Andrew G Horti

Summary

Affiliation: Johns Hopkins University
Country: USA

Publications

  1. ncbi request reprint Synthesis and structure-activity relationship of a novel series of aminoalkylindoles with potential for imaging the neuronal cannabinoid receptor by positron emission tomography
    Peter G Willis
    Neuroimaging Research Branch, Intramural Research Program, National Institute on Drug Abuse, NIH, DHHS, 5500 Nathan Shock Drive, Baltimore, Maryland 21224, USA
    J Med Chem 48:5813-22. 2005
  2. ncbi request reprint 11C-JHU75528: a radiotracer for PET imaging of CB1 cannabinoid receptors
    Andrew G Horti
    Department of Radiology, Johns Hopkins Medical Institutions, Baltimore, Maryland 21287 0816, USA
    J Nucl Med 47:1689-96. 2006
  3. pmc Synthesis and biodistribution of [11C]A-836339, a new potential radioligand for PET imaging of cannabinoid type 2 receptors (CB2)
    Andrew G Horti
    Division of Nuclear Medicine, Department of Radiology, Johns Hopkins Medical Institutions, 600 North Wolfe Street, Baltimore, MD 21287 0816, USA
    Bioorg Med Chem 18:5202-7. 2010
  4. pmc Synthesis and evaluation of new radioligands [(11)C]A-833834 and [(11)C]A-752274 for positron-emission tomography of α7-nicotinic acetylcholine receptors
    Andrew G Horti
    Division of Nuclear Medicine, Department of Radiology, Johns Hopkins School of Medicine, Baltimore, MD 21205, USA
    Nucl Med Biol 40:395-402. 2013
  5. ncbi request reprint Development of radioligands for in vivo imaging of type 1 cannabinoid receptors (CB1) in human brain
    Andrew G Horti
    PET Center, Division of Nuclear Medicine, Radiology, Johns Hopkins Medicine, Nelson B1 122, 600 North Wolfe Street, Baltimore, MD 21287 0816, USA
    Curr Pharm Des 14:3363-83. 2008
  6. ncbi request reprint The quest for Eldorado: development of radioligands for in vivo imaging of nicotinic acetylcholine receptors in human brain
    Andrew G Horti
    Division of Nuclear Medicine, Department of Radiology, Johns Hopkins Medicine, Baltimore, MD USA
    Curr Pharm Des 12:3877-900. 2006
  7. pmc Development of radioligands with optimized imaging properties for quantification of nicotinic acetylcholine receptors by positron emission tomography
    Andrew G Horti
    Division of Nuclear Medicine, Department of Radiology, Johns Hopkins University, Baltimore, Maryland, United States
    Life Sci 86:575-84. 2010
  8. ncbi request reprint Derivatives of (-)-7-methyl-2-(5-(pyridinyl)pyridin-3-yl)-7-azabicyclo[2.2.1]heptane are potential ligands for positron emission tomography imaging of extrathalamic nicotinic acetylcholine receptors
    Yongjun Gao
    Division of Nuclear Medicine, Department of Radiology, The Johns Hopkins University School of Medicine, 600 North Wolfe Street, Baltimore, MD 21287 0816, USA
    J Med Chem 50:3814-24. 2007
  9. pmc Synthesis and biological evaluation of novel carbon-11 labeled pyridyl ethers: candidate ligands for in vivo imaging of alpha4beta2 nicotinic acetylcholine receptors (alpha4beta2-nAChRs) in the brain with positron emission tomography
    Yongjun Gao
    Department of Radiology, Division of Nuclear Medicine, PET Center, The Johns Hopkins University School of Medicine, Baltimore, MD 21287 0816, USA
    Bioorg Med Chem 17:4367-77. 2009
  10. ncbi request reprint 5-substituted derivatives of 6-halogeno-3-((2-(S)-azetidinyl)methoxy)pyridine and 6-halogeno-3-((2-(S)-pyrrolidinyl)methoxy)pyridine with low picomolar affinity for alpha4beta2 nicotinic acetylcholine receptor and wide range of lipophilicity: potential pr
    Yi Zhang
    Neuroimaging Research Branch, Intramural Research Program, National Institute on Drug Abuse, NIH, DHHS, 5500 Nathan Shock Drive, Baltimore, Maryland 21224, USA
    J Med Chem 47:2453-65. 2004

Collaborators

Detail Information

Publications35

  1. ncbi request reprint Synthesis and structure-activity relationship of a novel series of aminoalkylindoles with potential for imaging the neuronal cannabinoid receptor by positron emission tomography
    Peter G Willis
    Neuroimaging Research Branch, Intramural Research Program, National Institute on Drug Abuse, NIH, DHHS, 5500 Nathan Shock Drive, Baltimore, Maryland 21224, USA
    J Med Chem 48:5813-22. 2005
    ..A pretreatement study for the other enantiomer found no displaceable radioactivity in the same group of mice; this result suggested the enantiomer was inactive...
  2. ncbi request reprint 11C-JHU75528: a radiotracer for PET imaging of CB1 cannabinoid receptors
    Andrew G Horti
    Department of Radiology, Johns Hopkins Medical Institutions, Baltimore, Maryland 21287 0816, USA
    J Nucl Med 47:1689-96. 2006
    ..The goal of this study was to evaluate 11C-JHU75528, an analog of the selective CB1 antagonist rimonabant, in vivo as a potential CB1 radioligand for PET...
  3. pmc Synthesis and biodistribution of [11C]A-836339, a new potential radioligand for PET imaging of cannabinoid type 2 receptors (CB2)
    Andrew G Horti
    Division of Nuclear Medicine, Department of Radiology, Johns Hopkins Medical Institutions, 600 North Wolfe Street, Baltimore, MD 21287 0816, USA
    Bioorg Med Chem 18:5202-7. 2010
    ..These data establish a proof of principle that CB2 receptors binding in the neuroinflammation and related disorders can be measured in vivo...
  4. pmc Synthesis and evaluation of new radioligands [(11)C]A-833834 and [(11)C]A-752274 for positron-emission tomography of α7-nicotinic acetylcholine receptors
    Andrew G Horti
    Division of Nuclear Medicine, Department of Radiology, Johns Hopkins School of Medicine, Baltimore, MD 21205, USA
    Nucl Med Biol 40:395-402. 2013
    ..7-nAChR is involved in variety of neuronal processes and disorders including schizophrenia and Alzheimer's disease. A number of α7-nAChR PET radioligands have been developed, but a quality radiotracer remains to be discovered...
  5. ncbi request reprint Development of radioligands for in vivo imaging of type 1 cannabinoid receptors (CB1) in human brain
    Andrew G Horti
    PET Center, Division of Nuclear Medicine, Radiology, Johns Hopkins Medicine, Nelson B1 122, 600 North Wolfe Street, Baltimore, MD 21287 0816, USA
    Curr Pharm Des 14:3363-83. 2008
    ..Current research efforts on the development of CB1 radioligands with higher binding potential, greater brain uptake and more optimal brain kinetics...
  6. ncbi request reprint The quest for Eldorado: development of radioligands for in vivo imaging of nicotinic acetylcholine receptors in human brain
    Andrew G Horti
    Division of Nuclear Medicine, Department of Radiology, Johns Hopkins Medicine, Baltimore, MD USA
    Curr Pharm Des 12:3877-900. 2006
    ..In particular, new PET nAChR radioligands will be examined that either present faster brain kinetics allowing simple and reliable quantification approaches or higher binding potentials suitable for the evaluation of extrathalamic nAChR...
  7. pmc Development of radioligands with optimized imaging properties for quantification of nicotinic acetylcholine receptors by positron emission tomography
    Andrew G Horti
    Division of Nuclear Medicine, Department of Radiology, Johns Hopkins University, Baltimore, Maryland, United States
    Life Sci 86:575-84. 2010
    ..Central nAChRs also contribute to a variety of brain functions, including cognition, behavior and memory...
  8. ncbi request reprint Derivatives of (-)-7-methyl-2-(5-(pyridinyl)pyridin-3-yl)-7-azabicyclo[2.2.1]heptane are potential ligands for positron emission tomography imaging of extrathalamic nicotinic acetylcholine receptors
    Yongjun Gao
    Division of Nuclear Medicine, Department of Radiology, The Johns Hopkins University School of Medicine, 600 North Wolfe Street, Baltimore, MD 21287 0816, USA
    J Med Chem 50:3814-24. 2007
    ..2.1]heptane, exhibited good properties as a first practical PET radioligand for imaging of extrathalamic nAChR in baboon brain and holds promise for further investigation for human studies...
  9. pmc Synthesis and biological evaluation of novel carbon-11 labeled pyridyl ethers: candidate ligands for in vivo imaging of alpha4beta2 nicotinic acetylcholine receptors (alpha4beta2-nAChRs) in the brain with positron emission tomography
    Yongjun Gao
    Department of Radiology, Division of Nuclear Medicine, PET Center, The Johns Hopkins University School of Medicine, Baltimore, MD 21287 0816, USA
    Bioorg Med Chem 17:4367-77. 2009
    ..Three of these novel nAChR ligands were radiolabeled with the positron-emitting isotope (11)C and evaluated in animal studies as potential PET radiotracers for imaging of cerebral nAChRs with improved brain kinetics...
  10. ncbi request reprint 5-substituted derivatives of 6-halogeno-3-((2-(S)-azetidinyl)methoxy)pyridine and 6-halogeno-3-((2-(S)-pyrrolidinyl)methoxy)pyridine with low picomolar affinity for alpha4beta2 nicotinic acetylcholine receptor and wide range of lipophilicity: potential pr
    Yi Zhang
    Neuroimaging Research Branch, Intramural Research Program, National Institute on Drug Abuse, NIH, DHHS, 5500 Nathan Shock Drive, Baltimore, Maryland 21224, USA
    J Med Chem 47:2453-65. 2004
    ..2.5 times those of 2-[(18)F]FA. Therefore, [(18)F]35 and several other members of the series, when radiolabeled, will be suitable for quantitative imaging of extrathalamic nAChRs...
  11. ncbi request reprint New synthesis and evaluation of enantiomers of 7-methyl-2-exo-(3'-iodo-5'-pyridinyl)-7-azabicyclo[2.2.1]heptane as stereoselective ligands for PET imaging of nicotinic acetylcholine receptors
    Yongjun Gao
    Division of Nuclear Medicine, Department of Radiology, The Johns Hopkins University School of Medicine, 600 North Wolfe Street, Baltimore, MD 21287 0816, USA
    Bioorg Med Chem Lett 18:6168-70. 2008
    ..In the baboon PET study [(11)C](-)-NMI-EPB did not reach steady-state within 90 min post-injection suggesting that the radioligand may have some limitations for quantitative imaging...
  12. ncbi request reprint NIDA522131, a new radioligand for imaging extrathalamic nicotinic acetylcholine receptors: in vitro and in vivo evaluation
    Svetlana I Chefer
    Neuroimaging Research Branch, Intramural Research Program, National Institute on Drug Abuse, National Institute of Health, Department of Health and Human Services, Baltimore, Maryland, USA
    J Neurochem 104:306-15. 2008
    ..These results suggest that [(18)F]NIDA522131 is a promising positron emission tomography radioligand for studying extrathalamic nAChR in humans...
  13. pmc Analogs of JHU75528, a PET ligand for imaging of cerebral cannabinoid receptors (CB1): development of ligands with optimized lipophilicity and binding affinity
    Hong Fan
    PET Center, Division of Nuclear Medicine, Department of Radiology, Johns Hopkins University School of Medicine, Baltimore, MD 21287, USA
    Eur J Med Chem 44:593-608. 2009
    ..Molecular modeling analysis revealed an important role of the binding of the cyano group with the CB1 binding pocket...
  14. doi request reprint PET Imaging of nicotinic acetylcholine receptors in baboons with 18F-AZAN, a radioligand with improved brain kinetics
    Hiroto Kuwabara
    Division of Nuclear Medicine, Department of Radiology, Johns Hopkins School of Medicine, Baltimore, Maryland 21287 0816, USA
    J Nucl Med 53:121-9. 2012
    ..2.1]heptane ((18)F-AZAN), our new radiolabeled antagonist of α4β2-nAChRs, that has high binding potential and rapid brain kinetics in baboons...
  15. ncbi request reprint Discovery of (-)-7-methyl-2-exo-[3'-(6-[18F]fluoropyridin-2-yl)-5'-pyridinyl]-7-azabicyclo[2.2.1]heptane, a radiolabeled antagonist for cerebral nicotinic acetylcholine receptor (alpha4beta2-nAChR) with optimal positron emission tomography imaging propert
    Yongjun Gao
    Department of Radiology, Division of Nuclear Medicine, The Johns Hopkins University School of Medicine, 600 North Wolfe Street, Baltimore, Maryland 21287 0816, USA
    J Med Chem 51:4751-64. 2008
    ..This combination of imaging properties suggests that [(18)F]-(-)- 6c is a potentially superior replacement for 2-[(18)F]fluoro-A-85380 and 6-[(18)F]fluoro-A-85380, the only available nAChR PET radioligands for humans...
  16. pmc 5-(5-(6-[(11)C]methyl-3,6-diazabicyclo[3.2.0]heptan-3-yl)pyridin-2-yl)-1H-indole as a potential PET radioligand for imaging cerebral α7-nAChR in mice
    Yongjun Gao
    Division of Nuclear Medicine, Department of Radiology, The Johns Hopkins University School of Medicine, 600 North Wolfe Street, Baltimore, MD 21287 0816, USA
    Bioorg Med Chem 20:3698-702. 2012
    ..The total synthesis time was 30 min from end-of-bombardment. Biodistribution studies in mice showed that [(11)C]rac-1 penetrates the blood-brain barrier and specifically labels neuronal α7-nAChRs...
  17. ncbi request reprint Evaluation of 5-(2-(4-pyridinyl)vinyl)-6-chloro-3-(1-methyl-2-(S)-pyrrolidinylmethoxy)pyridine and its analogues as PET radioligands for imaging nicotinic acetylcholine receptors
    LaVerne Brown
    Intramural Research Program, National Institute on Drug Abuse, Baltimore, Maryland 21224, USA
    J Neurochem 91:600-12. 2004
    ..Taken together, these results suggest that [(11)C]Me-p-PVC is a promising PET radioligand for studying nAChR occupancy by endogenous and exogenous ligands in the brain in vivo...
  18. ncbi request reprint In vitro characterization of 6-[18F]fluoro-A-85380, a high-affinity ligand for alpha4beta2* nicotinic acetylcholine receptors
    Daniela Gündisch
    Neuroimaging Research Branch, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, DHHS, Baltimore, Maryland 21224, USA
    Synapse 55:89-97. 2005
    ..These results suggest that 6-[18F]fluoro-A-85380 is a promising radioligand for in vivo imaging of brain alpha4beta2* nicotinic receptors...
  19. pmc Greater nicotinic acetylcholine receptor density in smokers than in nonsmokers: a PET study with 2-18F-FA-85380
    Alexey G Mukhin
    National Institute on Drug Abuse Intramural Research Program, National Institutes of Health, Department of Health and Human Services, Baltimore, Maryland, USA
    J Nucl Med 49:1628-35. 2008
    ..Quantitative PET imaging of nAChRs in humans has recently been reported using the alpha4beta2* subtype-specific radioligand 2-(18)F-FA-85380 (2FA)...
  20. ncbi request reprint 18F-ASEM, a radiolabeled antagonist for imaging the α7-nicotinic acetylcholine receptor with PET
    Andrew G Horti
    Department of Radiology, Johns Hopkins School of Medicine, Baltimore, Maryland
    J Nucl Med 55:672-7. 2014
    ..The goal of this study was to evaluate the potential of (18)F-ASEM ((18)F-JHU82132) as an α7-nAChR radioligand for PET...
  21. ncbi request reprint 6-Chloro-3-(((1-[11C]methyl)-2-(S)-pyrrolidinyl)methoxy)-5-(2-fluoropyridin-4-yl)pyridine ([11C]JHU85270), a potent ligand for nicotinic acetylcholine receptor imaging by positron emission tomography
    Yongjun Gao
    Division of Nuclear Medicine, Department of Radiology, The Johns Hopkins University, School of Medicine, 600 North Wolfe Street, Baltimore, MD 21287 0816, USA
    Appl Radiat Isot 65:947-51. 2007
    ..The average radiochemical yield of [(11)C]JHU85270 was 37%+/-3% (non-decay corrected). The average specific radioactivity was 398+/-165 GBq/micromol (10750+/-4468 mCi/micromol) and the radiochemical purity was greater than 99%...
  22. ncbi request reprint Graphical analysis of 2-[18F]FA binding to nicotinic acetylcholine receptors in rhesus monkey brain
    Svetlana I Chefer
    Neuroimaging Research Branch, Intramural Research Program, National Institute on Drug Abuse, Baltimore, Maryland 21224, USA
    Synapse 48:25-34. 2003
    ..1 nmol/kg body weight. The findings suggest that 2-[(18)F]FA is a promising ligand for quantitation of nAChRs in human brain...
  23. pmc Synthesis and in vivo evaluation of (S)-6-(4-fluorophenoxy)-3-((1-[11C]methylpiperidin-3-yl)methyl)-2-o-tolylquinazolin-4(3H)-one, a potential PET tracer for growth hormone secretagogue receptor (GHSR)
    Rachel Potter
    Division of Nuclear Medicine, Department of Radiology, The Johns Hopkins University School of Medicine, 600 North Wolfe Street, Baltimore, MD 21287 0816, USA
    Bioorg Med Chem 19:2368-72. 2011
    ..Described herein is the synthesis, in vitro, and in vivo evaluation of (S)-6-(4-fluorophenoxy)-3-((1-[(11)C]methylpiperidin-3-yl)methyl)-2-o-tolylquinazolin-4(3H)-one ([(11)C]1), a potential PET radioligand for imaging GHSR...
  24. ncbi request reprint Quantification of cerebral cannabinoid receptors subtype 1 (CB1) in healthy subjects and schizophrenia by the novel PET radioligand [11C]OMAR
    Dean F Wong
    Radiology, Johns Hopkins University, Baltimore, MD 21287, USA
    Neuroimage 52:1505-13. 2010
    ..In addition, our initial data in subjects with schizophrenia seem to suggest an association of elevated binding specific brain regions and symptoms of the disease...
  25. ncbi request reprint Pharmacological and toxicological evaluation of 2-fluoro-3-(2(S)-azetidinylmethoxy)pyridine (2-F-A-85380), a ligand for imaging cerebral nicotinic acetylcholine receptors with positron emission tomography
    D Bruce Vaupel
    NIDA IRP, Neuroimaging Research Branch, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA
    J Pharmacol Exp Ther 312:355-65. 2005
    ..v.) to elevate blood pressure and heart rate by 10% in humans and should elicit no clinically significant effects and have acceptable dosimetry...
  26. ncbi request reprint Recent PET radioligands with optimal brain kinetics for imaging nicotinic acetylcholine receptors
    Andrew G Horti
    Division of Nuclear Medicine, Department of Radiology, Johns Hopkins University, Baltimore, MD, USA
    J Labelled Comp Radiopharm 56:159-66. 2013
    ....
  27. pmc Derivatives of dibenzothiophene for positron emission tomography imaging of α7-nicotinic acetylcholine receptors
    Yongjun Gao
    Russell H Morgan Department of Radiology and Radiological Sciences, Division of Nuclear Medicine, The Johns Hopkins University School of Medicine, 600 North Wolfe Street, Baltimore, Maryland 21287 0816, United States
    J Med Chem 56:7574-89. 2013
    ..Thus, [(18)F]7a displays excellent imaging properties in mice and has been chosen for further evaluation as a potential PET radioligand for imaging of α7-nAChR in non-human primates. ..
  28. ncbi request reprint Synthesis, structure-activity relationship, and evaluation of SR141716 analogues: development of central cannabinoid receptor ligands with lower lipophilicity
    Reeti Katoch-Rouse
    Neuroimaging Research Branch and Cellular Neurophysiology Section, National Institute on Drug Abuse, Intramural Research Program, National Institutes of Health, 5500 Nathan Shock Drive, Baltimore, Maryland 21224, USA
    J Med Chem 46:642-5. 2003
    ..We have synthesized a series of less lipophilic analogues of SR141716 to serve as potential radioligands. Binding affinities of the series and a functional electrophysiological assay of three of our compounds have been presented...
  29. doi request reprint PET imaging of high-affinity α4β2 nicotinic acetylcholine receptors in humans with 18F-AZAN, a radioligand with optimal brain kinetics
    Dean F Wong
    Department of Radiology, School of Medicine, Johns Hopkins University, Baltimore, Maryland, USA
    J Nucl Med 54:1308-14. 2013
    ..2.1]heptane ((18)F-AZAN), a novel radiotracer that binds to α4β2 nicotinic acetylcholine receptors (α4β2-nAChRs) and shows high specific binding and rapid and reversible kinetics in the baboon and human brain...
  30. pmc Positron emission tomography experience with 2-[¹⁸F]fluoro-3-(2(S)-azetidinylmethoxy)pyridine (2-[¹⁸F]FA) in the living human brain of smokers with paranoid schizophrenia
    James Robert Brasic
    Division of Nuclear Medicine, The Russell H Morgan Department of Radiology and Radiological Science, The Johns Hopkins University School of Medicine, Johns Hopkins Outpatient Center, Baltimore, Maryland 21287 0807, USA
    Synapse 66:352-68. 2012
    ..0105) (StataCorp, 2003), which was likely due to occupancy of nAChRs by inhaled nicotine in smokers. Further research is needed to rule out the effects of confounding variables...
  31. ncbi request reprint Estimation of D2-like receptor occupancy by dopamine in the putamen of hemiparkinsonian Monkeys
    Svetlana I Chefer
    Neuroimaging Research Branch, Intramural Research Program, National Institute on Drug Abuse, NIH DHHS, Baltimore, MD, USA
    Neuropsychopharmacology 33:270-8. 2008
    ....
  32. ncbi request reprint Synthesis and evaluation of a novel series of 2-chloro-5-((1-methyl-2-(S)-pyrrolidinyl)methoxy)-3-(2-(4-pyridinyl)vinyl)pyridine analogues as potential positron emission tomography imaging agents for nicotinic acetylcholine receptors
    LaVerne L Brown
    Neuroimaging Research Branch and Medicinal Chemistry Section, Intramural Research Program, National Institute on Drug Abuse, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA
    J Med Chem 45:2841-9. 2002
    ..The N-methyl derivatives 3b and 6b demonstrated very high affinities at nAChRs (K(i) = 28 and 23 pM, respectively) and will be targets for development of (11)CH(3)-labeled derivatives as radiotracers for PET imaging of nAChRs...
  33. ncbi request reprint 2-[18F]F-A-85380: PET imaging of brain nicotinic acetylcholine receptors and whole body distribution in humans
    Alane S Kimes
    NIDA Intramural Research Program Baltimore, Maryland 21224, USA
    FASEB J 17:1331-3. 2003
    ..180 +/- 30 mSv/MBq or 0.7 rem/mCi with a 2.4 h void interval) suggests that multiple studies could be performed in a single subject. The results predict that quantitative PET imaging of nAChRs in human brain with 2-[18F]FA is feasible...
  34. ncbi request reprint Whole-body biodistribution, radiation absorbed dose, and brain SPET imaging with [123i]5-i-A-85380 in healthy human subjects
    Masahiro Fujita
    Department of Psychiatry, Yale University School of Medicine and VA Connecticut Healthcare System, VA Connecticut 116A2, West Haven 06516, USA
    Eur J Nucl Med Mol Imaging 29:183-90. 2002
    ..These results suggest that [123I]5-I-A-85380 is a promising SPET agent to image alpha4beta2 nAChRs in humans, with acceptable dosimetry and high brain uptake...
  35. ncbi request reprint Quantification of nicotinic acetylcholine receptors in human brain using [123I]5-I-A-85380 SPET
    Masahiro Fujita
    Molecular Imaging Branch, National Institute of Mental Health, Bethesda, MD 20892 0135, USA
    Eur J Nucl Med Mol Imaging 30:1620-9. 2003
    ..These results demonstrate the feasibility of quantifying high-affinity type nAChRs using [123I]5-I-A-85380 in humans and support the use of VT' measured by bolus studies...

Research Grants3