5-Iodo-A-85380, an α4β2 Subtype-Selective Ligand for Nicotinic Acetylcholine Receptors

Mukhin, Alexey G., Gündisch, Daniela, Horti, Andrew G., Koren, Andrei O., Tamagnan, Gilles, Kimes, Alane S., Chambers, Joann, Vaupel, D. Bruce +4 more·2000·Molecular Pharmacology
DOI 10.1124/mol.57.3.642

Cited by (181)

Items 101–181 of 181

  1. Modeling Differential Binding of α4β2 Nicotinic Acetylcholine Receptor with Agonists and Antagonists
    Xiaoqin Huang, Fang Zheng, Chang‐Guo Zhan · 2008 · Journal of the American Chemical Society
  2. Regulation of glutamate release by heteromeric nicotinic receptors in layer V of the secondary motor region (Fr2) in the dorsomedial shoulder of prefrontal cortex in mouse
    Patrizia Aracri, Alida Amadeo, Maria Enrica Pasini, Umberto Fascio, Andrea Becchetti · 2013 · Synapse
  3. In vivo imaging of Α7 nicotinic receptors as a novel method to monitor neuroinflammation after cerebral ischemia
    Lorena Colás, Marı́a Domercq, Pedro Ramos‐Cabrer, Ana Palma, Vanessa Gómez‐Vallejo, Daniel Padró, Sandra Plaza‐García, Krishna Reddy Pulagam, Makoto Higuchi, Carlos Matute et al. · 2018 · Glia
  4. 5-123I-A-85380 binding to the α4β2-nicotinic receptor in mild cognitive impairment
    Emma Terrière, Mary Frances Dempsey, Lucie L. Herrmann, Kevin M. Tierney, Jane A. Lonie, Ronan E. O’Carroll, Sally L. Pimlott, David J. Wyper, Karl Herholz, Klaus P. Ebmeier · 2008 · Neurobiology of Aging
  5. 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, Santosh S. Kulkarni, Olga Andreyevna Pavlova, Andrei O. Koren, Alexey G. Mukhin, Amy Hauck Newman, Andrew G. Horti · 2002 · Journal of Medicinal Chemistry
  6. Influence of acetylcholine levels on the binding of a SPECT nicotinic acetylcholine receptor ligand [<sup>123</sup>I]5‐I‐A‐85380
    Fujita, Masahiro, Al‐Tikriti, Mohammed S., Tamagnan, Gilles, Zoghbi, Sami S., Bozkurt, Ali, Baldwin, Ronald M., Innis, Robert B. · 2003 · Synapse
  7. Self-administration of 5-iodo-A-85380, a β2-selective nicotinic receptor ligand, by operantly trained rats
    Xiu Liu, Andrei O. Koren, Susan K. Yee, Robert N. Pechnick, Russell E. Poland, Edythe D. London · 2003 · Neuroreport
  8. In vitro evaluation of nicotinic acetylcholine receptors with 2-[18F]F-A85380 in Parkinson's disease
    Jörn Schmaljohann, Daniela Gündisch, Martina Minnerop, Jan A. Bucerius, Alexius Joe, Michael J. Reinhardt, Stefan Guhlke, Hans‐Jürgen Biersack, Ullrich Wüllner · 2006 · Nuclear Medicine and Biology
  9. Paeoniflorin has anti-inflammation and neurogenesis functions through nicotinic acetylcholine receptors in cerebral ischemia-reperfusion injury rats.
    Cheng-Hang Ko, Chun-Ping Huang, Yi‐Wen Lin, Ching‐Liang Hsieh · 2018 · Europe PMC (PubMed Central)
  10. Nicotinic acetylcholine receptors expressed in the ventralposterolateral thalamic nucleus play an important role in anti‐allodynic effects
    Masashi Ueda, Y Iida, Akiko Tominaga, T Yoneyama, Mikako Ogawa, Yasuhiro Magata, Hiroshi Nishimura, Yugi Kuge, Hideo Saji · 2010 · British Journal of Pharmacology
  11. In vitro characterization of 6-[18F]fluoro-A-85380, a high-affinity ligand for α4β2* nicotinic acetylcholine receptors
    Daniela Gündisch, Andrei O. Koren, Andrew G. Horti, Olga Andreyevna Pavlova, Alane S. Kimes, Alexey G. Mukhin, Edythe D. London · 2004 · Synapse
  12. Evaluation of the sensitivity of the novel α4β2* nicotinic acetylcholine receptor PET radioligand 18 F‐(‐)‐NCFHEB to increases in synaptic acetylcholine levels in rhesus monkeys
    Jean‐Dominique Gallezot, Irina Esterlis, Frederic Bois, Ming‐Qiang Zheng, Shu-fei Lin, Tracy Kloczynski, John Harrison Krystal, Yiyun Henry Huang, Osama Sabri, Richard E. Carson et al. · 2014 · Synapse
  13. Single photon emission computed tomography experience with (S)‐5‐[123I]iodo‐3‐(2‐azetidinylmethoxy)pyridine in the living human brain of smokers and nonsmokers
    James Robert Brašić, Yun Zhou, John L. Musachio, John Hilton, Hong Song Fan, Andrew H. Crabb, Christopher J. Endres, Melvin J. Reinhardt, Ahmet Semih DOĞAN, Mohab Alexander et al. · 2009 · Synapse
  14. Measurement of the α4β2* nicotinic acetylcholine receptor ligand 2-[18F]Fluoro-A-85380 and its metabolites in human blood during PET investigation: a methodological study
    Dietlind Sorger, Georg Becker, Marianne Patt, Andreas Schildan, Udo Großmann, Reinhard Schliebs, Anita Seese, Kai Kendziorra, Magnus Kluge, Peter Brust et al. · 2007 · Nuclear Medicine and Biology
  15. Whole-body radiation dosimetry of 2-[18F]Fluoro-A-85380 in human PET imaging studies
    Sebastian L. Obrzut, Andrei O. Koren, Mark A. Mandelkern, Arthur L. Brody, Carl K. Hoh, Edythe D. London · 2005 · Nuclear Medicine and Biology
  16. The 3,7-diazabicyclo[3.3.1]nonane scaffold for subtype selective nicotinic acetylcholine receptor ligands. Part 2: Carboxamide derivatives with different spacer motifs
    Christoph Eibl, Lenka Munoz, Isabelle Tomassoli, Clare A. Stokes, Roger L. Papke, Daniela Gündisch · 2013 · Bioorganic & Medicinal Chemistry
  17. Beta Amyloid Differently Modulate Nicotinic and Muscarinic Receptor Subtypes which Stimulate in vitro and in vivo the Release of Glycine in the Rat Hippocampus
    Stefania Zappettini, Massimo Grilli, Guendalina Olivero, Elisa Mura, Stefania Preda, Stefano M. Govoni, Alessia Salamone, Mario Marchi · 2012 · Frontiers in Pharmacology
  18. Effects of Nicotinic Acetylcholine Receptor Agonists in Assays of Acute Pain-Stimulated and Pain-Depressed Behaviors in Rats
    Kelen Freitas, F. Ivy Carroll, Sidney Stevens Negus · 2015 · Journal of Pharmacology and Experimental Therapeutics
  19. Synthesis and evaluation of [125I]I-TSA as a brain nicotinic acetylcholine receptor α7 subtype imaging agent
    Mikako Ogawa, Ryo Tatsumi, Masakazu Fujio, Jiro Katayama, Yasuhiro Magata · 2006 · Nuclear Medicine and Biology
  20. Synthesis of a new precursor to the nicotinic receptor tracer 5-IA-85380 precursor using trimethylsilyl iodide as deblocking agent
    Eric Brenner, Ronald M. Baldwin, Gilles D. Tamagnan · 2004 · Tetrahedron Letters
  21. 18F-ZW-104: A New Radioligand for Imaging Neuronal Nicotinic Acetylcholine Receptors—In Vitro Binding Properties and PET Studies in Baboons
    Héric Valette, Yingxiang Xiao, Marie‐Anne Peyronneau, Annelaure Damont, Alan P. Kozikowski, Zhi-Liang Wei, Michael Kassiou, Kenneth J. Kellar, Frédéric Dollé, Michel Bottlaender · 2009 · Journal of Nuclear Medicine
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  23. Comparison of effects produced by nicotine and the α4β2-selective agonist 5-I-A-85380 on intracranial self-stimulation in rats.
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  24. Decreased α4β2 nicotinic receptor number in the absence of mRNA changes suggests post‐transcriptional regulation in the spontaneously hypertensive rat model of ADHD
    Mattis B. Wigestrand, Yann S. Mineur, Christopher J. Heath, Frode Fonnum, Marina R. Picciotto, Sven Ivar Walaas · 2011 · Journal of Neurochemistry
  25. α4β2-Nicotinic Receptor Binding with 5-IA in Alzheimer’s Disease: Methods of Scan Analysis
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  26. Synthesis and evaluation of phenylcarbamate derivatives as ligands for nicotinic acetylcholine receptors
    Daniela Gündisch, Matthias Andrä, Lenka Munoz, Maria Cristina Tilotta · 2004 · Bioorganic & Medicinal Chemistry
  27. Synthesis of novel halo-oxybispyridines, new building blocks in cholinergic medicinal chemistry
    Anne Sophie Voisin‐Chiret, Alexandre Bouillon, Jean‐Charles Lancelot, Aurélien Lesnard, Sylvain Rault · 2006 · Tetrahedron
  28. Pharmacological Differences Between Rat Frontal Cortex and Hippocampus in the Nicotinic Modulation of Noradrenaline Release Implicate Distinct Receptor Subtypes
    Alexandra Kennett, David J. Heal, Susan Wonnacott · 2012 · Nicotine & Tobacco Research
  29. Inhibitory effects of beta-amyloid on the nicotinic receptors which stimulate glutamate release in rat hippocampus: the glial contribution
    Alessia Salamone, Elisa Mura, Stefania Zappettini, Massimo Grilli, Guendalina Olivero, Stefania Preda, Stefano M. Govoni, Mario Marchi · 2013 · European Journal of Pharmacology
  30. Synthesis and evaluation of N1-alkylindole-3-ylalkylammonium compounds as nicotinic acetylcholine receptor ligands
    Edwin G. Pérez, Bruce K. Cassels, Christoph Eibl, Daniela Gündisch · 2012 · Bioorganic & Medicinal Chemistry
  31. 5-Iodo-A-85380, a specific ligand for α4β2 nicotinic acetylcholine receptors, prevents glutamate neurotoxicity in rat cortical cultured neurons
    Masashi Ueda, Yasuhiko Iida, Youji Kitamura, Hidekazu Kawashima, Mikako Ogawa, Yasuhiro Magata, Hideo Saji · 2008 · Brain Research
  32. Altered release and uptake of gamma-aminobutyric acid in the cerebellum of dystrophin-deficient mice
    Jânyerson Dannys Pereira da Silva, Diego Vannucci Campos, Fabiana Moreira Nogueira-Bechara, Roberta Sessa Stilhano, Sang Won Han, Rita Sinigaglia‐Coimbra, Maria Teresa R. Lima‐Landman, Antônio José Lapa, Caden Souccar · 2018 · Neurochemistry International
  33. [ 125/123 I] 5-Iodo-3-pyridyl ethers
    Hong Song Fan, Ursula Scheffel, Paige A. Rauseo, Yingxian Xiao, A.Semih Dogan, Fuji Yokoi, John Hilton, Kenneth J. Kellar, Dean Foster Wong, John L. Musachio · 2001 · Nuclear Medicine and Biology
  34. 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 L. Brown, Svetlana I. Chefer, Olga Andreyevna Pavlova, D. Bruce Vaupel, Andrei O. Koren, Alane S. Kimes, Andrew G. Horti, Alexey G. Mukhin · 2004 · Journal of Neurochemistry
  35. The 3,7-diazabicyclo[3.3.1]nonane scaffold for subtype selective nicotinic acetylcholine receptor (nAChR) ligands. Part 1: The influence of different hydrogen bond acceptor systems on alkyl and (hetero)aryl substituents
    Christoph Eibl, Isabelle Tomassoli, Lenka Munoz, Clare A. Stokes, Roger L. Papke, Daniela Gündisch · 2013 · Bioorganic & Medicinal Chemistry
  36. Radiotracer development in psychiatry
    Sally L. Pimlott · 2005 · Nuclear Medicine Communications
  37. Pharmacology, toxicology, and radiation dosimetry evaluation of [123I]5‐I‐A‐85380, a radioligand for in vivo imaging of cerebral neuronal nicotinic acetylcholine receptors in humans
    D. Bruce Vaupel, Srihari R. Tella, David L. Huso, Alexey G. Mukhin, Ira Baum, Valentine O. Wagner, Andrew G. Horti, Edythe D. London, Andrei O. Koren, Alane S. Kimes · 2003 · Drug Development Research
  38. Monkey Adrenal Chromaffin Cells Express α6β4* Nicotinic Acetylcholine Receptors
    Alicia Hernández‐Vivanco, Arik J. Hone, Mick'l Scadden, Beatriz Carmona‐Hidalgo, J. Michael McIntosh, Almudena Albillos · 2014 · PLoS ONE
  39. Differential expression of the beta4 neuronal nicotinic receptor subunit affects tolerance development and nicotinic binding sites following chronic nicotine treatment
    Erin E. Meyers, Esteban C. Loetz, Michael J. Marks · 2015 · Pharmacology Biochemistry and Behavior
  40. Medicinal Chemistry of α4β2 Nicotinic Cholinergic Receptor Ligands
    Richard A. Glennon · 2004 · Progress in medicinal chemistry
  41. Decreased vesicular acetylcholine transporter and α4β2 nicotinic receptor density in the rat brain following 192 IgG-saporin immunolesioning
    Mitchell Quinlivan, Sylvie Chalon, Jackie Vergote, J. M. Henderson, Andrew G. Katsifis, Michael Kassiou, Denis Guilloteau · 2007 · Neuroscience Letters
  42. Design, Synthesis, and Preliminary Pharmacological Evaluation of New Quinoline Derivatives as Nicotinic Ligands
    Luca Guandalini, Monica Norcini, Katia Varani, Marco Pistolozzi, Cecilia Gotti, Carla Bazzicalupi, Elisabetta Martini, Silvia Dei, Dina Manetti, Serena Scapecchi et al. · 2007 · Journal of Medicinal Chemistry
  43. Quantitative Molecular Imaging of Neuronal Nicotinic Acetylcholine Receptors in the Human Brain with A-85380 Radiotracers
    Shahrdad Lotfipour, Mark A. Mandelkern, Arthur L. Brody · 2011 · Current Medical Imaging Formerly Current Medical Imaging Reviews
  44. Selective recovery of striatal 125I-α-conotoxinmii nicotinic receptors after nigrostriatal damage in monkeys
    Albert Lai, Jocelyn Sum, H Fan, J. Michael McIntosh, Maryka Quik · 2004 · Neuroscience
  45. Involvement of Nicotinic Receptor Subtypes in the Behavioral Effects of Nicotinic Drugs in Squirrel Monkeys
    Sarah Louise Withey, Michelle R. Doyle, Jack Bergman, Rajeev I. Desai · 2018 · Journal of Pharmacology and Experimental Therapeutics
  46. NIDA522131, a new radioligand for imaging extrathalamic nicotinic acetylcholine receptors: in vitro and in vivo evaluation
    Svetlana I. Chefer, Olga A. Pavlova, Yi Zhang, D. Bruce Vaupel, Alane S. Kimes, Andrew G. Horti, Elliot A. Stein, Alexey G. Mukhin · 2007 · Journal of Neurochemistry
  47. Radiosynthesis of 5-(2-(4-pyridinyl)vinyl)-6-chloro-3-(1-[11C]methyl-2-(S)-pyrrolidinylmethoxy)pyridine, a high affinity ligand for studying nicotinic acetylcholine receptors by positron emission tomography
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  48. [18F]ZW‐104, a new radioligand for imaging α2‐α3‐α4/β2 central nicotinic acetylcholine receptors: Evaluation in mutant mice
    Wadad Saba, Héric Valette, Sylvie Granon, Yingxian Xiao, Kenneth J. Kellar, Frédéric Dollé, Michel Bottlaender · 2010 · Synapse
  49. Human [/sup 123/I]5-I-A-85380 dynamic SPECT studies in normals: kinetic analysis and parametric imaging
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  50. In vivo relationship between thalamic nicotinic acetylcholine receptor occupancy rates and antiallodynic effects in a rat model of neuropathic pain: Persistent agonist binding inhibits the expression of antiallodynic effects
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    Baldwin, Ronald M., Zoghbi, Sami S., Staley, Julie K., Brenner, Eric, Al-Tikriti, Mohammed S., Amici, Louis, Fujita, Masahiro, Innis, Robert B., Tamagnan, Gilles · 2006 · Nuclear Medicine and Biology
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    Dongyuan Zhang, Hanyuan Zheng, Kun Cui, Yawen Li, Chang Liu, Jian Mao, Jie Zheng, You Wan · 2026 · European Journal of Medicinal Chemistry
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    Mario Marchi, Stefania Zappettini, Guendalina Olivero, Anna Pittaluga, Massimo Grilli · 2012 · Neurochemistry International
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  75. BindingDB Entry 50012106: 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.
    BindingDB · 2009 · UC San Diego
  76. BindingDB Entry 50043624: The 3,7-diazabicyclo[3.3.1]nonane scaffold for subtype selective nicotinic acetylcholine receptor (nAChR) ligands. Part 1: the influence of different hydrogen bond acceptor systems on alkyl and (hetero)aryl substituents.
    BindingDB · 2014 · UC San Diego
  77. BindingDB Entry 50021185: Design, synthesis, and preliminary pharmacological evaluation of new quinoline derivatives as nicotinic ligands.
    BindingDB · 2009 · UC San Diego
  78. BindingDB Entry 50003666: 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 probes for imaging with positron emission tomog
    BindingDB · 2020 · UC San Diego
  79. BindingDB Entry 5433: Carbamoylcholine homologs: novel and potent agonists at neuronal nicotinic acetylcholine receptors.
    BindingDB · 2012 · UC San Diego
  80. BindingDB Entry 50005811: The 3,7-diazabicyclo[3.3.1]nonane scaffold for subtype selective nicotinic acetylcholine receptor ligands. Part 2: carboxamide derivatives with different spacer motifs.
    BindingDB · 2020 · UC San Diego
  81. BindingDB Entry 50037112: Synthesis and nicotinic binding studies on enantiopure diazine analogues of the novel (2-chloro-5-pyridyl)-9-azabicyclo[4.2.1]non-2-ene UB-165.
    BindingDB · 2012 · UC San Diego