Selective blockade of the capsaicin receptor TRPV1 attenuates bone cancer pain

…, SR Chaplan, AE Dubin, NI Carruthers… - Journal of …, 2005 - Soc Neuroscience
Cancer colonization of bone leads to the activation of osteoclasts, thereby producing local
tissue acidosis and bone resorption. This process may contribute to the generation of both …

The First Potent and Selective Non-Imidazole Human Histamine H4 Receptor Antagonists

…, TW Lovenberg, NI Carruthers - Journal of medicinal …, 2003 - ACS Publications
Following the discovery of the human histamine H 4 receptor, a high throughput screen of our
corporate compound collection identified compound 6 as a potential lead. Investigation of …

Enriching extracellular vesicles for mass spectrometry

JB Burton, NJ Carruthers… - Mass Spectrometry …, 2023 - Wiley Online Library
Extracellular vesicles from plasma, other body fluids and cell culture media hold great promise
in the search for biomarkers. Exosomes in particular, the vesicle type that is secreted after …

Blockade of orexin-1 receptors attenuates orexin-2 receptor antagonism-induced sleep promotion in the rat

…, S Yun, X Li, B Lord, CA Dvorak, NI Carruthers… - … of Pharmacology and …, 2009 - ASPET
Orexins are peptides produced by lateral hypothalamic neurons that exert a prominent role
in the maintenance of wakefulness by activating orexin-1 (OX1R) and orexin-2 (OX2R) …

Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2-yl) piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl) amide, a high affinity TRPV1 (VR1 …

…, SP Zhang, SR Chaplan, NI Carruthers - Journal of medicinal …, 2005 - ACS Publications
High throughput screening using the recombinant human TRPV1 receptor was used to identify
a series of pyridinylpiperazine ureas (3) as TRPV1 vanilloid receptor ligands. Exploration …

Copper-mediated synthesis of drug-like bicyclopentanes

…, C Le, SJ McCarver, BT Shireman, NI Carruthers… - Nature, 2020 - nature.com
Multicomponent reactions are relied on in both academic and industrial synthetic organic
chemistry owing to their step- and atom-economy advantages over traditional synthetic …

Selective blockade of the orexin-2 receptor attenuates ethanol self-administration, place preference, and reinstatement

…, K Morton, J Palmer, P Bonaventure, NI Carruthers… - …, 2011 - Springer
Rationale Orexin-1 receptor antagonists have been shown to block the reinforcing effects of
drugs of abuse and food. However, whether blockade of orexin-2 receptor has similar effects …

Preparation and Biological Evaluation of Indole, Benzimidazole, and Thienopyrrole Piperazine Carboxamides:  Potent Human Histamine H4 Antagonists

…, TW Lovenberg, L Karlsson, NI Carruthers… - Journal of medicinal …, 2005 - ACS Publications
Three series of H 4 receptor ligands, derived from indoly-2-yl-(4-methyl-piperazin-1-yl)-methanones,
have been synthesized and their structure−activity relationships evaluated for …

Discovery and characterization of AMPA receptor modulators selective for TARP-γ8

…, T Steckler, AD Wickenden, NI Carruthers… - … of Pharmacology and …, 2016 - ASPET
Members of the α-amino-3-hydroxyl-5-methyl-4-isoxazole-propionic acid (AMPA) subtype of
ionotropic glutamate receptors mediate the majority of fast synaptic transmission within the …

Characterization of JNJ-42847922, a selective orexin-2 receptor antagonist, as a clinical candidate for the treatment of insomnia

…, M Rizzolio, M Letavic, NI Carruthers… - … of Pharmacology and …, 2015 - ASPET
Dual orexin receptor antagonists have been shown to promote sleep in various species,
including humans. Emerging research indicates that selective orexin-2 receptor (OX2R) …