Yiyun Huang

Summary

Affiliation: Columbia University
Country: USA

Publications

  1. ncbi Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands
    Y Huang
    Department of Psychiatry, Columbia University College of Physicians and Surgeons, New York, NY 10032, USA
    Bioorg Med Chem Lett 11:1375-7. 2001
  2. ncbi A positron emission tomography radioligand for the in vivo labeling of metabotropic glutamate 1 receptor: (3-ethyl-2-[11C]methyl-6-quinolinyl)(cis- 4-methoxycyclohexyl)methanone
    Yiyun Huang
    Departments of Psychiatry and Radiology, Columbia University College of Physicians and Surgeons, 1051 Riverside Drive, New York, NY 10032, USA
    J Med Chem 48:5096-9. 2005
  3. ncbi A PET imaging agent with fast kinetics: synthesis and in vivo evaluation of the serotonin transporter ligand [11C]2-[2-dimethylaminomethylphenylthio)]-5-fluorophenylamine ([11C]AFA)
    Yiyun Huang
    Department of Psychiatry, Columbia University College of Physicians and Surgeons, 1051 Riverside Drive, Box 31, New York, NY 10032, USA
    Nucl Med Biol 31:727-38. 2004
  4. ncbi Epibatidine analogues as selective ligands for the alpha(x)beta2-containing subtypes of nicotinic acetylcholine receptors
    Yiyun Huang
    Department of Psychiatry, Columbia University College of Physicians and Surgeons, New York, NY 10032, USA
    Bioorg Med Chem Lett 15:4385-8. 2005
  5. ncbi Synthesis of potent and selective serotonin 5-HT1B receptor ligands
    Yiyun Huang
    Department of Psychiatry, Columbia University College of Physicians and Surgeons, New York, NY 10032, USA
    Bioorg Med Chem Lett 15:4786-9. 2005
  6. ncbi Comparative evaluation in nonhuman primates of five PET radiotracers for imaging the serotonin transporters: [11C]McN 5652, [11C]ADAM, [11C]DASB, [11C]DAPA, and [11C]AFM
    Yiyun Huang
    Department of Psychiatry, Columbia University College of Physicians and Surgeons, New York, NY, USA
    J Cereb Blood Flow Metab 22:1377-98. 2002
  7. ncbi Synthesis and pharmacological characterization of a new PET ligand for the serotonin transporter: [11C]5-bromo-2-[2-(dimethylaminomethylphenylsulfanyl)]phenylamine ([11C]DAPA)
    Yiyun Huang
    Department of Psychiatry, Columbia University College of Physicians and Surgeons, New York, NY 10032, USA
    Nucl Med Biol 29:741-51. 2002
  8. ncbi In vivo vulnerability to competition by endogenous dopamine: comparison of the D2 receptor agonist radiotracer (-)-N-[11C]propyl-norapomorphine ([11C]NPA) with the D2 receptor antagonist radiotracer [11C]-raclopride
    Rajesh Narendran
    Department of Psychiatry, Columbia University College of Physicians and Surgeons and the New York State Psychiatric Institute, New York, NY 10032, USA
    Synapse 52:188-208. 2004
  9. ncbi The new PET imaging agent [11C]AFE is a selective serotonin transporter ligand with fast brain uptake kinetics
    Zhihong Zhu
    Department of Psychiatry, Columbia University College of Physicians and Surgeons, New York, NY 10032, USA
    Nucl Med Biol 31:983-94. 2004
  10. ncbi Increased synaptic dopamine function in associative regions of the striatum in schizophrenia
    Lawrence S Kegeles
    Department of Psychiatry, Columbia University College of Physicians and Surgeons, New York, New York, USA
    Arch Gen Psychiatry 67:231-9. 2010

Research Grants

  1. New PET radioligand for the serotonin transporter
    Yiyun Huang; Fiscal Year: 2007

Detail Information

Publications45

  1. ncbi Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands
    Y Huang
    Department of Psychiatry, Columbia University College of Physicians and Surgeons, New York, NY 10032, USA
    Bioorg Med Chem Lett 11:1375-7. 2001
    ..All new compounds display high affinity and selectivity for the D(4) receptors and compounds 5b, 5d, and 5e were identified as candidates for radioligand development...
  2. ncbi A positron emission tomography radioligand for the in vivo labeling of metabotropic glutamate 1 receptor: (3-ethyl-2-[11C]methyl-6-quinolinyl)(cis- 4-methoxycyclohexyl)methanone
    Yiyun Huang
    Departments of Psychiatry and Radiology, Columbia University College of Physicians and Surgeons, 1051 Riverside Drive, New York, NY 10032, USA
    J Med Chem 48:5096-9. 2005
    ..Results from animal experiments demonstrate that the radioligand [11C]2 is the first PET tracer capable of labeling the rat mGlu1 receptor in vivo...
  3. ncbi A PET imaging agent with fast kinetics: synthesis and in vivo evaluation of the serotonin transporter ligand [11C]2-[2-dimethylaminomethylphenylthio)]-5-fluorophenylamine ([11C]AFA)
    Yiyun Huang
    Department of Psychiatry, Columbia University College of Physicians and Surgeons, 1051 Riverside Drive, Box 31, New York, NY 10032, USA
    Nucl Med Biol 31:727-38. 2004
    ..In summary, [11C]AFA appears to be an appropriate PET radioligand with a fast brain uptake kinetics:..
  4. ncbi Epibatidine analogues as selective ligands for the alpha(x)beta2-containing subtypes of nicotinic acetylcholine receptors
    Yiyun Huang
    Department of Psychiatry, Columbia University College of Physicians and Surgeons, New York, NY 10032, USA
    Bioorg Med Chem Lett 15:4385-8. 2005
    ..As a result they might become lead structures for the design and synthesis of highly selective ligands for nAChR subtypes containing the beta2 subunit...
  5. ncbi Synthesis of potent and selective serotonin 5-HT1B receptor ligands
    Yiyun Huang
    Department of Psychiatry, Columbia University College of Physicians and Surgeons, New York, NY 10032, USA
    Bioorg Med Chem Lett 15:4786-9. 2005
    ..Many of these new compounds displayed high affinity and selectivity for the 5-HT1B receptor and compound 6c was found to have the in vitro binding profile necessary for development as a PET radioligand...
  6. ncbi Comparative evaluation in nonhuman primates of five PET radiotracers for imaging the serotonin transporters: [11C]McN 5652, [11C]ADAM, [11C]DASB, [11C]DAPA, and [11C]AFM
    Yiyun Huang
    Department of Psychiatry, Columbia University College of Physicians and Surgeons, New York, NY, USA
    J Cereb Blood Flow Metab 22:1377-98. 2002
    ....
  7. ncbi Synthesis and pharmacological characterization of a new PET ligand for the serotonin transporter: [11C]5-bromo-2-[2-(dimethylaminomethylphenylsulfanyl)]phenylamine ([11C]DAPA)
    Yiyun Huang
    Department of Psychiatry, Columbia University College of Physicians and Surgeons, New York, NY 10032, USA
    Nucl Med Biol 29:741-51. 2002
    ..In summary, [11C]DAPA appears to be a promising radioligand suitable for the visualization of SERT in vivo using PET...
  8. ncbi In vivo vulnerability to competition by endogenous dopamine: comparison of the D2 receptor agonist radiotracer (-)-N-[11C]propyl-norapomorphine ([11C]NPA) with the D2 receptor antagonist radiotracer [11C]-raclopride
    Rajesh Narendran
    Department of Psychiatry, Columbia University College of Physicians and Surgeons and the New York State Psychiatric Institute, New York, NY 10032, USA
    Synapse 52:188-208. 2004
    ..In conclusion, [11C]NPA might provide a superior radiotracer to probe presynaptic DA function with PET in health and disease...
  9. ncbi The new PET imaging agent [11C]AFE is a selective serotonin transporter ligand with fast brain uptake kinetics
    Zhihong Zhu
    Department of Psychiatry, Columbia University College of Physicians and Surgeons, New York, NY 10032, USA
    Nucl Med Biol 31:983-94. 2004
    ..In summary, [(11)C]AFE appears to be a PET radioligand with fast brain uptake kinetics and can be used for the visualization and quantification of SERT in vivo...
  10. ncbi Increased synaptic dopamine function in associative regions of the striatum in schizophrenia
    Lawrence S Kegeles
    Department of Psychiatry, Columbia University College of Physicians and Surgeons, New York, New York, USA
    Arch Gen Psychiatry 67:231-9. 2010
    ....
  11. ncbi Serotonin transporter availability in patients with schizophrenia: a positron emission tomography imaging study with [11C]DASB
    W Gordon Frankle
    Department of Psychiatry, Columbia University College of Physicians and Surgeons and the New York State Psychiatric Institute, New York, New York 10032, USA
    Biol Psychiatry 57:1510-6. 2005
    ..The aim of this study was to compare SERT availability in vivo in patients with schizophrenia and matched control subjects...
  12. ncbi Amphetamine-induced dopamine release: markedly blunted in cocaine dependence and predictive of the choice to self-administer cocaine
    Diana Martinez
    Department of Psychiatry, Columbia University College of Physicians and Surgeons, New York, NY 10032, USA
    Am J Psychiatry 164:622-9. 2007
    ..Furthermore, the relationship between this dopamine response and the choice to self-administer cocaine in a laboratory model of relapse was investigated...
  13. ncbi A new positron emission tomography imaging agent for the serotonin transporter: synthesis, pharmacological characterization, and kinetic analysis of [11C]2-[2-(dimethylaminomethyl)phenylthio]-5-fluoromethylphenylamine ([11C]AFM)
    Yiyun Huang
    Department of Psychiatry, Columbia University College of Physicians and Surgeons, 1051 Riverside Drive, Box 31, New York, NY 10032, USA
    Nucl Med Biol 31:543-56. 2004
    ..In summary, [(11)C]AFM appears to be an excellent PET radioligand for the visualization and reliable quantification of SERT in vivo...
  14. ncbi Fluorinated diaryl sulfides as serotonin transporter ligands: synthesis, structure-activity relationship study, and in vivo evaluation of fluorine-18-labeled compounds as PET imaging agents
    Yiyun Huang
    Department of Psychiatry and Radiology, Columbia University College of Physicians and Surgeons, New York, New York 10032, USA
    J Med Chem 48:2559-70. 2005
    ..Among these four ligands, three appear to be promising radioligands suitable for the labeling of SERT in vivo, with 18a providing a higher specific binding in vivo than 16 or 18b...
  15. ncbi Measurement of the serotonin 1A receptor availability in patients with schizophrenia during treatment with the antipsychotic medication ziprasidone
    W Gordon Frankle
    Department of Psychiatry, Columbia University College of Physicians and Surgeons, New York, USA
    J Psychopharmacol 25:734-43. 2011
    ..The finding of a relationship between 5-HT(1A) binding and the degree of improvement in negative symptoms provides further support for the role of the 5-HT(1A) receptor in the pathophysiology and treatment of this symptom domain...
  16. ncbi Serotonin 1A receptor availability in patients with schizophrenia and schizo-affective disorder: a positron emission tomography imaging study with [11C]WAY 100635
    W Gordon Frankle
    Departments of Psychiatry and Radiology, Western Psychiatric Institute and Clinic, University of Pittsburgh, Pittsburgh, PA 15213, USA
    Psychopharmacology (Berl) 189:155-64. 2006
    ..This study examines 5-HT(1A) availability in vivo in individuals with schizophrenia and schizo-affective disorder...
  17. ncbi Modulation of amphetamine-induced dopamine release by group II metabotropic glutamate receptor agonist LY354740 in non-human primates studied with positron emission tomography
    Bart N M van Berckel
    Department of Psychiatry, Columbia University, New York, NY, USA
    Neuropsychopharmacology 31:967-77. 2006
    ....
  18. ncbi Altered prefrontal dopaminergic function in chronic recreational ketamine users
    Rajesh Narendran
    Department of Psychiatry, Columbia University College of Physicians and Surgeons, New York, NY, USA
    Am J Psychiatry 162:2352-9. 2005
    ..In this study, dopamine D1 receptor availability was assessed by using positron emission tomography and the selective D1 receptor radioligand [11C]NNC 112 in a group of 14 recreational chronic ketamine users and matched healthy subjects...
  19. ncbi Synthesis and characterization of two PET radioligands for the metabotropic glutamate 1 (mGlu1) receptor
    Yiyun Huang
    Department of Psychiatry, Columbia University College of Physicians and Surgeons, New York, New York, USA
    Synapse 66:1002-14. 2012
    ..Radioligands with higher affinity and/or lower lipophilicity are needed to successfully image the mGlu1 receptor in humans...
  20. ncbi Effects of reduced endogenous 5-HT on the in vivo binding of the serotonin transporter radioligand 11C-DASB in healthy humans
    Peter S Talbot
    Department of Psychiatry, Columbia University College of Physicians and Surgeons, New York State Psychiatric Institute, New York, New York 10032, USA
    Synapse 55:164-75. 2005
    ..These results suggest that (11)C-DASB in vivo binding is not affected by reductions in endogenous 5-HT...
  21. ncbi 11C-GR103545, a radiotracer for imaging kappa-opioid receptors in vivo with PET: synthesis and evaluation in baboons
    Peter S Talbot
    Department of Psychiatry, Columbia University College of Physicians and Surgeons and the New York State Psychiatric Institute, New York, NY 10032, USA
    J Nucl Med 46:484-94. 2005
    ..The (-)-isomer, GR103545, is the active enantiomer of GR89696. The aim of this study was to characterize the potential of 11C-GR103545 to image kappa-OR in vivo with PET...
  22. ncbi Comparative evaluation of serotonin transporter radioligands 11C-DASB and 11C-McN 5652 in healthy humans
    W Gordon Frankle
    Department of Psychiatry, Columbia University College of Physicians and Surgeons, and the New York State Psychiatric Institute, New York, New York, USA
    J Nucl Med 45:682-94. 2004
    ..The purpose of this study was to compare these 2 agents in healthy humans...
  23. ncbi Positron emission tomography imaging of the serotonin transporter and 5-HT(1A) receptor in alcohol dependence
    Diana Martinez
    Department of Psychiatry, Columbia University College of Physicians and Surgeons, 1051 Riverside Drive, New York, NY 10032, USA
    Biol Psychiatry 65:175-80. 2009
    ..This is the first report of combined tracers for pre- and postsynaptic serotonergic transmission in the same alcoholic subjects and the first study of 5-HT(1A) receptors in alcoholism...
  24. ncbi Alcohol dependence is associated with blunted dopamine transmission in the ventral striatum
    Diana Martinez
    Department of Psychiatry, Columbia University College of Physicians and Surgeons, New York, USA
    Biol Psychiatry 58:779-86. 2005
    ..This study measured D2 receptors and dopamine transmission in human alcohol-dependent (AD) subjects using positron emission tomography (PET) and [11C]raclopride...
  25. ncbi Cocaine dependence and d2 receptor availability in the functional subdivisions of the striatum: relationship with cocaine-seeking behavior
    Diana Martinez
    Department of Psychiatry, Columbia University College of Physicians and Surgeons, New York, NY, USA
    Neuropsychopharmacology 29:1190-202. 2004
    ..Additional research is warranted to unravel potential neurobiological traits that might confer vulnerability to relapse in detoxified CCD subjects...
  26. ncbi Brain serotonin transporter distribution in subjects with impulsive aggressivity: a positron emission study with [11C]McN 5652
    W Gordon Frankle
    Department of Psychiatry, Columbia University College of Physicians and Surgeons, and the New York State Psychiatric Institute, 1051 Riverside Dr, Box 31, New York, NY 10032, USA
    Am J Psychiatry 162:915-23. 2005
    ..This study evaluated regional serotonin transporter distribution in the brain of individuals with impulsive aggression by using positron emission tomography (PET) with the serotonin transporter PET radiotracer [(11)C]McN 5652...
  27. ncbi Measurement of the proportion of D2 receptors configured in state of high affinity for agonists in vivo: a positron emission tomography study using [11C]N-propyl-norapomorphine and [11C]raclopride in baboons
    Rajesh Narendran
    New York State Psychiatric Institute, 1051 Riverside Dr, Box 31, New York, NY 10032, USA
    J Pharmacol Exp Ther 315:80-90. 2005
    ....
  28. ncbi Effect of amphetamine on [(18)F]fallypride in vivo binding to D(2) receptors in striatal and extrastriatal regions of the primate brain: Single bolus and bolus plus constant infusion studies
    Mark Slifstein
    Department of Psychiatry, Columbia University College of Physicians and Surgeons and the New York State Psychiatric Institute, New York, New York 10032, USA
    Synapse 54:46-63. 2004
    ....
  29. ncbi Occupancy of brain serotonin transporters during treatment with paroxetine in patients with social phobia: a positron emission tomography study with 11C McN 5652
    Justine M Kent
    New York State Psychiatry Institute, New York, NY 10032, USA
    Psychopharmacology (Berl) 164:341-8. 2002
    ....
  30. ncbi Biodistribution and radiation dosimetry of the dopamine D2 ligand 11C-raclopride determined from human whole-body PET
    Mark Slifstein
    Department of Psychiatry, Columbia University, New York, New York 10032, USA
    J Nucl Med 47:313-9. 2006
    ..Whole-body radiation dosimetry of 11C-raclopride was performed in healthy human volunteers...
  31. ncbi Lower serotonin transporter binding potential in the human brain during major depressive episodes
    Ramin V Parsey
    Department of Psychiatry, Columbia University College of Physicians and Surgeons, New York, USA
    Am J Psychiatry 163:52-8. 2006
    ..On the basis of postmortem and imaging studies, the authors hypothesized that subjects with major depressive disorder in a major depressive episode have fewer serotonin transporter sites, compared with healthy subjects...
  32. ncbi Estimation of serotonin transporter parameters with 11C-DASB in healthy humans: reproducibility and comparison of methods
    W Gordon Frankle
    Department of Psychiatry, Columbia University College of Physicians and Surgeons, New York State Psychiatric Institute, New York, NY 10032, USA
    J Nucl Med 47:815-26. 2006
    ..The aim of the present study was to define the optimal analytic method to derive accurate and reliable serotonin transporter (SERT) receptor parameters with (11)C-3-amino-4-(2-[(dimethylamino)methyl]phenylthio)benzonitrile ((11)C-DASB)...
  33. ncbi Imaging human mesolimbic dopamine transmission with positron emission tomography. Part II: amphetamine-induced dopamine release in the functional subdivisions of the striatum
    Diana Martinez
    Department of Psychiatry, Columbia University College of Physicians and Surgeons, 1051 Riverside Drive, New York, NY 10032, USA
    J Cereb Blood Flow Metab 23:285-300. 2003
    ....
  34. ncbi Quantitative analysis of (-)-N-(11)C-propyl-norapomorphine in vivo binding in nonhuman primates
    Dah Ren Hwang
    Department of Psychiatry, Columbia University College of Physicians and Surgeons, New York, NY, USA
    J Nucl Med 45:338-46. 2004
    ..The goal of this study was to develop and evaluate analytic strategies to derive in vivo (11)C-NPA binding parameters...
  35. ncbi In vivo affinity of [18F]fallypride for striatal and extrastriatal dopamine D2 receptors in nonhuman primates
    Mark Slifstein
    Department of Psychiatry, Columbia University College of Physicians and Surgeons, New York, NY, USA
    Psychopharmacology (Berl) 175:274-86. 2004
    ..The high signal to noise ratio of [18F]fallypride has been attributed to its high affinity for D2 receptors (K(D) of 0.03 nM, measured in vitro at room temperature)...
  36. ncbi Relationships between radiotracer properties and image quality in molecular imaging of the brain with positron emission tomography
    Marc Laruelle
    Department of Psychiatry, Columbia University College of Physicians and Surgeons, New York, NY 10032, USA
    Mol Imaging Biol 5:363-75. 2003
    ..It is shown that, within a given structural family, affinity and lipophilicity are associated with scan outcome in a relatively predictable manner...
  37. ncbi Extended characterisation of the serotonin 2A (5-HT2A) receptor-selective PET radiotracer 11C-MDL100907 in humans: quantitative analysis, test-retest reproducibility, and vulnerability to endogenous 5-HT tone
    Peter S Talbot
    Department of Psychiatry, Columbia University College of Physicians and Surgeons and the New York State Psychiatric Institute, New York, NY 10032, USA
    Neuroimage 59:271-85. 2012
    ..We present an extended characterisation in healthy human subjects...
  38. ncbi Reduced amygdala serotonin transporter binding in posttraumatic stress disorder
    James W Murrough
    Mood and Anxiety Disorders Program, Department of Psychiatry, Mount Sinai School of Medicine, New York, NY, USA
    Biol Psychiatry 70:1033-8. 2011
    ....
  39. ncbi Prefrontal dopamine D1 receptors and working memory in schizophrenia
    Anissa Abi-Dargham
    Department of Psychiatry, Columbia University College of Physicians and Surgeons and New York State Psychiatric Institute, New York, New York 10032, USA
    J Neurosci 22:3708-19. 2002
    ..Increased D1 receptor availability observed in patients with schizophrenia might represent a compensatory (but ineffective) upregulation secondary to sustained deficiency in mesocortical DA function...
  40. ncbi Positron emission tomography: imaging and quantification of neurotransporter availability
    Marc Laruelle
    Department of Psychiatry and Department of Radiology, Columbia University College of Physicians and Surgeons, 1051 Riverside Drive, Unit 31, New York, New York 10032, USA
    Methods 27:287-99. 2002
    ..In conclusion, no universally "best" method is applicable to all neurotransporter imaging studies, and careful evaluation of model-based methods is required for each radiotracer...
  41. ncbi NMDA antagonist effects on striatal dopamine release: positron emission tomography studies in humans
    Lawrence S Kegeles
    Department of Psychiatry, Columbia University College of Physicians and Surgeons and the New York State Psychiatric Institute, New York, NY 10032, USA
    Synapse 43:19-29. 2002
    ....
  42. ncbi The effect of early trauma exposure on serotonin type 1B receptor expression revealed by reduced selective radioligand binding
    James W Murrough
    Mood and Anxiety Disorders Program, Department of Psychiatry, Mount Sinai School of Medicine, One Gustave L Levy Place, New York, USA
    Arch Gen Psychiatry 68:892-900. 2011
    ..However, the specific role of the serotonin type 1B receptor has not been studied in patients with PTSD...
  43. ncbi Effect of a triallelic functional polymorphism of the serotonin-transporter-linked promoter region on expression of serotonin transporter in the human brain
    Ramin V Parsey
    Department of Psychiatry, Columbia University College of Physicians and Surgeons, New York, USA
    Am J Psychiatry 163:48-51. 2006
    ....
  44. ncbi Positron emission tomography shows elevated cannabinoid CB (1) receptor binding in men with alcohol dependence
    Alexander Neumeister
    Molecular Imaging Program, Department of Psychiatry and Radiology, New York University School of Medicine, New York, New York 10016, USA
    Alcohol Clin Exp Res 36:2104-9. 2012
    ..This is an important gap in the literature, because recent therapeutic developments suggest that these receptors could be targeted for the treatment for AD...
  45. ncbi Decreased hippocampal 5-HT2A receptor binding in major depressive disorder: in vivo measurement with [18F]altanserin positron emission tomography
    Mark A Mintun
    Department of Radiology, Mallinckrodt Institute of Radiology, Box 8225, Washington University School of Medicine, 510 South Kingshighway Boulevard, St Louis, MO 63110, USA
    Biol Psychiatry 55:217-24. 2004
    ..Postmortem and positron emission tomography studies have reported both increased and decreased 5-HT(2A) receptor binding in different limbic and paralimbic regions...

Research Grants1

  1. New PET radioligand for the serotonin transporter
    Yiyun Huang; Fiscal Year: 2007
    ..Introduction of [18F]AFM would constitute the first PET tracer for the SERT that can be prepared in a central facility and distributed to various sites for clinical imaging purposes. ..