Browsing Discipline of Pharmacology by publication year
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Glutamate transporter dysfunction associated with nerve injury-induced pain in mice
Published 2012-01-01Dysfunction at glutamatergic synapses has been proposed as a mechanism in the development of neuropathic pain. Here we sought to determine whether peripheral nerve injury-induced neuropathic pain results in functional ...Article -
PP2A phosphatase suppresses function of the mesenchymal invasion regulator NEDD9
Published 2012-02-01The mesenchymal mode of cancer cell invasion characterized by active adhesion turnover and a polarized actin cytoskeleton, is critically regulated by the adaptor protein NEDD9/HEF1/Cas-L. While it is known that NEDD9 is ...Article -
Mechanisms of rapid opioid receptor desensitization, resensitization and tolerance in brain neurons
Published 2012-03-01Agonists acting on µ-opioid receptors (MOR) are very effective analgesics but cause tolerance during long-term or repeated exposure. Intensive efforts have been made to find novel opioid agonists that are efficacious ...Article -
Opioid-related (ORL1) receptors are enriched in a subpopulation of sensory neurons and prolonged activation produces no functional loss of surface N-type calcium channels.
Published 2012-03-29The opioid-related receptor, ORL1, is activated by the neuropeptide nociceptin/orphanin FQ (N/OFQ) and inhibits high-voltage-activated (HVA) calcium channel currents (I(Ca)) via a G-protein-coupled mechanism. Endocytosis ...Article -
Multiple mechanisms of microglia: A gatekeeper's contribution to pain states
Published 2012-04-01Microglia are gatekeepers in the CNS for a wide range of pathological stimuli and they blow the whistle when things go wrong. Collectively, microglia form a CNS tissue alarm system (Kreutzberg's “sensor of pathology”), and ...Article -
NEDD9 Stabilizes Focal Adhesions, Increases Binding to the Extra-Cellular Matrix and Differentially Effects 2D versus 3D Cell Migration
Published 2012-04-11The speed of cell migration on 2-dimensional (2D) surfaces is determined by the rate of assembly and disassembly of clustered integrin receptors known as focal adhesions. Different modes of cell migration that have been ...Article -
Nucleus accumbens D2- and D1-receptor expressing medium spiny neurons are selectively activated by morphine withdrawal and acute morphine, respectively.
Published 2012-06-01Opioids are effective analgesic agents but serious adverse effects such as tolerance and withdrawal contribute to opioid dependence and limit their use. Opioid withdrawal involves numerous brain regions and includes ...Article -
Intrathecal α-conotoxins Vc1.1, AuIB and MII acting on distinct nicotinic receptor subtypes reverse signs of neuropathic pain
Published 2012-06-01The large diversity of peptides from venomous creatures with high affinity for molecules involved in the development and maintenance of neuropathic pain has led to a surge in venom-derived analgesic research. Some members ...Article -
Characterisation of Nav types endogenously expressed in human SH-SY5Y neuroblastoma cells
Published 2012-06-01The human neuroblastoma cell line SH-SY5Y is a potentially useful model for the identification and characterisation of Na(v) modulators, but little is known about the pharmacology of their endogenously expressed Na(v)s. ...Article -
Occupy tissue: the movement in cancer metastasis
Published 2012-09-01The critical role of migration and invasion in cancer metastasis warrants new therapeutic approaches targeting the machinery regulating cell migration and invasion. While 2-dimensional (2D) models have helped identify a ...Article -
Osteoblasts mediate the adverse effects of glucocorticoids on fuel metabolism
Published 2012-10-24Long-term glucocorticoid treatment is associated with numerous adverse outcomes, including weight gain, insulin resistance, and diabetes; however, the pathogenesis of these side effects remains obscure. Glucocorticoids ...Article -
A Continuous, Fluorescence-based Assay of µ-Opioid Receptor Activation in AtT-20 Cells
Published 2013-03-01Opioids are widely prescribed analgesics, but their use is limited due to development of tolerance and addiction, as well as high variability in individual response. The development of improved opioid analgesics requires ...Article -
Tyrosine Y189 in the Substrate Domain of the Adhesion Docking Protein NEDD9 Is Conserved with p130Cas Y253 and Regulates NEDD9-Mediated Migration and Focal Adhesion Dynamics
Published 2013-07-09The focal adhesion docking protein NEDD9/HEF1/Cas-L regulates cell migration and cancer invasion. NEDD9 is a member of the Cas family of proteins that share conserved overall protein-protein interaction domain structure, ...Article -
Human chorionic gonadotropin increases β-cleavage of amyloid precursor protein in SH-SY5Y cells
Published 2013-08-01Elevated levels of amyloid-β (Aβ) peptides, the main component of amyloid plaques in Alzheimer's disease, are the result of excessive β- and γ-cleavage of the amyloid precursor protein (APP) and/or impaired Aβ clearance ...Article -
Functional Analysis of Novel Polymorphisms in the Human SLCO1A2 Gene that Encodes the Transporter OATP1A2
Published 2013-08-06The solute carrier organic anion transporting polypeptide 1A2 (OATP1A2, SLCO1A2) is implicated in the cellular influx of a number of drugs. We identified five novel single nucleotide polymorphisms (SNPs) in coding exons ...Article -
Spinal actions of ω-conotoxins, CVID, MVIIA and related peptides in a rat neuropathic pain model
Published 2013-09-01"BACKGROUND AND PURPOSE: Antagonists of the N-type voltage gated calcium channel (VGCC), Cav 2.2, have a potentially important role in the treatment of chronic neuropathic pain. ω-conotoxins, such MVIIA and CVID are effective ...Article -
Vicinal Disulfide Constrained Cyclic Peptidomimetics: a Turn Mimetic Scaffold Targeting the Norepinephrine Transporter
Published 2013-09-24Loopy peptides: Peptide turn mimetics of a clinically relevant norepinephrine reuptake inhibitor were developed employing a high-throughput synthesis approach to generate peptide thioesters, with subsequent cyclization ...Article -
NEDD9 regulates 3D migratory activity independent of the Rac1 morphology switch in glioma and neuroblastoma.
Published 2014-02-01Metastasizing tumor cells must transmigrate the dense extracellular matrix that surrounds most organs. The use of three-dimensional (3D) collagen gels has revealed that many cancer cells can switch between different modes ...Article -
Use of a glyphosate-based herbicide-induced nephrotoxicity model to investigate a panel of kidney injury biomarkers
Published 2014-02-10Accidental or intentional ingestion of glyphosate surfactant-based herbicides, like Roundup, leads to nephrotoxicity as well as death. In this study, a panel of kidney injury biomarkers was evaluated in terms of suitability ...Article -
Kidney biomarkers in MCPA-induced acute kidney injury in rats: reduced clearance enhances early biomarker performance
Published 2014-03-21For improved early detection and assessment of severe acute kidney damage following accidental or intentional ingestion of the herbicide MCPA, we compared a panel of 14 novel kidney injury biomarkers with plasma creatinine. ...Article