P2X receptor antagonists for pain management: examination of binding and physicochemical properties
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[1] P. Leeson,et al. The influence of drug-like concepts on decision-making in medicinal chemistry , 2007, Nature Reviews Drug Discovery.
[2] T. Ritchie,et al. The impact of aromatic ring count on compound developability--are too many aromatic rings a liability in drug design? , 2009, Drug discovery today.
[3] G. Dubyak,et al. Oxidized ATP (oATP) attenuates proinflammatory signaling via P2 receptor‐independent mechanisms , 2003, British journal of pharmacology.
[4] J. Krause,et al. 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, Journal of Pharmacology and Experimental Therapeutics.
[5] C. Gabel,et al. Interleukin-1 beta maturation and release in response to ATP and nigericin. Evidence that potassium depletion mediated by these agents is a necessary and common feature of their activity. , 1994, The Journal of biological chemistry.
[6] C. Keele,et al. Observations on the algogenic actions of adenosine compounds on the human blister base preparation , 1977, Pain.
[7] D. Donnelly-roberts,et al. Painful Purinergic Receptors , 2008, Journal of Pharmacology and Experimental Therapeutics.
[8] D. Chadwick,et al. Purinergic signalling in neuron-glia interactions , 2006 .
[9] Susanne Winiwarter,et al. Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. , 2009, Journal of medicinal chemistry.
[10] J. Ando,et al. Fibronectin/integrin system is involved in P2X4 receptor upregulation in the spinal cord and neuropathic pain after nerve injury , 2008, Glia.
[11] Y. Hiroaki,et al. Reconstruction of the P2X(2) receptor reveals a vase-shaped structure with lateral tunnels above the membrane. , 2009, Structure.
[12] F. Di Virgilio,et al. The P2X7 Receptor: A Key Player in IL-1 Processing and Release1 , 2006, The Journal of Immunology.
[13] J. Cashman,et al. Inhibition of serotonin and norepinephrine reuptake and inhibition of phosphodiesterase by multi-target inhibitors as potential agents for depression. , 2009, Bioorganic & medicinal chemistry.
[14] D. Donnelly-roberts,et al. The antihyperalgesic activity of a selective P2X7 receptor antagonist, A-839977, is lost in IL-1αβ knockout mice , 2009, Behavioural Brain Research.
[15] J. de Zeeuw,et al. [Acute and chronic pain]. , 2005, Medizinische Klinik.
[16] David Julius,et al. Cellular and Molecular Mechanisms of Pain , 2009, Cell.
[17] T. Brennan,et al. A-317491, a novel potent and selective non-nucleotide antagonist of P2X3 and P2X2/3 receptors, reduces chronic inflammatory and neuropathic pain in the rat , 2002, Proceedings of the National Academy of Sciences of the United States of America.
[18] K. Jacobson. P2X and P2Y Receptors , 2010 .
[19] E. Gouaux,et al. Crystal structure of the ATP-gated P2X4 ion channel in the closed state , 2009, Nature.
[20] G. Pei,et al. Human μ-opioid receptor overexpressed in Sf9 insect cells functionally coupled to endogenous Gi/o proteins , 2000, Cell Research.
[21] A. Surprenant,et al. The P2X7 receptor–pannexin connection to dye uptake and IL-1β release , 2009, Purinergic Signalling.
[22] M. Kassiou,et al. P2X purinergic receptor ligands: recently patented compounds , 2010, Expert opinion on therapeutic patents.
[23] H. Tozaki-Saitoh,et al. Modification of neuropathic pain sensation through microglial ATP receptors , 2007, Purinergic Signalling.
[24] C. Gabel,et al. Absence of the P2X7 Receptor Alters Leukocyte Function and Attenuates an Inflammatory Response , 2002, The Journal of Immunology.
[25] F. Lombardo,et al. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings , 1997 .
[26] J. Gever,et al. Discovery and optimization of RO-85, a novel drug-like, potent, and selective P2X3 receptor antagonist. , 2010, Bioorganic & medicinal chemistry letters.
[27] D. Donnelly-roberts,et al. P2X7-related modulation of pathological nociception in rats , 2007, Neuroscience.
[28] M. Jarvis. Contributions of P2X3 homomeric and heteromeric channels to acute and chronic pain , 2003, Expert opinion on therapeutic targets.
[29] Betsy S. Pierce,et al. 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, Bioorganic & medicinal chemistry letters.
[30] J. Deleo,et al. Morphine Enhances Microglial Migration through Modulation of P2X4 Receptor Signaling , 2009, The Journal of Neuroscience.
[31] T. van Biesen,et al. Modulation of BzATP and formalin induced nociception: attenuation by the P2X receptor antagonist, TNP‐ATP and enhancement by the P2X3 allosteric modulator, cibacron blue , 2001, British journal of pharmacology.
[32] R. North,et al. Brilliant blue G selectively blocks ATP-gated rat P2X(7) receptors. , 2000, Molecular pharmacology.
[33] J. Sullivan,et al. Interleukin-1alphabeta gene-deficient mice show reduced nociceptive sensitivity in models of inflammatory and neuropathic pain but not post-operative pain. , 2006, Behavioural brain research.
[34] S. Beggs,et al. 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, The Journal of Neuroscience.
[35] R. North,et al. Rapid secretion of interleukin-1β by microvesicle shedding , 2001 .
[36] P. Verhoest,et al. Moving beyond rules: the development of a central nervous system multiparameter optimization (CNS MPO) approach to enable alignment of druglike properties. , 2010, ACS chemical neuroscience.
[37] B. Khakh,et al. ATP-gated P2X cation-channels , 2009, Neuropharmacology.
[38] J. Sawynok. Adenosine and ATP receptors. , 2007, Handbook of experimental pharmacology.
[39] S. Stojilkovic,et al. P2X7 receptor-deficient mice are susceptible to bone cancer pain , 2011, PAIN®.
[40] P. Verhoest,et al. Defining desirable central nervous system drug space through the alignment of molecular properties, in vitro ADME, and safety attributes. , 2010, ACS chemical neuroscience.
[41] J. Gever,et al. Identification and SAR of novel diaminopyrimidines. Part 2: The discovery of RO-51, a potent and selective, dual P2X(3)/P2X(2/3) antagonist for the treatment of pain. , 2009, Bioorganic & medicinal chemistry letters.
[42] K. Jacobson,et al. Purine and pyrimidine (P2) receptors as drug targets. , 2002, Journal of medicinal chemistry.
[43] F. Conquet,et al. Up-Regulation of P2X4 Receptors in Spinal Microglia after Peripheral Nerve Injury Mediates BDNF Release and Neuropathic Pain , 2008, The Journal of Neuroscience.
[44] C. Müller. Emerging structures and ligands for P2X3 and P2X4 receptors—towards novel treatments of neuropathic pain , 2010, Purinergic Signalling.
[45] Yves De Koninck,et al. Trans-synaptic shift in anion gradient in spinal lamina I neurons as a mechanism of neuropathic pain , 2003, Nature.
[46] J. Peters,et al. Pharmacological Promiscuity: Dependence on Compound Properties and Target Specificity in a Set of Recent Roche Compounds , 2009, ChemMedChem.
[47] J. Falgueyret,et al. Biochemical and pharmacological profile of a tetrasubstituted furanone as a highly selective COX‐2 inhibitor , 1997, British journal of pharmacology.
[48] J. Gever,et al. Pharmacology of P2X channels , 2006, Pflügers Archiv.
[49] O. Cruz-López,et al. From tyrosine to glycine: synthesis and biological activity of potent antagonists of the purinergic P2X7 receptor. , 2007, Journal of medicinal chemistry.
[50] S. McMahon,et al. ATP in human skin elicits a dose-related pain response which is potentiated under conditions of hyperalgesia. , 2000, Brain : a journal of neurology.
[51] C. Shieh,et al. P2X receptor ligands and pain , 2006, Expert opinion on therapeutic patents.
[52] J. Gever,et al. Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X(3)/P2X(2/3) antagonist for the treatment of pain. , 2009, Bioorganic & medicinal chemistry letters.
[53] D. Donnelly-roberts,et al. A-740003 [N-(1-{[(Cyanoimino)(5-quinolinylamino) methyl]amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide], a Novel and Selective P2X7 Receptor Antagonist, Dose-Dependently Reduces Neuropathic Pain in the Rat , 2006, Journal of Pharmacology and Experimental Therapeutics.
[54] H. Tozaki-Saitoh,et al. Lyn tyrosine kinase is required for P2X4 receptor upregulation and neuropathic pain after peripheral nerve injury , 2008, Glia.
[55] J. Gever,et al. AF‐353, a novel, potent and orally bioavailable P2X3/P2X2/3 receptor antagonist , 2010, British journal of pharmacology.
[56] E. Perl,et al. Ideas about pain, a historical view , 2007, Nature Reviews Neuroscience.
[57] S. Maeda,et al. Intrathecal administration of ATP produces long-lasting allodynia in rats: Differential mechanisms in the phase of the induction and maintenance , 2007, Neuroscience.
[58] S. Hitchcock,et al. Blood-brain barrier permeability considerations for CNS-targeted compound library design. , 2008, Current opinion in chemical biology.
[59] P. Leeson,et al. A comparison of physiochemical property profiles of development and marketed oral drugs. , 2003, Journal of medicinal chemistry.
[60] P. Anand,et al. Disruption of the P2X7 purinoceptor gene abolishes chronic inflammatory and neuropathic pain , 2005, Pain.
[61] B. Bean,et al. Inhibition of Neuronal Voltage-Gated Sodium Channels by Brilliant Blue G , 2011, Molecular Pharmacology.
[62] M. Jarvis. The neural–glial purinergic receptor ensemble in chronic pain states , 2010, Trends in Neurosciences.
[63] O. Cruz-López,et al. The P2X7 receptor as a therapeutic target , 2008, Expert opinion on therapeutic targets.
[64] Kazuhide Inoue. The function of microglia through purinergic receptors: neuropathic pain and cytokine release. , 2006, Pharmacology & therapeutics.
[65] J. T. Metz,et al. Ligand efficiency indices as guideposts for drug discovery. , 2005, Drug discovery today.
[66] P. Séguéla,et al. Differential regulation of microglial P2X4 and P2X7 ATP receptors following LPS-induced activation , 2007, Neuropharmacology.
[67] Chih-Hung Lee,et al. Effects of A‐317491, a novel and selective P2X3/P2X2/3 receptor antagonist, on neuropathic, inflammatory and chemogenic nociception following intrathecal and intraplantar administration , 2003, British journal of pharmacology.
[68] H. Pajouhesh,et al. Medicinal chemical properties of successful central nervous system drugs , 2005, NeuroRX.
[69] B. Ferrell. Acute and Chronic Pain , 2003 .
[70] D. Donnelly-roberts,et al. Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists. , 2006, Journal of medicinal chemistry.
[71] Michael F. Jarvis,et al. Interleukin-1αβ gene-deficient mice show reduced nociceptive sensitivity in models of inflammatory and neuropathic pain but not post-operative pain , 2006, Behavioural Brain Research.
[72] Jens Sadowski,et al. Properties Guiding Drug‐ and Lead‐Likeness , 2007 .
[73] D. Donnelly-roberts,et al. Discovery of P2X7 receptor‐selective antagonists offers new insights into P2X7 receptor function and indicates a role in chronic pain states , 2007, British journal of pharmacology.
[74] Geoffrey Burnstock,et al. Physiology and pathophysiology of purinergic neurotransmission. , 2007, Physiological reviews.
[75] B. Khakh,et al. P2X receptors as cell-surface ATP sensors in health and disease , 2006, Nature.
[76] Mark Furber,et al. Antagonists of the P2X7 Receptor. From Lead Identification to Drug Development , 2009 .
[77] G. V. Paolini,et al. Global mapping of pharmacological space , 2006, Nature Biotechnology.
[78] G. Burnstock,et al. Purinergic signalling in neuron–glia interactions , 2006, Nature Reviews Neuroscience.
[79] R. Evans,et al. 2′,3′‐O‐(2,4,6‐ trinitrophenyl) adenosine 5′‐triphosphate (TNP‐ATP)–a nanomolar affinity antagonist at rat mesenteric artery P2X receptor ion channels , 1998, British journal of pharmacology.
[80] M. Edwards,et al. Using the Golden Triangle to optimize clearance and oral absorption. , 2009, Bioorganic & medicinal chemistry letters.
[81] I. Goshen,et al. Impairment of interleukin-1 (IL-1) signaling reduces basal pain sensitivity in mice: genetic, pharmacological and developmental aspects , 2003, Pain.
[82] Geoffrey Burnstock,et al. Purinergic signalling , 2012, Acta physiologica.
[83] R. North. Molecular physiology of P2X receptors. , 2002, Physiological reviews.
[84] L. Rodella,et al. 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 , 2008, PAIN®.
[85] P. Séguéla,et al. Phosphoinositides Regulate P2X4 ATP-Gated Channels through Direct Interactions , 2008, The Journal of Neuroscience.
[86] C. Gravel,et al. BDNF from microglia causes the shift in neuronal anion gradient underlying neuropathic pain , 2005, Nature.
[87] R. S. Rogers,et al. Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib). , 1997, Journal of medicinal chemistry.
[88] C. Woolf. Central sensitization: Implications for the diagnosis and treatment of pain , 2011, PAIN.
[89] J. Hughes,et al. Physiochemical drug properties associated with in vivo toxicological outcomes. , 2008, Bioorganic & medicinal chemistry letters.
[90] D. Donnelly-roberts,et al. Mammalian P2X7 receptor pharmacology: comparison of recombinant mouse, rat and human P2X7 receptors , 2009, British journal of pharmacology.