Pharmacological characterization of a novel centrally permeable P2X7 receptor antagonist: JNJ‐47965567

…, L Aluisio, I Fraser, D Nepomuceno… - British journal of …, 2013 - Wiley Online Library
Background and Purpose An increasing body of evidence suggests that the purinergic
receptor P2X , ligand‐gated ion channel, 7 ( P2X7 ) in the CNS may play a key role in …

[HTML][HTML] INSL5 is a high affinity specific agonist for GPCR142 (GPR100)

…, J Chen, P Bonaventure, J Wu, D Nepomuceno… - Journal of Biological …, 2005 - ASBMB
Insulin-like peptide 5 (INSL5) is a peptide that belongs to the relaxin/insulin family, and its
receptor has not been identified. In this report, we demonstrate that INSL5 is a specific agonist …

[HTML][HTML] R3 (BΔ23–27) R/I5 chimeric peptide, a selective antagonist for GPCR135 and GPCR142 over relaxin receptor LGR7: In vitro and in vivo characterization

…, C Pudiak, J Shelton, J Zhu, D Nepomuceno… - Journal of Biological …, 2007 - ASBMB
Both relaxin-3 and its receptor (GPCR135) are expressed predominantly in brain regions
known to play important roles in processing sensory signals. Recent studies have shown that …

Relaxin-3/insulin-like peptide 5 chimeric peptide, a selective ligand for G protein-coupled receptor (GPCR) 135 and GPCR142 over leucine-rich repeat-containing G …

C Liu, J Chen, C Kuei, S Sutton, D Nepomuceno… - Molecular …, 2005 - ASPET
Relaxin-3, the most recently identified member of relaxin/insulin family, is an agonist for
leucine-rich repeat-containing G protein-coupled receptor (LGR)7, GPCR135, and GPCR142. …

Distribution of G-protein-coupled receptor (GPCR) 135 binding sites and receptor mRNA in the rat brain suggests a role for relaxin-3 in neuroendocrine and sensory …

…, C Kuei, B Roland, J Chen, D Nepomuceno… - …, 2005 - karger.com
G-protein-coupled receptor 135 (GPCR135), a former orphan GPCR also known as SALPR,
has recently been shown to be modulated by relaxin-3 (R3). In addition to GPCR135, R3 …

Translational evaluation of JNJ-18038683, a 5-hydroxytryptamine type 7 receptor antagonist, on rapid eye movement sleep and in major depressive disorder

…, L Dvorak, I Fraser, B Lord, D Nepomuceno… - … of Pharmacology and …, 2012 - ASPET
In rodents 5-hydroxytryptamine type 7 (5-HT 7 ) receptor blockade has been shown to be
effective in models of depression and to increase the latency to rapid eye movement (REM) …

A selective orexin-1 receptor antagonist attenuates stress-induced hyperarousal without hypnotic effects

…, BT Shireman, TP Lebold, D Nepomuceno… - … of Pharmacology and …, 2015 - ASPET
Orexins (OXs) are peptides produced by perifornical (PeF) and lateral hypothalamic neurons
that exert a prominent role in arousal-related processes, including stress. A critical role for …

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

…, J Shelton, S Yun, D Nepomuceno… - … 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) …

GPR139, an orphan receptor highly enriched in the habenula and septum, is activated by the essential amino acids L-tryptophan and L-phenylalanine

C Liu, P Bonaventure, G Lee, D Nepomuceno… - Molecular …, 2015 - ASPET
GPR139 is an orphan G-protein–coupled receptor expressed in the central nervous system.
To identify its physiologic ligand, we measured GPR139 receptor activity from recombinant …

Pharmacological characterization of relaxin-3/INSL7 receptors GPCR135 and GPCR142 from different mammalian species

…, SW Sutton, P Bonaventure, D Nepomuceno… - … of Pharmacology and …, 2005 - ASPET
Relaxin-3 has recently been identified as a ligand for two structurally related G-protein-coupled
receptors, human GPCR135 and GPCR142. This current study reports the …