Pharmacological blockade of the vanilloid receptor TRPV1 elicits marked hyperthermia in humans
…, A Gore, GR Jang, JP Kesslak, L Ni, MH Norman… - Pain, 2008 - journals.lww.com
The vanilloid receptor TRPV1 has been identified as a molecular target for the treatment of
pain associated with inflammatory diseases and cancer. Hence, TRPV1 antagonists have …
pain associated with inflammatory diseases and cancer. Hence, TRPV1 antagonists have …
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 …
…, F Porreca, EM Doherty, MH Norman… - … 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 …
expressed by peripheral sensory neurons. TRPV1 antagonists produce antihyperalgesic …
The vanilloid receptor TRPV1 is tonically activated in vivo and involved in body temperature regulation
…, B Youngblood, D Zhu, MH Norman… - Journal of …, 2007 - Soc Neuroscience
The vanilloid receptor TRPV1 (transient receptor potential vanilloid 1) is a cation channel that
serves as a polymodal detector of pain-producing stimuli such as capsaicin, protons (pH <…
serves as a polymodal detector of pain-producing stimuli such as capsaicin, protons (pH <…
The transient receptor potential vanilloid-1 channel in thermoregulation: a thermosensor it is not
The development of antagonists of the transient receptor potential vanilloid-1 (TRPV1) channel
as pain therapeutics has revealed that these compounds cause hyperthermia in humans. …
as pain therapeutics has revealed that these compounds cause hyperthermia in humans. …
Nonthermal activation of transient receptor potential vanilloid-1 channels in abdominal viscera tonically inhibits autonomic cold-defense effectors
…, JL Roberts, AW Bannon, MH Norman… - Journal of …, 2007 - Soc Neuroscience
An involvement of the transient receptor potential vanilloid (TRPV) 1 channel in the regulation
of body temperature (T b ) has not been established decisively. To provide decisive …
of body temperature (T b ) has not been established decisively. To provide decisive …
Effect of linking bridge modifications on the antipsychotic profile of some phthalimide and isoindolinone derivatives
MH Norman, DJ Minick, GC Rigdon - Journal of medicinal …, 1996 - ACS Publications
A series of phthalimide and isoindolinone derivatives bridged to 4-(1,2-benzisothiazol-3-yl)-1-piperazinyl
was prepared. The compounds were evaluated in vitro at dopamine D 2 and …
was prepared. The compounds were evaluated in vitro at dopamine D 2 and …
Repeated administration of vanilloid receptor TRPV1 antagonists attenuates hyperthermia elicited by TRPV1 blockade
…, J Wang, W Wang, G Zajic, D Zhu, MH Norman… - … of Pharmacology and …, 2007 - ASPET
Capsaicin, the active ingredient in some pain-relieving creams, is an agonist of a nonselective
cation channel known as the transient receptor potential vanilloid type 1 (TRPV1). The …
cation channel known as the transient receptor potential vanilloid type 1 (TRPV1). The …
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 …
…, B Youngblood, M Zhang, D Zhu, MH Norman… - … 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 …
have been reported to produce antihyperalgesic effects in animal models of pain. These …
Discovery and optimization of a series of benzothiazole phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors
…, N Zhang, P Hughes, MH Norman - Journal of medicinal …, 2011 - ACS Publications
Phosphoinositide 3-kinase α (PI3Kα) is a lipid kinase that plays a key regulatory role in
several cellular processes. The mutation or amplification of this kinase in humans has been …
several cellular processes. The mutation or amplification of this kinase in humans has been …
Discovery of 1H-Pyrazol-3(2H)-ones as Potent and Selective Inhibitors of Protein Kinase R-like Endoplasmic Reticulum Kinase (PERK)
…, P Mitchell, MH Norman… - Journal of medicinal …, 2015 - ACS Publications
The structure-based design and optimization of a novel series of selective PERK inhibitors
are described resulting in the identification of 44 as a potent, highly selective, and orally …
are described resulting in the identification of 44 as a potent, highly selective, and orally …