R D Blakely

Summary

Affiliation: Vanderbilt University
Country: USA

Publications

  1. ncbi Physiological genomics of antidepressant targets: keeping the periphery in mind
    R D Blakely
    Department of Pharmacology, Center for Molecular Neuroscience, Vanderbilt University School of Medicine, Nashville, Tennessee 37232 6420, USA
    J Neurosci 21:8319-23. 2001
  2. ncbi Biogenic amine transporters: regulation in flux
    R D Blakely
    Department of Pharmacology, Center for Molecular Neuroscience, Vanderbilt University School of Medicine, Nashville, 37232 6420, USA
    Curr Opin Neurobiol 10:328-36. 2000
  3. ncbi Cocaine and antidepressant-sensitive biogenic amine transporters exist in regulated complexes with protein phosphatase 2A
    A L Bauman
    Department of Pharmacology and Center for Molecular Neuroscience, Vanderbilt University School of Medicine, Nashville, Tennessee 37232 6420, USA
    J Neurosci 20:7571-8. 2000
  4. ncbi Protein kinase C activation regulates human serotonin transporters in HEK-293 cells via altered cell surface expression
    Y Qian
    Department of Pharmacology and Center for Molecular Neuroscience, Vanderbilt School of Medicine, Nashville, Tennessee 37232 6600, USA
    J Neurosci 17:45-57. 1997
  5. ncbi Multivariate permutation analysis associates multiple polymorphisms with subphenotypes of major depression
    M K Hahn
    Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, TN 37232, USA
    Genes Brain Behav 7:487-95. 2008
  6. ncbi The Caenorhabditis elegans gene T23G5.5 encodes an antidepressant- and cocaine-sensitive dopamine transporter
    L D Jayanthi
    Department of Pharmacology, Nashville TN 37232 6600 and Fort Dodge Animal Health, Princeton, New Jersey 08543 0400, USA
    Mol Pharmacol 54:601-9. 1998
  7. ncbi Interactions of tryptamine derivatives with serotonin transporter species variants implicate transmembrane domain I in substrate recognition
    E M Adkins
    Department of Pharmacology and Center for Molecular Neuroscience, Vanderbilt University Medical Center, Nashville, Tennessee, USA
    Mol Pharmacol 59:514-23. 2001
  8. ncbi High affinity recognition of serotonin transporter antagonists defined by species-scanning mutagenesis. An aromatic residue in transmembrane domain I dictates species-selective recognition of citalopram and mazindol
    E L Barker
    Department of Pharmacology and Center for Molecular Neuroscience, Vanderbilt University School of Medicine, Nashville, Tennessee 37232 6600, USA
    J Biol Chem 273:19459-68. 1998
  9. ncbi Molecular cloning of a human, hemicholinium-3-sensitive choline transporter
    S Apparsundaram
    Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, Tennessee, 37232 3420, USA
    Biochem Biophys Res Commun 276:862-7. 2000
  10. ncbi Molecular cloning and characterization of a murine hemicholinium-3-sensitive choline transporter
    S Apparsundaram
    Department of Pharmacology, Vanderbilt University Medical School, Nashville, TN 37232 6600, USA
    Biochem Soc Trans 29:711-6. 2001

Detail Information

Publications87

  1. ncbi Physiological genomics of antidepressant targets: keeping the periphery in mind
    R D Blakely
    Department of Pharmacology, Center for Molecular Neuroscience, Vanderbilt University School of Medicine, Nashville, Tennessee 37232 6420, USA
    J Neurosci 21:8319-23. 2001
    ....
  2. ncbi Biogenic amine transporters: regulation in flux
    R D Blakely
    Department of Pharmacology, Center for Molecular Neuroscience, Vanderbilt University School of Medicine, Nashville, 37232 6420, USA
    Curr Opin Neurobiol 10:328-36. 2000
    ..The theory that dysregulation of transporters may contribute to disease states is supported by the recent discovery that a coding mutation in the human norepinephrine transporter contributes to orthostatic intolerance...
  3. ncbi Cocaine and antidepressant-sensitive biogenic amine transporters exist in regulated complexes with protein phosphatase 2A
    A L Bauman
    Department of Pharmacology and Center for Molecular Neuroscience, Vanderbilt University School of Medicine, Nashville, Tennessee 37232 6420, USA
    J Neurosci 20:7571-8. 2000
    ....
  4. ncbi Protein kinase C activation regulates human serotonin transporters in HEK-293 cells via altered cell surface expression
    Y Qian
    Department of Pharmacology and Center for Molecular Neuroscience, Vanderbilt School of Medicine, Nashville, Tennessee 37232 6600, USA
    J Neurosci 17:45-57. 1997
    ..These data indicate that altered surface abundance, rather than reduced catalytic transport efficiency, mediates acute PKC-dependent modulation of 5-HT uptake...
  5. ncbi Multivariate permutation analysis associates multiple polymorphisms with subphenotypes of major depression
    M K Hahn
    Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, TN 37232, USA
    Genes Brain Behav 7:487-95. 2008
    ..74 (1.05-7.18)]}. These relationships illustrate an approach to the elucidation of gene influences on trait components of MDD and with replication, may help identify MDD subpopulations that can benefit from more targeted pharmacotherapy...
  6. ncbi The Caenorhabditis elegans gene T23G5.5 encodes an antidepressant- and cocaine-sensitive dopamine transporter
    L D Jayanthi
    Department of Pharmacology, Nashville TN 37232 6600 and Fort Dodge Animal Health, Princeton, New Jersey 08543 0400, USA
    Mol Pharmacol 54:601-9. 1998
    ..elegans cDNA in vivo...
  7. ncbi Interactions of tryptamine derivatives with serotonin transporter species variants implicate transmembrane domain I in substrate recognition
    E M Adkins
    Department of Pharmacology and Center for Molecular Neuroscience, Vanderbilt University Medical Center, Nashville, Tennessee, USA
    Mol Pharmacol 59:514-23. 2001
    ..These findings support a critical role for TMD I residues in defining shared aspects of SERT substrate and antagonist recognition...
  8. ncbi High affinity recognition of serotonin transporter antagonists defined by species-scanning mutagenesis. An aromatic residue in transmembrane domain I dictates species-selective recognition of citalopram and mazindol
    E L Barker
    Department of Pharmacology and Center for Molecular Neuroscience, Vanderbilt University School of Medicine, Nashville, Tennessee 37232 6600, USA
    J Biol Chem 273:19459-68. 1998
    ....
  9. ncbi Molecular cloning of a human, hemicholinium-3-sensitive choline transporter
    S Apparsundaram
    Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, Tennessee, 37232 3420, USA
    Biochem Biophys Res Commun 276:862-7. 2000
    ..These studies elucidate the primary structure and chromosomal localization of hCHT and provide a basis for mechanistic analysis of HACU regulation and an investigation of the role of hCHT in disease states...
  10. ncbi Molecular cloning and characterization of a murine hemicholinium-3-sensitive choline transporter
    S Apparsundaram
    Department of Pharmacology, Vanderbilt University Medical School, Nashville, TN 37232 6600, USA
    Biochem Soc Trans 29:711-6. 2001
    ..The availability of cloned, functional mCHT and its cognate genomic DNA should prove useful for studies of mCHT regulation and should open possibilities for evaluation of CHT dysfunction in murine models...
  11. ncbi Motor neuron-specific overexpression of the presynaptic choline transporter: impact on motor endurance and evoked muscle activity
    D Lund
    Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, TN 37232 8548, USA
    Neuroscience 171:1041-53. 2010
    ..To explain our findings, we propose a model whereby CHT support for neuromuscular signaling involves contributions to ACh synthesis as well as cholinergic synaptic vesicle availability...
  12. ncbi Deficits in acetylcholine homeostasis, receptors and behaviors in choline transporter heterozygous mice
    M H Bazalakova
    Neuroscience Graduate Program, MSTP, Vanderbilt University School of Medicine, Vanderbilt University, Nashville, TN 37242 8548, USA
    Genes Brain Behav 6:411-24. 2007
    ..Our studies suggest that CHT hemizygosity results in adequate baseline ACh stores, sufficient to sustain many phenotypes, but normal sensitivities to physical and/or pharmacological challenge require full cholinergic signaling capacity...
  13. ncbi Cholinergic neurons of mouse intrinsic cardiac ganglia contain noradrenergic enzymes, norepinephrine transporters, and the neurotrophin receptors tropomyosin-related kinase A and p75
    J L Hoard
    Department of Pharmacology, James H Quillen College of Medicine, East Tennessee State University, Johnson City, TN 37614, USA
    Neuroscience 156:129-42. 2008
    ..They also suggest that neurotrophins and local NE synthesis might have important effects on neurons of the mouse ICG...
  14. ncbi Novel fluorescence-based approaches for the study of biogenic amine transporter localization, activity, and regulation
    J N Mason
    Department of Pharmacology, Vanderbilt University School of Medicine, MRBII, Suite 7140, 465 21st Ave South, Nashville, TN 37232-8548, USA
    J Neurosci Methods 143:3-25. 2005
    ..Together, these approaches offer novel opportunities to investigate changes in transporter function and distribution in real-time with superior spatial and temporal resolution...
  15. ncbi Trafficking-dependent and -independent pathways of neurotransmitter transporter regulation differentially involving p38 mitogen-activated protein kinase revealed in studies of insulin modulation of norepinephrine transport in SK-N-SH cells
    S Apparsundaram
    Department of Pharmacology and Center for Molecular Neuroscience, Vanderbilt University School of Medicine, Nashville, Tennessee 37232-6600, USA
    J Pharmacol Exp Ther 299:666-77. 2001
    ..Our findings establish two distinct pathways for regulation of NE uptake involving PI3K, one linked to transporter trafficking and a second linked to Ca2+-dependent, p38 MAPK phosphorylation that promotes activation of cell surface NETs...
  16. ncbi Linkage and association analysis at the serotonin transporter (SLC6A4) locus in a rigid-compulsive subset of autism
    J L McCauley
    Program in Human Genetics, Department of Molecular Physiology and Biophysics, Vanderbilt University, Nashville, Tennessee 37232-0615, USA
    Am J Med Genet B Neuropsychiatr Genet 127:104-12. 2004
    ..In fact, such variants may well account for linkage to 17q11.2 in our families...
  17. ncbi Acute regulation of norepinephrine transport: II. PKC-modulated surface expression of human norepinephrine transporter proteins
    S Apparsundaram
    Department of Pharmacology and Center for Molecular Neuroscience, Vanderbilt University School of Medicine, Nashville, Tennessee, USA
    J Pharmacol Exp Ther 287:744-51. 1998
    ..Together these findings argue for kinase-modulated protein trafficking as a potential route for acute regulation of antidepressant-sensitive NE clearance...
  18. ncbi Familial orthostatic tachycardia due to norepinephrine transporter deficiency
    D Robertson
    Autonomic Dysfunction Center, AA3228 MCN, Vanderbilt University, Nashville, TN 37232 2195, USA
    Ann N Y Acad Sci 940:527-43. 2001
    ..Identification of this mechanism may facilitate our understanding of genetic causes of OI and lead to the development of more effective therapeutic modalities...
  19. ncbi Monoamine transporter gene structure and polymorphisms in relation to psychiatric and other complex disorders
    M K Hahn
    Department of Pharmacology and Center for Molecular Neuroscience, Vanderbilt University, Nashville, TN 37232 6420, USA
    Pharmacogenomics J 2:217-35. 2002
    ....
  20. ncbi Drosophila serotonin transporters have voltage-dependent uptake coupled to a serotonin-gated ion channel
    A Galli
    Center for Molecular Neuroscience, Department of Pharmacology, Vanderbilt University Medical Center, Nashville, Tennessee 37232 6600, USA
    J Neurosci 17:3401-11. 1997
    ..These data support a model in which 500 SERT cycles occur for each 5HT-induced channel opening or a model in which 500 5HT molecules and 10,000 electronic charges pass through a common pore...
  21. ncbi Natural and engineered coding variation in antidepressant-sensitive serotonin transporters
    R Ye
    Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, TN 37232 8548, USA
    Neuroscience 197:28-36. 2011
    ..Each of these activities has driven the development of new model systems that can be further exploited to understand the contribution of 5-HT signaling to risk for neuropsychiatric disorders and their treatment...
  22. ncbi Psychiatric profile and attention deficits in postural tachycardia syndrome
    V Raj
    Department of Psychiatry, Vanderbilt University School of Medicine, 1500 21st Ave, South, Nashville, TN 37212, USA
    J Neurol Neurosurg Psychiatry 80:339-44. 2009
    ..Patients with POTS were formally assessed for psychiatric disorders and inattention and compared with patients with attention deficit hyperactivity disorder (ADHD) and control subjects...
  23. ncbi A novel nonopioid action of enkephalins: competitive inhibition of the mammalian brain high affinity L-proline transporter
    R T Fremeau
    Department of Pharmacology, Duke University Medical Center, Durham, North Carolina 27710, USA
    Mol Pharmacol 49:1033-41. 1996
    ..The high potency and specificity of des-tyrosyl-Leu-enkephalin make this compound a useful tool for elucidating the structure-function properties and physiological role(s) of PROT...
  24. ncbi Cloning and chromosomal mapping of the murine norepinephrine transporter
    J D Fritz
    Department of Pharmacology and Center for Molecular Neuroscience, Vanderbilt University Medical Center, Nashville, Tennessee 37232 6600, USA
    J Neurochem 70:2241-51. 1998
    ..The status of Slc6a5 as a candidate gene for alcohol sensitivity is discussed with respect to studies noting ethanol-induced alterations in brain NE receptors, NE receptor-linked adenylate cyclase, and NE transport...
  25. ncbi Norepinephrine transporter-deficient mice respond to anxiety producing and fearful environments with bradycardia and hypotension
    N R Keller
    Autonomic Dysfunction Center, Division of Clinical Pharmacology, Department of Medicine, Vanderbilt University Medical Center, AA3228 MCN, Nashville, TN 37232 2195, USA
    Neuroscience 139:931-46. 2006
    ....
  26. ncbi The Caenorhabditis elegans choline transporter CHO-1 sustains acetylcholine synthesis and motor function in an activity-dependent manner
    Dawn Signor Matthies
    Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, Tennessee 37232 8548, USA
    J Neurosci 26:6200-12. 2006
    ..Our findings establish a requirement for presynaptic choline transport activity in vivo in a model amenable to a genetic dissection of CHO-1 regulation...
  27. ncbi Tyr-95 and Ile-172 in transmembrane segments 1 and 3 of human serotonin transporters interact to establish high affinity recognition of antidepressants
    L Keith Henry
    Department of Pharmacology and Center for Molecular Neuroscience, Vanderbilt University Medical Center, Nashville, TN 37232, USA
    J Biol Chem 281:2012-23. 2006
    ..These studies provided evidence for distinct binding sites coordinating SERT antagonists and revealed a close interaction between TM1 and TM3 differentially targeted by stereoisomers of CIT...
  28. ncbi Inhibitors of the serotonin transporter protein (SERT): the design and synthesis of biotinylated derivatives of 3-(1,2,3,6-tetrahydro-pyridin-4-yl)-1H-indoles. High-affinity serotonergic ligands for conjugation with quantum dots
    Ian D Tomlinson
    The Department of Chemistry, Vanderbilt University, Station B, 351822, Nashville, TN 37235-1822, USA
    Bioorg Med Chem Lett 15:5307-10. 2005
    ..This letter describes the design and synthesis of two different biotinylated SERT antagonists that can be attached to streptavidin-coated cadmium selenide/zinc sulfide core shell nanocrystals...
  29. ncbi Sequence variation in the human dopamine transporter gene in children with attention deficit hyperactivity disorder
    Michelle S Mazei-Robison
    Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232 8548, USA
    Neuropharmacology 49:724-36. 2005
    ..Interestingly, the A559V variant was previously identified in a subject with bipolar disorder [. Molecular Psychiatry 5, 275], a psychiatric disorder that has a significant number of overlapping symptoms with ADHD...
  30. ncbi Biogenic amine neurotransmitter transporters: just when you thought you knew them
    Randy D Blakely
    Department of Pharmacology, Molecular Physiology and Biophysics, Vanderbilt School of Medicine, Nashville, TN, USA
    Physiology (Bethesda) 20:225-31. 2005
    ....
  31. ncbi Allelic heterogeneity at the serotonin transporter locus (SLC6A4) confers susceptibility to autism and rigid-compulsive behaviors
    James S Sutcliffe
    Center for Molecular Neuroscience, Department of Molecular Physiology and Biophysics, Vanderbilt University, Nashville, TN 37232 0615, USA
    Am J Hum Genet 77:265-79. 2005
    ..In the aggregate, these variants show significant linkage to and association with autism. Our data provide strong support for a collection of multiple, often rare, alleles at SLC6A4 as imposing risk of autism...
  32. ncbi A genetic screen in Caenorhabditis elegans for dopamine neuron insensitivity to 6-hydroxydopamine identifies dopamine transporter mutants impacting transporter biosynthesis and trafficking
    Richard Nass
    Department of Anesthesiology, Vanderbilt School of Medicine, Nashville, Tennessee 37232-8548, USA
    J Neurochem 94:774-85. 2005
    ....
  33. ncbi High affinity inhibitors of the dopamine transporter (DAT): novel biotinylated ligands for conjugation to quantum dots
    Ian D Tomlinson
    The Department of Chemistry, Vanderbilt University, Nashville, TN 37235 1822, USA
    Bioorg Med Chem Lett 16:4664-7. 2006
    ..This letter describes the synthesis of biotinylated analogs of the DAT antagonists GBR 12909 and GBR 12935 that can be attached to streptavidin coated cadmium selenide/zinc sulfide/core shell nanocrystals...
  34. ncbi Na+, Cl-, and pH dependence of the human choline transporter (hCHT) in Xenopus oocytes: the proton inactivation hypothesis of hCHT in synaptic vesicles
    Hideki Iwamoto
    Department of Pharmacology and Center for Molecular Neuroscience, Vanderbilt University School of Medicine, Nashville, Tennessee 37232 8548, USA
    J Neurosci 26:9851-9. 2006
    ..This mechanism would allow cholinergic, activity-triggered delivery of silent choline transporters to the plasma membrane, in which normal pH would reactivate the transporters for choline uptake and subsequent acetylcholine synthesis...
  35. ncbi Dopamine transporter/syntaxin 1A interactions regulate transporter channel activity and dopaminergic synaptic transmission
    Lucia Carvelli
    Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, TN 37232 8548, USA
    Proc Natl Acad Sci U S A 105:14192-7. 2008
    ..We propose that loss of UNC-64/DAT-1 interactions leads to enhanced synaptic DA release, providing a novel mechanism for DA neuron sensitization that may be relevant to mechanisms of DA-associated disorders...
  36. ncbi Anomalous dopamine release associated with a human dopamine transporter coding variant
    Michelle S Mazei-Robison
    Department of Pharmacology, Vanderbilt University Medical Center, Nashville, Tennessee 37232 8548, USA
    J Neurosci 28:7040-6. 2008
    ..Additionally, they suggest that block of inappropriate neurotransmitter efflux may be an unsuspected mechanism supporting the therapeutic actions of existing transporter-directed medications...
  37. ncbi Functional gene variation in the human norepinephrine transporter: association with attention deficit hyperactivity disorder
    Chun Hyung Kim
    Molecular Neurobiology Laboratory, McLean Hospital, Harvard Medical School, 115 Mill St, Belmont, MA 02478, USA
    Ann N Y Acad Sci 1129:256-60. 2008
    ..Moreover, we observed a significant association of the -3081(T) variant with ADHD. Altered transcription of SLC6A2 may therefore represent a novel risk factor for the development of ADHD...
  38. ncbi Interactions between integrin alphaIIbbeta3 and the serotonin transporter regulate serotonin transport and platelet aggregation in mice and humans
    Ana Marin D Carneiro
    Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, Tennessee 37232 8548, USA
    J Clin Invest 118:1544-52. 2008
    ....
  39. ncbi Bound to be different: neurotransmitter transporters meet their bacterial cousins
    L Keith Henry
    Department of Pharmacology, Vanderbilt University Nashville, TN 37232 8548, USA
    Mol Interv 7:306-9. 2007
    ....
  40. ncbi Vigorous motor activity in Caenorhabditis elegans requires efficient clearance of dopamine mediated by synaptic localization of the dopamine transporter DAT-1
    Paul W McDonald
    Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, Tennessee 37232 8548, USA
    J Neurosci 27:14216-27. 2007
    ..elegans are tightly regulated by synaptic DAT-1...
  41. ncbi Synthesis and characterization of a pegylated derivative of 3-(1,2,3,6-tetrahydro-pyridin-4yl)-1H-indole (IDT199): a high affinity SERT ligand for conjugation to quantum dots
    Ian D Tomlinson
    The Department of Chemistry, Vanderbilt University, Station B, 351822, Nashville, TN 37235 1822, USA
    Bioorg Med Chem Lett 17:5656-60. 2007
    ..In this paper we report the design and synthesis of a ligand that has a high affinity for the serotonin transporter (SERT) that may be conjugated to quantum dots...
  42. ncbi All aglow about presynaptic receptor regulation of neurotransmitter transporters
    Randy D Blakely
    Department of Pharmacology, Center for Molecular Neuroscience, Vanderbilt University School of Medicine, Nashville, TN 37232 8548, USA
    Mol Pharmacol 71:1206-8. 2007
    ....
  43. ncbi The functional impact of SLC6 transporter genetic variation
    Maureen K Hahn
    Department of Pharmacology and Center for Molecular Neuroscience, Vanderbilt University School of Medicine, Nashville, TN 37232, USA
    Annu Rev Pharmacol Toxicol 47:401-41. 2007
    ..Refining phenotypes, through assessment of endophenotypes, specific behavioral tasks, medication response, and brain network properties has also improved detection of the impact of genetic variation on complex behavior and disease...
  44. ncbi A polymorphism in the norepinephrine transporter gene alters promoter activity and is associated with attention-deficit hyperactivity disorder
    Chun Hyung Kim
    Molecular Neurobiology, McLean Hospital, Harvard Medical School, Belmont, MA 02478, USA
    Proc Natl Acad Sci U S A 103:19164-9. 2006
    ....
  45. ncbi p38 MAPK activation elevates serotonin transport activity via a trafficking-independent, protein phosphatase 2A-dependent process
    Chong-Bin Zhu
    Department of Psychiatry, Vanderbilt University School of Medicine, Nashville, Tennessee 37232-8548, USA
    J Biol Chem 280:15649-58. 2005
    ....
  46. ncbi Neurotoxin-induced degeneration of dopamine neurons in Caenorhabditis elegans
    Richard Nass
    Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, TN 37232 6420, USA
    Proc Natl Acad Sci U S A 99:3264-9. 2002
    ..6-OHDA-triggered neural degeneration does not require the CED-3/CED-4 cell death pathway, but is abolished by the genetic disruption of the C. elegans DAT...
  47. ncbi Dopaminergic neuronal loss and motor deficits in Caenorhabditis elegans overexpressing human alpha-synuclein
    Merja Lakso
    Department of Neurobiology, A I Virtanen Institute, Kuopio University, Finland
    J Neurochem 86:165-72. 2003
    ..This transgenic model in C. elegans, an invertebrate organism with excellent experimental resources for further genetic manipulation, may help facilitate dissection of pathophysiologic mechanisms of various synucleopathies...
  48. ncbi A regulated interaction of syntaxin 1A with the antidepressant-sensitive norepinephrine transporter establishes catecholamine clearance capacity
    Uhna Sung
    Department of Pharmacology and Center for Molecular Neuroscience, Vanderbilt University School of Medicine, Nashville, Tennessee 37232 8548, USA
    J Neurosci 23:1697-709. 2003
    ..These two contradictory roles of syntaxin 1A on NET appear to be linked and reveal a dynamic cycle of interactions that allow for the coordinated control between NE release and reuptake...
  49. ncbi Adenosine receptor, protein kinase G, and p38 mitogen-activated protein kinase-dependent up-regulation of serotonin transporters involves both transporter trafficking and activation
    Chong-Bin Zhu
    Department of Psychiatry, Vanderbilt School of Medicine, Nashville, Tennessee 37232-8548, USA
    Mol Pharmacol 65:1462-74. 2004
    ..Together, these results reveal two PKG-dependent pathways supporting rapid SERT regulation by A3 ARs, one leading to enhanced SERT surface trafficking, and a separate, p38 MAPK-dependent process augmenting SERT intrinsic activity...
  50. ncbi Calcium-dependent inhibition of synaptosomal serotonin transport by the alpha 2-adrenoceptor agonist 5-bromo-N-[4,5-dihydro-1H-imidazol-2-yl]-6-quinoxalinamine (UK14304)
    Twum Ampofo Ansah
    Department of Pharmacology, Meharry Medical College, 1005 D B Todd Blvd, Nashville, TN 37208, USA
    J Pharmacol Exp Ther 305:956-65. 2003
    ..Our findings suggest that UK14304 modulates SERT function in vitro and in vivo via signaling pathways, possibly supported by an influx of Ca2+ through voltage-sensitive Ca2+ channels...
  51. ncbi Expression studies of naturally occurring human dopamine transporter variants identifies a novel state of transporter inactivation associated with Val382Ala
    Michelle S Mazei-Robison
    Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN, USA
    Neuropharmacology 49:737-49. 2005
    ..Analysis of PMA-induced V382A internalization revealed a trafficking-independent action of PMA, consistent with the existence of a surface-localized, transport-inactive state...
  52. ncbi Stimulation of serotonin transport by the cyclic GMP phosphodiesterase-5 inhibitor sildenafil
    Chong-Bin Zhu
    Department of Psychiatry, Vanderbilt University School of Medicine, Nashville, TN 37232-8548, USA
    Eur J Pharmacol 504:1-6. 2004
    ..These findings implicate cGMP-targeted PDEs in limiting the regulation of antidepressant-sensitive 5-HT transport...
  53. ncbi Dopamine transporters depolarize neurons by a channel mechanism
    Lucia Carvelli
    Department of Pharmacology and Center of Neuroscience, Vanderbilt University School of Medicine, Nashville, TN 37232 8548, USA
    Proc Natl Acad Sci U S A 101:16046-51. 2004
    ..Thus, DA transporters not only transport DA but also exhibit a channel mode of conduction that directly modulates membrane potential and neuronal function...
  54. ncbi 5-Hydroxytryptamine drives apoptosis in biopsylike Burkitt lymphoma cells: reversal by selective serotonin reuptake inhibitors
    Adamantios Serafeim
    MRC Centre for Immune Regulation and the Department of Pharmacology, Medical School, University of Birmingham, Vincent Drive, Birmingham B15 2TT, UK
    Blood 99:2545-53. 2002
    ..These data indicate that serotonin drives apoptosis in biopsylike BL cells after its entry through an active transport mechanism, and they suggest a novel therapeutic modality for Burkitt lymphoma...
  55. ncbi Evidence for biphasic effects of protein kinase C on serotonin transporter function, endocytosis, and phosphorylation
    Lankupalle D Jayanthi
    Department of Physiology and Neuroscience, Medical University of South Carolina, 173 Ashley Ave, BSB 403, Charleston, SC 29425, USA
    Mol Pharmacol 67:2077-87. 2005
    ....
  56. ncbi Amphetamine induces dopamine efflux through a dopamine transporter channel
    Kristopher M Kahlig
    Department of Molecular Physiology and Biophysics, Vanderbilt University School of Medicine, 465 21st Avenue South, Nashville, TN 37232-8548, USA
    Proc Natl Acad Sci U S A 102:3495-500. 2005
    ..Unlike AMPH, the endogenous substrate DA, when present on both sides of the plasma membrane, inhibits this channel-like activity, thereby suggesting that the DAT channel-like mode cannot accumulate DA against a concentration gradient...
  57. ncbi Targeting cell surface receptors with ligand-conjugated nanocrystals
    Sandra J Rosenthal
    Department of Chemistry, Vanderbilt University School of Medicine, Vanderbilt University, Nashville, Tennessee 37235, USA
    J Am Chem Soc 124:4586-94. 2002
    ..These findings support further consideration of ligand-conjugated nanocrystals as versatile probes of membrane proteins in living cells...
  58. ncbi The Caenorhabditis elegans dopaminergic system: opportunities for insights into dopamine transport and neurodegeneration
    Richard Nass
    Department of Pharmacology, Vanderbilt University Medical Center, Nashville, Tennessee 37232 6420, USA
    Annu Rev Pharmacol Toxicol 43:521-44. 2003
    ..elegans with an eye toward opportunities for uncovering DAT mutants, DAT regulators, and components of toxin-mediated cell death...
  59. ncbi Distribution of high affinity choline transporter immunoreactivity in the primate central nervous system
    Laura Kus
    Department of Neurological Sciences, Rush Presbyterian-St. Luke's Medical Center, Chicago, Illinois 60612
    J Comp Neurol 463:341-57. 2003
    ..The present observations indicate that the present CHT antibody labels cholinergic structures within the primate CNS and provides an additional marker for the investigation of cholinergic neuronal function in aging and disease...
  60. ncbi Hypoinsulinemia regulates amphetamine-induced reverse transport of dopamine
    Jason M Williams
    Department of Molecular Physiology and Biophysics, Vanderbilt University Medical Center, Nashville, Tennessee, USA
    PLoS Biol 5:e274. 2007
    ..These data suggest that insulin signaling pathways may represent a novel mechanism for regulating DA transmission, one which may be targeted for the treatment of AMPH abuse and potentially other dopaminergic disorders...
  61. ncbi Desvenlafaxine succinate identifies novel antagonist binding determinants in the human norepinephrine transporter
    John N Mason
    Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, Tennessee, USA
    J Pharmacol Exp Ther 323:720-9. 2007
    ..In an initial search for molecular features that differentially define antagonist binding determinants, we document that Val148 in hNET transmembrane domain 3 selectively disrupts NIS binding but not that of DVS...
  62. ncbi Serotonin and cocaine-sensitive inactivation of human serotonin transporters by methanethiosulfonates targeted to transmembrane domain I
    L Keith Henry
    Department of Pharmacology, Vanderbilt University Medical Center, Nashville, Tennessee 37232-8548, USA
    J Biol Chem 278:37052-63. 2003
    ..Moreover, we identify a limit to accessibility for membrane-impermeant MTS reagents that may reflect aspects of an occluded permeation pathway...
  63. ncbi Distinctions between dopamine transporter antagonists could be just around the bend
    L Keith Henry
    Department of Pharmacology, Physiology, and Therapeutics, University of North Dakota School of Medicine and Health Sciences, Grand Forks, ND 58203, USA
    Mol Pharmacol 73:616-8. 2008
    ....
  64. ncbi Quantum dot ex vivo labeling of neuromuscular synapses
    Rebecca L Orndorff
    Department of Chemistry, Vanderbilt University, Vanderbilt School of Medicine, Vanderbilt University, Nashville, Tennessee 37235 1822, USA
    Nano Lett 8:780-5. 2008
    ..This approach provides a novel methodology for the direct assessment of the presence and mobility of neurotransmitter receptors in native tissue...
  65. ncbi Aberrant trafficking of the high-affinity choline transporter in AP-3-deficient mice
    Hidemi Misawa
    Department of Pharmacology, Kyoritsu University of Pharmacy, Tokyo 105 8512, Japan
    Eur J Neurosci 27:3109-17. 2008
    ..The amounts of CHT detected on SLMV are greatly reduced by treating the cell with agents that halt AP-dependent membrane trafficking. These results demonstrate that APs have important functions for CHT trafficking in neuronal cells...
  66. ncbi Binding and transport in norepinephrine transporters. Real-time, spatially resolved analysis in single cells using a fluorescent substrate
    Joel W Schwartz
    Department of Pharmacology, Center for Molecular Neuroscience, Vanderbilt University Medical Center, Nashville, Tennessee 37232-8548, USA
    J Biol Chem 278:9768-77. 2003
    ....
  67. ncbi Genetic basis of clinical catecholamine disorders
    Emily M Garland
    Vanderbilt U, Nashville, TN
    Ann N Y Acad Sci 971:506-14. 2002
    ....
  68. ncbi A mutation in the human norepinephrine transporter gene (SLC6A2) associated with orthostatic intolerance disrupts surface expression of mutant and wild-type transporters
    Maureen K Hahn
    Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, Tennessee 37232 8548, USA
    J Neurosci 23:4470-8. 2003
    ..These results elucidate a molecular mechanism for the disrupted NE homeostasis and cardiovascular function evident in OI patients with the hNET-A457P mutation...
  69. ncbi Rapid stimulation of presynaptic serotonin transport by A(3) adenosine receptors
    Chong Bin Zhu
    Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, TN 37232, USA
    J Pharmacol Exp Ther 322:332-40. 2007
    ..Together, these results identify a novel, region-specific action of CNS A(3)ARs in the modulation of SERT-mediated 5-HT transport that may be relevant for the etiology and/or therapy of 5-HT-linked brain disorders...
  70. ncbi Ultrastructural localization of the norepinephrine transporter in superficial and deep layers of the rat prelimbic prefrontal cortex and its spatial relationship to probable dopamine terminals
    LeeAnn H Miner
    Department of Neuroscience, University of Pittsburgh, Pittsburgh, Pennsylvania 15260, USA
    J Comp Neurol 466:478-94. 2003
    ..These results suggest that, in the rat PFC, NE axons (1) contain predominantly cytoplasmic NET, (2) infrequently contain TH immunolabeling, and (3) may interact with probable DA afferents by means of extrasynaptic mechanisms...
  71. ncbi Peptide-conjugated quantum dots: imaging the angiotensin type 1 receptor in living cells
    Ian D Tomlinson
    Department of Chemistry, Vanderbilt University, Nashville, TN, USA
    Methods Mol Biol 303:51-60. 2005
    ..The Ang II-quantum dot conjugates did not bind to parental cells and showed similar staining patterns when compared with a commercially available Ang II Alexa 488 conjugate...
  72. ncbi Single nucleotide polymorphisms in the human norepinephrine transporter gene affect expression, trafficking, antidepressant interaction, and protein kinase C regulation
    Maureen K Hahn
    Center for Molecular Neuroscience, 6133 Medical Research Building III, Suite 7140, Vanderbilt School of Medicine, Nashville, TN 37232-8548, USA
    Mol Pharmacol 68:457-66. 2005
    ..These findings reveal functional deficits that are likely to compromise NE signaling in SNP carriers in the population and identify key regions of NET contributing to transporter biosynthesis, activity, and regulation...
  73. ncbi Human serotonin transporter variants display altered sensitivity to protein kinase G and p38 mitogen-activated protein kinase
    Harish C Prasad
    Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, TN 37232 8548, USA
    Proc Natl Acad Sci U S A 102:11545-50. 2005
    ....
  74. ncbi Regulation of choline transporter surface expression and phosphorylation by protein kinase C and protein phosphatase 1/2A
    Jeremiah Gates
    Department of Anatomy and Neurobiology, University of Kentucky Medical Center, 306 Whitney Hendrickson Building, 800 Rose Street, Lexington, KY 40536 0098, USA
    J Pharmacol Exp Ther 310:536-45. 2004
    ..These studies also provide the first evidence that CHT is a phosphoprotein and that the basal PP1/PP2A activity may have a dominant role in controlling the levels of CHT phosphorylation...
  75. ncbi Lethal impairment of cholinergic neurotransmission in hemicholinium-3-sensitive choline transporter knockout mice
    Shawn M Ferguson
    Neuroscience Graduate Program, Vanderbilt University, Nashville, TN 37232, USA
    Proc Natl Acad Sci U S A 101:8762-7. 2004
    ..Our results demonstrate that CHT is an essential and regulated presynaptic component of cholinergic signaling and indicate that CHT warrants consideration as a candidate gene for disorders characterized by cholinergic hypofunction...
  76. ncbi The N-terminus of the norepinephrine transporter regulates the magnitude and selectivity of the transporter-associated leak current
    Francesca Binda
    Department of Molecular Physiology and Biophysics, Vanderbilt University, 465 21st Ave. South, Nashville, TN 37232-8548, USA
    Neuropharmacology 50:354-61. 2006
    ..These data suggest that the NET N-terminus regulates and defines the ionic specificity of the NET-mediated leak current...
  77. ncbi The proinflammatory cytokines interleukin-1beta and tumor necrosis factor-alpha activate serotonin transporters
    Chong-Bin Zhu
    Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, TN 37232-8645, USA
    Neuropsychopharmacology 31:2121-31. 2006
    ..These results provide the first evidence that proinflammatory cytokines can acutely regulate neuronal SERT activity via p38 MAPK-linked pathways...
  78. ncbi Getting the message across: a recent transporter structure shows the way
    L Keith Henry
    Department of Pharmacology and Center for Molecular Neuroscience, Vanderbilt University School of Medicine, Nashville, Tennessee 37232, USA
    Neuron 49:791-6. 2006
    ....
  79. ncbi Dopamine signaling architecture in Caenorhabditis elegans
    Paul W McDonald
    Graduate Program in Neuroscience, Department of Pharmacology, Center for Molecular Neuroscience, Vanderbilt University School of Medicine, Nashville, Tennessee 37232-8548, USA
    Cell Mol Neurobiol 26:593-618. 2006
    ..Further use of the model offers prospects for the identification of novel genes and proteins whose study may yield benefits for DA-supported neural disorders in man...
  80. ncbi Ultrastructural interactions between terminals expressing the norepinephrine transporter and dopamine neurons in the rat and monkey ventral tegmental area
    Lindsay A Liprando
    Departments of Neuroscience and Psychiatry, University of Pittsburgh, Pittsburgh, Pennsylvania 15260, USA
    Synapse 52:233-44. 2004
    ..The latter finding agrees with observations in cortical regions and represents the first report of its type in a subcortical structure...
  81. ncbi Serotonin-, protein kinase C-, and Hic-5-associated redistribution of the platelet serotonin transporter
    Ana Marin D Carneiro
    Departments of Pharmacology and Psychiatry, Center for Molecular Neuroscience, Vanderbilt University School of Medicine, Nashville, Tennessee 37232-8548, USA
    J Biol Chem 281:24769-80. 2006
    ..Associations of SERT with Hic-5 are evident in brain synaptosomes, suggesting the existence of parallel mechanisms operating to regulate SERT at serotonergic synapses...
  82. ncbi The choline transporter resurfaces: new roles for synaptic vesicles?
    Shawn M Ferguson
    Neuroscience Graduate Program, Vanderbilt Brain Institute, Vanderbilt University Medical Center, Nashville, TN 37232, USA
    Mol Interv 4:22-37. 2004
    ....
  83. ncbi Acetylcholine is an autocrine or paracrine hormone synthesized and secreted by airway bronchial epithelial cells
    Becky J Proskocil
    Division of Neuroscience, Oregon National Primate Research Center, 505 Northwest 185th Avenue, Beaverton, Oregon 97006, USA
    Endocrinology 145:2498-506. 2004
    ..This pathway may also explain some of the effects of nicotine on fetal development and also provides additional mechanisms by which smoking affects lung cancer growth and development...
  84. ncbi Cell surface trafficking of the antidepressant-sensitive norepinephrine transporter revealed with an ectodomain antibody
    Valentina Savchenko
    Department of Pharmacology and Center for Molecular Neuroscience, Vanderbilt University School of Medicine, Nashville, TN 37232-8548, USA
    Mol Cell Neurosci 24:1131-50. 2003
    ..These findings provide the first evidence for regulated trafficking of NET in neurons and support the suggestion that activity-dependent NET trafficking may provide additional modulatory capacity for noradrenergic signaling...
  85. ncbi Vesicular localization and activity-dependent trafficking of presynaptic choline transporters
    Shawn M Ferguson
    Neuroscience Graduate Program, Center for Molecular Neuroscience, Vanderbilt University, Nashville, Tennessee 37232, USA
    J Neurosci 23:9697-709. 2003
    ....
  86. ncbi Calcium-dependent interactions of the human norepinephrine transporter with syntaxin 1A
    Uhna Sung
    Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, TN 37232 8548, USA
    Mol Cell Neurosci 34:251-60. 2007
    ..Furthermore, PMA enhanced Ca2+-dependent modulation of NE transport in synaptosomes. Our data reveal roles for SYN1A in the Ca2+-dependent regulation of NET, likely reliant on regulation by PKC signaling, but independent of CaMK...
  87. ncbi Labeling cell-surface proteins via antibody quantum dot streptavidin conjugates
    John N Mason
    Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, TN, USA
    Methods Mol Biol 303:35-50. 2005
    ..In this chapter, we outline the methodology for using streptavidin quantum dots to label biotinylated antibodies that target cell-surface ectodomain proteins on both living and fixed cells...