P2X receptor antagonists for pain management: examination of binding and physicochemical properties

Inhibition of Neuronal Voltage-Gated Sodium Channels by Brilliant Blue G

(2011) S. Jo et al.   MOLECULAR PHARMACOLOGY

P2X7 receptor-deficient mice are susceptible to bone cancer pain

(2011) Rikke Rie Hansen et al.   PAIN

Defining Desirable Central Nervous System Drug Space through the Alignment of Molecular Properties, in Vitro ADME, and Safety Attributes

(2010) Travis T. Wager et al.   ACS Chemical Neuroscience

Moving beyond Rules: The Development of a Central Nervous System Multiparameter Optimization (CNS MPO) Approach To Enable Alignment of Druglike Properties

(2010) Travis T. Wager et al.   ACS Chemical Neuroscience

Discovery of 2-chloro-N-((4,4-difluoro-1-hydroxycyclohexyl)methyl)-5-(5-fluoropyrimidin-2-yl)benzamide as a potent and CNS penetrable P2X7 receptor antagonist

(2010) Xiangyang Chen et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

AF-353, a novel, potent and orally bioavailable P2X3/P2X2/3 receptor antagonist

(2010) Joel R Gever et al.   BRITISH JOURNAL OF PHARMACOLOGY

P2X purinergic receptor ligands: recently patented compounds

(2010) Hendra Gunosewoyo et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Central sensitization: Implications for the diagnosis and treatment of pain

(2010) Clifford J. Woolf   PAIN

Emerging structures and ligands for P2X3 and P2X4 receptors—towards novel treatments of neuropathic pain

(2010) Christa E. Müller   Purinergic Signalling

The antihyperalgesic activity of a selective P2X7 receptor antagonist, A-839977, is lost in IL-1αβ knockout mice

(2009) Prisca Honore et al.   BEHAVIOURAL BRAIN RESEARCH

Inhibition of serotonin and norepinephrine reuptake and inhibition of phosphodiesterase by multi-target inhibitors as potential agents for depression

(2009) John R. Cashman et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Identification and SAR of novel diaminopyrimidines. Part 2: The discovery of RO-51, a potent and selective, dual P2X3/P2X2/3 antagonist for the treatment of pain

(2009) Alam Jahangir et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X3/P2X2/3 antagonist for the treatment of pain

(2009) David S. Carter et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Using the Golden Triangle to optimize clearance and oral absorption

(2009) Ted W. Johnson et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and in vivo evaluation of 3-substituted gababutins

(2009) David C. Blakemore et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery and optimization of RO-85, a novel drug-like, potent, and selective P2X3 receptor antagonist

(2009) Christine E. Brotherton-Pleiss et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Mammalian P2X7 receptor pharmacology: comparison of recombinant mouse, rat and human P2X7 receptors

(2009) Diana L Donnelly-Roberts et al.   BRITISH JOURNAL OF PHARMACOLOGY

Cellular and Molecular Mechanisms of Pain

(2009) Allan I. Basbaum et al.   CELL

Pharmacological Promiscuity: Dependence on Compound Properties and Target Specificity in a Set of Recent Roche Compounds

(2009) Jens-Uwe Peters et al.   ChemMedChem

Structure−Brain Exposure Relationships in Rat and Human Using a Novel Data Set of Unbound Drug Concentrations in Brain Interstitial and Cerebrospinal Fluids

(2009) Markus Fridén et al.   JOURNAL OF MEDICINAL CHEMISTRY

Antagonists of the P2X7Receptor. From Lead Identification to Drug Development

(2009) Simon D. Guile et al.   JOURNAL OF MEDICINAL CHEMISTRY

Morphine Enhances Microglial Migration through Modulation of P2X4 Receptor Signaling

(2009) R. J. Horvath et al.   JOURNAL OF NEUROSCIENCE

P2X4-Receptor-Mediated Synthesis and Release of Brain-Derived Neurotrophic Factor in Microglia Is Dependent on Calcium and p38-Mitogen-Activated Protein Kinase Activation

(2009) T. Trang et al.   JOURNAL OF NEUROSCIENCE

Crystal structure of the ATP-gated P2X4 ion channel in the closed state

(2009) Toshimitsu Kawate et al.   NATURE

The P2X7 receptor–pannexin connection to dye uptake and IL-1β release

(2009) Pablo Pelegrin et al.   Purinergic Signalling

Reconstruction of the P2X2 Receptor Reveals a Vase-Shaped Structure with Lateral Tunnels above the Membrane

(2009) Kazuhiro Mio et al.   STRUCTURE

The neural–glial purinergic receptor ensemble in chronic pain states

(2009) Michael F. Jarvis   TRENDS IN NEUROSCIENCES

Physiochemical drug properties associated with in vivo toxicological outcomes

(2008) Jason D. Hughes et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Blood–brain barrier permeability considerations for CNS-targeted compound library design

(2008) Stephen A Hitchcock   CURRENT OPINION IN CHEMICAL BIOLOGY

The P2X7receptor as a therapeutic target

(2008) Romeo Romagnoli et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Fibronectin/integrin system is involved in P2X4 receptor upregulation in the spinal cord and neuropathic pain after nerve injury

(2008) Makoto Tsuda et al.   GLIA

Phosphoinositides Regulate P2X4 ATP-Gated Channels through Direct Interactions

(2008) L.-P. Bernier et al.   JOURNAL OF NEUROSCIENCE

Up-Regulation of P2X4 Receptors in Spinal Microglia after Peripheral Nerve Injury Mediates BDNF Release and Neuropathic Pain

(2008) L. Ulmann et al.   JOURNAL OF NEUROSCIENCE

Characterization of N-(Adamantan-1-ylmethyl)-5-[(3R-aminopyrrolidin-1-yl)methyl]-2-chloro-benzamide, a P2X7 Antagonist in Animal Models of Pain and Inflammation

(2008) D. C. Broom et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

ATP-gated P2X cation-channels

(2008) Michael F. Jarvis et al.   NEUROPHARMACOLOGY

The purinergic antagonist PPADS reduces pain related behaviours and interleukin-1β, interleukin-6, iNOS and nNOS overproduction in central and peripheral nervous system after peripheral neuropathy in mice

(2007) Cataldo Martucci et al.   PAIN