increasing interest in TRPA1 channel as a pain target, its role in cold sensation
and body temperature regulation is not clear; the efficacy and particularly side effects …

Clinical data demonstrating target-mediated elevation of core body temperature in humans
have been a major setback in the development of TRPV1 antagonists as novel therapeutics …

1-Benzyl-5-aryltetrazoles were discovered to be novel antagonists for the P2X 7 receptor.
Structure−activity relationship (SAR) studies were conducted around both the benzyl and …

Growing evidence supports a role for the immune system in the induction and maintenance
of chronic pain. ATP is a key neurotransmitter in this process. Recent studies demonstrate …

… Platinum-iridium microelectrodes (Frederick Haer, Brunswick, ME) were used to record
extracellular activity of spinal dorsal horn neurons. The activity of WDR neurons was recorded …

Transient receptor potential vanilloid type 1 (TRPV1) is a ligand-gated ion channel that
functions as an integrator of multiple pain stimuli including heat, acid, capsaicin and a variety of …

… Continuing work in the aryl(benzyl)urea class, a variety of NH and N-Me indazole ureas
20 were disclosed, all with bulky aliphatic ortho substitutents on the benzyl portion of the …

The discovery of TRPV1 antagonists as a new class of analgesic agents for the treatment of
chronic pathological pain has been pursued aggressively across the pharmaceutical industry…

TRPA1 is an excitatory, nonselective cation channel implicated in somatosensory function,
pain, and neurogenic inflammation. Through covalent modification of cysteine and lysine …

The preparation and characterization of a series of C-10 substituted 5-allyl-2,5-dihydro-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines
as a novel class of selective ligands for the …