John Malysz

Summary

Affiliation: Abbott Laboratories
Country: USA

Publications

  1. doi In vitro pharmacological characterization of a novel selective alpha7 neuronal nicotinic acetylcholine receptor agonist ABT-107
    John Malysz
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott, Abbott Park, Illinois 60064 6125, USA
    J Pharmacol Exp Ther 334:863-74. 2010
  2. doi Evaluation of alpha7 nicotinic acetylcholine receptor agonists and positive allosteric modulators using the parallel oocyte electrophysiology test station
    John Malysz
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott, Abbott Park, Illinois 60064 6125, USA
    Assay Drug Dev Technol 7:374-90. 2009
  3. doi In vitro pharmacological characterization of a novel allosteric modulator of alpha 7 neuronal acetylcholine receptor, 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744), exhibiting unique pharmacological profile
    John Malysz
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Rd, Abbott Park, IL 60064 6125, USA
    J Pharmacol Exp Ther 330:257-67. 2009
  4. doi Characterization of human cannabinoid CB2 receptor coupled to chimeric Galpha(qi5) and Galpha(qo5) proteins
    John Malysz
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
    Eur J Pharmacol 603:12-21. 2009
  5. ncbi Characterization of human ASIC2a homomeric channels stably expressed in murine Ltk- cells
    John Malysz
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA
    Life Sci 82:30-40. 2008
  6. ncbi Functional characterization of large conductance calcium-activated K+ channel openers in bladder and vascular smooth muscle
    John Malysz
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA
    Naunyn Schmiedebergs Arch Pharmacol 369:481-9. 2004
  7. pmc Role of channel activation in cognitive enhancement mediated by alpha7 nicotinic acetylcholine receptors
    Clark A Briggs
    Neuroscience Research, Abbott Laboratories, Abbott Park, IL, USA
    Br J Pharmacol 158:1486-94. 2009
  8. doi Importance of M2-M3 loop in governing properties of genistein at the α7 nicotinic acetylcholine receptor inferred from α7/5-HT3A chimera
    Jens Halvard Grønlien
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott, Oslo, Norway
    Eur J Pharmacol 647:37-47. 2010
  9. doi Stimulation of dopamine release by nicotinic acetylcholine receptor ligands in rat brain slices correlates with the profile of high, but not low, sensitivity alpha4beta2 subunit combination
    David J Anderson
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
    Biochem Pharmacol 78:844-51. 2009
  10. doi Alpha3* and alpha 7 nAChR-mediated Ca2+ transient generation in IMR-32 neuroblastoma cells
    Hilde Ween
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott, Oslo Research Park, Gaustadaleen 21, Oslo, Norway
    Neurochem Int 57:269-77. 2010

Collaborators

Detail Information

Publications22

  1. doi In vitro pharmacological characterization of a novel selective alpha7 neuronal nicotinic acetylcholine receptor agonist ABT-107
    John Malysz
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott, Abbott Park, Illinois 60064 6125, USA
    J Pharmacol Exp Ther 334:863-74. 2010
    ..In summary, ABT-107 is a selective high affinity alpha7 nAChR agonist suitable for characterizing the roles of this subtype in pharmacological studies...
  2. doi Evaluation of alpha7 nicotinic acetylcholine receptor agonists and positive allosteric modulators using the parallel oocyte electrophysiology test station
    John Malysz
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott, Abbott Park, Illinois 60064 6125, USA
    Assay Drug Dev Technol 7:374-90. 2009
    ....
  3. doi In vitro pharmacological characterization of a novel allosteric modulator of alpha 7 neuronal acetylcholine receptor, 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744), exhibiting unique pharmacological profile
    John Malysz
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Rd, Abbott Park, IL 60064 6125, USA
    J Pharmacol Exp Ther 330:257-67. 2009
    ..In summary, this study identifies a novel and selective alpha7 PAM showing activity at recombinant and native alpha7 nAChRs exhibiting a unique pharmacological interaction with the receptor...
  4. doi Characterization of human cannabinoid CB2 receptor coupled to chimeric Galpha(qi5) and Galpha(qo5) proteins
    John Malysz
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
    Eur J Pharmacol 603:12-21. 2009
    ....
  5. ncbi Characterization of human ASIC2a homomeric channels stably expressed in murine Ltk- cells
    John Malysz
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA
    Life Sci 82:30-40. 2008
    ....
  6. ncbi Functional characterization of large conductance calcium-activated K+ channel openers in bladder and vascular smooth muscle
    John Malysz
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA
    Naunyn Schmiedebergs Arch Pharmacol 369:481-9. 2004
    ....
  7. pmc Role of channel activation in cognitive enhancement mediated by alpha7 nicotinic acetylcholine receptors
    Clark A Briggs
    Neuroscience Research, Abbott Laboratories, Abbott Park, IL, USA
    Br J Pharmacol 158:1486-94. 2009
    ..The possibility that agonists of this receptor actually function in vivo as inhibitors via desensitization has not been finally resolved...
  8. doi Importance of M2-M3 loop in governing properties of genistein at the α7 nicotinic acetylcholine receptor inferred from α7/5-HT3A chimera
    Jens Halvard Grønlien
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott, Oslo, Norway
    Eur J Pharmacol 647:37-47. 2010
    ..The identification of distinct α7 receptor modulatory sites offers unique opportunities for developing CNS therapeutics and understanding its pharmacology...
  9. doi Stimulation of dopamine release by nicotinic acetylcholine receptor ligands in rat brain slices correlates with the profile of high, but not low, sensitivity alpha4beta2 subunit combination
    David J Anderson
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
    Biochem Pharmacol 78:844-51. 2009
    ..In summary, this study provides support for HS alpha4beta2* nAChR involvement in neurotransmitter release...
  10. doi Alpha3* and alpha 7 nAChR-mediated Ca2+ transient generation in IMR-32 neuroblastoma cells
    Hilde Ween
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott, Oslo Research Park, Gaustadaleen 21, Oslo, Norway
    Neurochem Int 57:269-77. 2010
    ..These mechanisms may, however, be still involved in other forms of nAChR-mediated Ca(2+) signaling...
  11. doi Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor
    Ramin Faghih
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, Illinois 60064, USA
    J Med Chem 52:3377-84. 2009
    ..In a rodent model of sensory gating, 19 normalized gating deficits. These results suggest that 19 represents a novel class of molecules capable of allosteric modulation of the alpha7 nAChRs...
  12. doi Functional characterization and high-throughput screening of positive allosteric modulators of α7 nicotinic acetylcholine receptors in IMR-32 neuroblastoma cells
    Sujatha M Gopalakrishnan
    Advanced Technology, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, Illinois 60064, USA
    Assay Drug Dev Technol 9:635-45. 2011
    ..This format demonstrated the feasibility of this approach for high-throughput screening to identify small molecule, PAMs, which were further confirmed in electrophysiological assays of human α7 nAChR expressed in oocytes...
  13. doi Structure-activity studies of diazabicyclo[3.3.0]octane-substituted pyrazines and pyridines as potent α4β2 nicotinic acetylcholine receptor ligands
    Marc J C Scanio
    Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL, USA
    J Med Chem 54:7678-92. 2011
    ..3.0]octane)-substituted pyridines or 2-(diazabicyclo[3.3.0]octane)-substituted pyrazines were found to have the desired binding and activity profile. The structure-activity relationship of these compounds is presented...
  14. doi Syntheses and structure-activity relationship (SAR) studies of 2,5-diazabicyclo[2.2.1]heptanes as novel alpha7 neuronal nicotinic receptor (NNR) ligands
    Tao Li
    Neuroscience Research, GPRD, Abbott, Abbott Park, IL 60064 6117, USA
    Bioorg Med Chem Lett 20:3636-9. 2010
    ..SAR studies established that 5-N-methyl substituent, heteroaryl linker and the nature of terminal aryl group are critical for the ligand to achieve potent alpha7 NNR agonist activity...
  15. doi Role of α7 nicotinic acetylcholine receptors in regulating tumor necrosis factor-α (TNF-α) as revealed by subtype selective agonists
    Jinhe Li
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, United States
    J Neuroimmunol 239:37-43. 2011
    ..These studies collectively demonstrate that selectively targeting α7 nAChRs could offer a novel therapeutic modality to treat acute and chronic inflammatory disease states...
  16. doi Preclinical characterization of A-582941: a novel alpha7 neuronal nicotinic receptor agonist with broad spectrum cognition-enhancing properties
    Karin R Tietje
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, Illinois 60064, USA
    CNS Neurosci Ther 14:65-82. 2008
    ....
  17. ncbi Broad-spectrum efficacy across cognitive domains by alpha7 nicotinic acetylcholine receptor agonism correlates with activation of ERK1/2 and CREB phosphorylation pathways
    Robert S Bitner
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, Illinois 60064, USA
    J Neurosci 27:10578-87. 2007
    ....
  18. doi α4β2 neuronal nicotinic receptor positive allosteric modulation: an approach for improving the therapeutic index of α4β2 nAChR agonists in pain
    Chih Hung Lee
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064 3500, USA
    Biochem Pharmacol 82:959-66. 2011
    ..Cardiovascular studies in anesthetized dogs achieve supra-therapeutic plasma concentrations of ABT-594 (>20-fold) without hemodynamic or electrophysiological effects using the co-administration paradigm...
  19. ncbi [125I]A-312110, a novel high-affinity 1,4-dihydropyridine ATP-sensitive K+ channel opener: characterization and pharmacology of binding
    Rachel Davis-Taber
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, Illinois, USA
    Mol Pharmacol 64:143-53. 2003
    ....
  20. ncbi Distinct profiles of alpha7 nAChR positive allosteric modulation revealed by structurally diverse chemotypes
    Jens Halvard Grønlien
    Oslo Research Park, Oslo, Norway
    Mol Pharmacol 72:715-24. 2007
    ..In summary, our studies reveal two distinct alpha7 PAM profiles, which could offer unique opportunities for modulating alpha7 nAChRs in vivo and in the development of novel therapeutics for central nervous system indications...
  21. ncbi An allosteric modulator of the alpha7 nicotinic acetylcholine receptor possessing cognition-enhancing properties in vivo
    Daniel B Timmermann
    Neurosearch A S, Ballerup, Denmark
    J Pharmacol Exp Ther 323:294-307. 2007
    ..These data support the notion that alpha7 nAChR allosteric modulation may constitute a novel pharmacological principle for the treatment of cognitive dysfunction...
  22. ncbi The Kv2.2 alpha subunit contributes to delayed rectifier K(+) currents in myocytes from rabbit corpus cavernosum
    John Malysz
    Department of Physiology, Mayo Clinic, Rochester, Minnesota 55905, USA
    J Androl 23:899-910. 2002
    ..We conclude that Kv2.2 alpha subunits contribute to whole-cell currents in rabbit canvernosal myocytes. Further, K(v) currents play a role in regulating membrane potential and hence excitability in rabbit cavernosal myocytes...