Tomas de Paulis

Summary

Affiliation: Vanderbilt University
Country: USA

Publications

  1. ncbi request reprint Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes
    Tomas de Paulis
    Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, Tennessee 37232, USA
    J Med Chem 49:3332-44. 2006
  2. ncbi request reprint The discovery of epidepride and its analogs as high-affinity radioligands for imaging extrastriatal dopamine D(2) receptors in human brain
    Tomas de Paulis
    Departments of Psychiatry and Radiology, Vanderbilt University School of Medicine, Nashville TN 37232, USA
    Curr Pharm Des 9:673-96. 2003
  3. ncbi request reprint Sumanirole Pharmacia
    Tomas de Paulis
    Psychiatry Department, MCN AA 2213, Vanderbilt University School of Medicine, Nashville, TN 37232, USA
    Curr Opin Investig Drugs 4:77-82. 2003
  4. ncbi request reprint ONO-2506. Ono
    Tomas de Paulis
    Psychiatry Department, MCN AA 2213, Vanderbilt University School of Medicine, Nashville, TN 37232, USA
    Curr Opin Investig Drugs 4:863-7. 2003
  5. ncbi request reprint 4-Caffeoyl-1,5-quinide in roasted coffee inhibits [3H]naloxone binding and reverses anti-nociceptive effects of morphine in mice
    Tomas de Paulis
    Department of Psychiatry, Vanderbilt Institute for Coffee Studies, Vanderbilt University School of Medicine, MCN AA 2213, Nashville, TN 37232, USA
    Psychopharmacology (Berl) 176:146-53. 2004
  6. ncbi request reprint A novel class of positive allosteric modulators of metabotropic glutamate receptor subtype 1 interact with a site distinct from that of negative allosteric modulators
    Kamondanai Hemstapat
    Department of Pharmacology, Vanderbilt University Medical Center, 23rd Ave South at Pierce, 417 D Preston Research Bldg, Nashville, TN 37232 6600, USA
    Mol Pharmacol 70:616-26. 2006
  7. ncbi request reprint Interaction of novel positive allosteric modulators of metabotropic glutamate receptor 5 with the negative allosteric antagonist site is required for potentiation of receptor responses
    Yelin Chen
    Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232 6600, USA
    Mol Pharmacol 71:1389-98. 2007
  8. ncbi request reprint Dicinnamoylquinides in roasted coffee inhibit the human adenosine transporter
    Tomas de Paulis
    Institute for Coffee Studies, Department of Psychiatry, Vanderbilt University School of Medicine, Nashville, TN 37232, USA
    Eur J Pharmacol 442:215-23. 2002
  9. ncbi request reprint Chlorogenic acids and lactones in regular and water-decaffeinated arabica coffees
    Adriana Farah
    Vanderbilt Institute for Coffee Studies, Division of Addiction Medicine, Department of Psychiatry, Vanderbilt University School of Medicine, Nashville, Tennessee 37232, USA
    J Agric Food Chem 54:374-81. 2006
  10. ncbi request reprint Biphenyl-indanone A, a positive allosteric modulator of the metabotropic glutamate receptor subtype 2, has antipsychotic- and anxiolytic-like effects in mice
    Ruggero Galici
    Program in Translational Neuropharmacology, Department of Pharmacology, Vanderbilt University Medical Center, 23rd Ave S at Pierce, 417 D Preston Research Building, Nashville, TN 37232 6600, USA
    J Pharmacol Exp Ther 318:173-85. 2006

Detail Information

Publications18

  1. ncbi request reprint Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes
    Tomas de Paulis
    Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, Tennessee 37232, USA
    J Med Chem 49:3332-44. 2006
    ..6 +/- 1.9 nM in the binding and functional assays, respectively...
  2. ncbi request reprint The discovery of epidepride and its analogs as high-affinity radioligands for imaging extrastriatal dopamine D(2) receptors in human brain
    Tomas de Paulis
    Departments of Psychiatry and Radiology, Vanderbilt University School of Medicine, Nashville TN 37232, USA
    Curr Pharm Des 9:673-96. 2003
    ..4))), estimates of maximal binding potential of any radioligand for imaging of any neurotransmitter receptor or transporter site seem possible...
  3. ncbi request reprint Sumanirole Pharmacia
    Tomas de Paulis
    Psychiatry Department, MCN AA 2213, Vanderbilt University School of Medicine, Nashville, TN 37232, USA
    Curr Opin Investig Drugs 4:77-82. 2003
    ..The compound is currently undergoing phase II trials in Japan and phase III clinical trials in the US...
  4. ncbi request reprint ONO-2506. Ono
    Tomas de Paulis
    Psychiatry Department, MCN AA 2213, Vanderbilt University School of Medicine, Nashville, TN 37232, USA
    Curr Opin Investig Drugs 4:863-7. 2003
    ..Japanese and European phase I trials for AD, PD and amyotropic lateral sclerosis (ALS) had commenced by March 2002 and phase II trials for ALS are underway in Europe...
  5. ncbi request reprint 4-Caffeoyl-1,5-quinide in roasted coffee inhibits [3H]naloxone binding and reverses anti-nociceptive effects of morphine in mice
    Tomas de Paulis
    Department of Psychiatry, Vanderbilt Institute for Coffee Studies, Vanderbilt University School of Medicine, MCN AA 2213, Nashville, TN 37232, USA
    Psychopharmacology (Berl) 176:146-53. 2004
    ..Instant coffee has been shown to displace binding of the mu opioid receptor antagonist, [3H]naloxone, but the putative active agent, feruloylquinide, has not been characterized...
  6. ncbi request reprint A novel class of positive allosteric modulators of metabotropic glutamate receptor subtype 1 interact with a site distinct from that of negative allosteric modulators
    Kamondanai Hemstapat
    Department of Pharmacology, Vanderbilt University Medical Center, 23rd Ave South at Pierce, 417 D Preston Research Bldg, Nashville, TN 37232 6600, USA
    Mol Pharmacol 70:616-26. 2006
    ..Site-directed mutagenesis revealed that valine at position 757 in transmembrane V of mGluR1a is crucial for the activity of multiple classes of allosteric mGluR1 potentiators...
  7. ncbi request reprint Interaction of novel positive allosteric modulators of metabotropic glutamate receptor 5 with the negative allosteric antagonist site is required for potentiation of receptor responses
    Yelin Chen
    Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232 6600, USA
    Mol Pharmacol 71:1389-98. 2007
    ....
  8. ncbi request reprint Dicinnamoylquinides in roasted coffee inhibit the human adenosine transporter
    Tomas de Paulis
    Institute for Coffee Studies, Department of Psychiatry, Vanderbilt University School of Medicine, Nashville, TN 37232, USA
    Eur J Pharmacol 442:215-23. 2002
    ..This suggests that 3,4-dicinnamoyl-1,5-quinides in coffee could have the potential to raise extra-cellular adenosine levels, thereby counteracting the stimulant effect of caffeine...
  9. ncbi request reprint Chlorogenic acids and lactones in regular and water-decaffeinated arabica coffees
    Adriana Farah
    Vanderbilt Institute for Coffee Studies, Division of Addiction Medicine, Department of Psychiatry, Vanderbilt University School of Medicine, Nashville, Tennessee 37232, USA
    J Agric Food Chem 54:374-81. 2006
    ....
  10. ncbi request reprint Biphenyl-indanone A, a positive allosteric modulator of the metabotropic glutamate receptor subtype 2, has antipsychotic- and anxiolytic-like effects in mice
    Ruggero Galici
    Program in Translational Neuropharmacology, Department of Pharmacology, Vanderbilt University Medical Center, 23rd Ave S at Pierce, 417 D Preston Research Building, Nashville, TN 37232 6600, USA
    J Pharmacol Exp Ther 318:173-85. 2006
    ....
  11. pmc Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4
    Colleen M Niswender
    Department of Pharmacology, Vanderbilt University, Nashville, TN 37232, USA
    Mol Pharmacol 74:1345-58. 2008
    ..These exciting results provide continued support for mGluR4 as a therapeutic target in PD...
  12. ncbi request reprint Quinides of roasted coffee enhance insulin action in conscious rats
    Jane Shearer
    Department of Molecular Physiology and Biophysics, Vanderbilt University, Nashville, TN, USA
    J Nutr 133:3529-32. 2003
    ..These results demonstrate that DIFEQ increases whole-body glucose disposal independently of skeletal muscle Rg...
  13. ncbi request reprint Discrimination in 5-HT(3) receptor binding in murine brain and cultured cell preparations
    Zhang Jin Zhang
    Department of Psychiatry, Vanderbilt University Medical Center, Nashville, TN 37232, USA
    Naunyn Schmiedebergs Arch Pharmacol 365:123-32. 2002
    ....
  14. ncbi request reprint Effect of roasting on the formation of chlorogenic acid lactones in coffee
    Adriana Farah
    Vanderbilt Institute for Coffee Studies, Vanderbilt University School of Medicine, Nashville, Tennessee 37232, USA
    J Agric Food Chem 53:1505-13. 2005
    ..This suggests that roasting causes isomerization of chlorogenic acids prior to the formation of lactones and that the levels of lactones in roasted coffee do not reflect the levels of precursors in green coffee...
  15. ncbi request reprint Perospirone (Sumitomo Pharmaceuticals)
    Tomas de Paulis
    Psychiatry Department, Vanderbilt University School of Medicine, Nashville, TN 37232, USA
    Curr Opin Investig Drugs 3:121-9. 2002
    ..In February 2001, Sumitomo predicted that perospirone would reach sales of yen10 billion within five to six years [399401]...
  16. ncbi request reprint Drug evaluation: Lymphoseek - Neoprobe's sentinel lymph node imaging agent for use in cancer patients
    Tomas de Paulis
    Curr Opin Investig Drugs 7:1100-7. 2006
    ..Phase II trials of Lymphoseek were initiated in mid 2006...
  17. ncbi request reprint Drug evaluation: PRX-00023, a selective 5-HT1A receptor agonist for depression
    Tomas de Paulis
    Curr Opin Investig Drugs 8:78-86. 2007
    ..In November 2006, EPIX reported that it planned to initiate a phase II trial in patients with depression in the first half of 2007...
  18. ncbi request reprint Drug evaluation: Vilazodone--a combined SSRI and 5-HT1A partial agonist for the treatment of depression
    Tomas de Paulis
    IDrugs 10:193-201. 2007
    ....