Synthesis and evaluation of two positron-labeled nitric oxide synthase inhibitors, S-[11C]methylisothiourea and S-(2-[18F]fluoroethyl)isothiourea, as potential positron emission tomography tracers.

No abstract is available for this paper.

• Publication year

  1996

• Venue

  Journal of Medicinal Chemistry

• Publication date

  1996-12-20

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1021/JM960481QPMID 8978842
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Synthesis and in vivo distribution of no-carrier-added N(omega)-Nitro-L-arginine [11C]methyl ester, a nitric oxide synthase inhibitor.

  1996cited by this paper
• Isothioureas: potent inhibitors of nitric oxide synthases with variable isoform selectivity

  1995cited by this paper
• Lipopolysaccharide-induced hypotension and vascular hyporeactivity in the rat: tissue analysis of nitric oxide synthase mRNA and protein expression in the presence and absence of dexamethasone, NG-monomethyl-L-arginine or indomethacin.

  1995cited by this paper
• Novel potent and selective inhibitors of inducible nitric oxide synthase.

  1995cited by this paper
• Induction of NG-monomethyl-L-arginine uptake: a mechanism for differential inhibition of NO synthases?

  1995cited by this paper
• Nitric oxide: a new paradigm for second messengers.

  1995cited by this paper
• Immunochemical localization of inducible nitric oxide synthase in endotoxin-treated rats.

  1994cited by this paper
• Beneficial effects and improved survival in rodent models of septic shock with S-methylisothiourea sulfate, a potent and selective inhibitor of inducible nitric oxide synthase.

  1994cited by this paper
• Synthesis and tissue biodistribution of [omega-11C]palmitic acid. A novel PET imaging agent for cardiac fatty acid metabolism.

  1994cited by this paper
• Selective targeting of nitric oxide synthase inhibitors to system y+ in activated macrophages.

  1994cited by this paper
• Nitric oxide synthase isozymes. Characterization, purification, molecular cloning, and functions.

  1994cited by this paper
• The arginine‐nitric oxide pathway: A target for new drugs

  1994cited by this paper
• Potent and selective inhibition of human nitric oxide synthases. Inhibition by non-amino acid isothioureas.

  1994cited by this paper
• L-N6-(1-iminoethyl)lysine: a selective inhibitor of inducible nitric oxide synthase.

  1994cited by this paper
• Monocyte chemotactic protein-1 inhibits the induction of nitric oxide synthase in J774 cells.

  1993cited by this paper
• The L-arginine-nitric oxide pathway.

  1993cited by this paper
• Selective inhibition of the inducible nitric oxide synthase by aminoguanidine.

  1993cited by this paper
• Nitric oxide synthase structure and mechanism.

  1993cited by this paper
• Synthesis and in vivo distribution in the rat of several fluorine-18 labeled N-fluoroalkylaporphines.

  1993cited by this paper
• Nitric oxide as a secretory product of mammalian cells

  1992cited by this paper
• NG-allyl- and NG-cyclopropyl-L-arginine: two novel inhibitors of macrophage nitric oxide synthase.

  1992cited by this paper
• Cloning and characterization of inducible nitric oxide synthase from mouse macrophages.

  1992cited by this paper
• Chromosome size-dependent control of meiotic recombination.

  1992cited by this paper
• Purification of a distinctive form of endotoxin-induced nitric oxide synthase from rat liver.

  1992cited by this paper
• Positron-labeled angiotensin-converting enzyme (ACE) inhibitor: fluorine-18-fluorocaptopril. Probing the ACE activity in vivo by positron emission tomography.

  1991cited by this paper
• Dopa decarboxylase activity of the living human brain.

  1991cited by this paper
• Nitric oxide: physiology, pathophysiology, and pharmacology.

  1991cited by this paper
• Differential induction of brain, lung and liver nitric oxide synthase by endotoxin in the rat.

  1990cited by this paper
• Reversal of endotoxin-mediated shock by NG-methyl-L-arginine, an inhibitor of nitric oxide synthesis.

  1990cited by this paper
• Radiochemical synthesis of [18F]fluororaclopride.

  1989cited by this paper
• Mapping human brain monoamine oxidase A and B with 11C-labeled suicide inactivators and PET.

  1987cited by this paper
• Kinetics of [11C]N,N-dimethylphenylethylamine in mice and humans: potential for measurement of brain MAO-B activity.

  1987cited by this paper
• MPTP‐induced up‐regulation of in vivo dopaminergic radioligand‐receptor binding in humans

  1987cited by this paper
• Radioactive N,N‐Dimethylphenylethylamine: A Selective Radiotracer for In Vivo Measurement of Monoamine Oxidase‐B Activity in the Brain

  1985cited by this paper
• An improved [18O]water target for [18F]fluoride production.

  1985cited by this paper
• Comparison in animal models of 18F-spiroperidol and 18F-haloperidol: potential agents for imaging the dopamine receptor.

  1983cited by this paper
• Positron-emission tomography.

  1980cited by this paper
• Measurement of regional cerebral blood volume by emission tomography

  1978cited by this paper
• The circulatory effects of some iso‐thiourea derivatives, with special reference to the sensitization of animals to the pressor action of adrenaline

  1943cited by this paper

• Novel PET Imaging of Inflammatory Targets and Cells for the Diagnosis and Monitoring of Giant Cell Arteritis and Polymyalgia Rheumatica

  2022cites this paper
• Easy S-Alkylation of Arylthioureas and 2-Mercaptobenzothiazoles Using Tetraalkylammonium Salts under Transition-Metal-Free Conditions.

  2022cites this paper
• Automated Synthesis and Initial Evaluation of (4′-Amino-5′,8′-difluoro-1′H-spiro[piperidine-4,2′-quinazolin]-1-yl)(4-[18F]fluorophenyl)methanone for PET/MR Imaging of Inducible Nitric Oxide Synthase

  2021cites this paper
• An Efficient Chan-Lam S -Arylation of Arylthioureas with Arylboronic Acids

  2018cites this paper
• NaH-Promoted Transformation of Arylthioureas to Aryl-Isothioureas by S-Allylation and S-Benzylation Reactions

  2017cites this paper
• Copper-Catalyzed C–S Cross-Coupling Reaction: S-Arylation of Arylthioureas

  2017cites this paper
• Radiopharmaceuticals for PET imaging of neuroinflammation

  2016cites this paper
• Re(I) and Tc(I) Complexes for Targeting Nitric Oxide Synthase: Influence of the Chelator in the Affinity for the Enzyme

  2015cites this paper
• Carbon-11 radiolabelling of organosulfur compounds: (11) C synthesis of the progesterone receptor agonist tanaproget.

  2015cites this paper
• Imaging brain inflammation in epilepsy.

  2014cites this paper
• Synthesis and biological evaluation of positron emission tomography radiotracers targeting serotonin 4 receptors in brain: [18F]MNI-698 and [18F]MNI-699.

  2013cites this paper
• Dual peptide nucleic acid- and peptide-functionalized shell cross-linked nanoparticles designed to target mRNA toward the diagnosis and treatment of acute lung injury.

  2012cites this paper
• Re and Tc Complexes with Pyrazolyl-Containing Chelators: from Coordination Chemistry to Target-Specific Delivery of Radioactivity

  2009cites this paper
• Re and (99m)Tc organometallic complexes containing pendant l-arginine derivatives as potential probes of inducible nitric oxide synthase.

  2009cites this paper
• Design and synthesis of 2-amino-4-methylpyridine analogues as inhibitors for inducible nitric oxide synthase and in vivo evaluation of [18F]6-(2-fluoropropyl)-4-methyl-pyridin-2-amine as a potential PET tracer for inducible nitric oxide synthase.

  2009cites this paper
• Nuclear imaging of neuroinflammation: a comprehensive review of [11C]PK11195 challengers

  2008cites this paper
• [18F]Fluoroalkyl agents: synthesis, reactivity and application for development of PET ligands in molecular imaging.

  2007cites this paper
• Synthesis of (E)-2,3′,4,5′-tetramethoxy[2-11C]stilbene

  2007cites this paper
• Synthesis and biological evaluation of S‐[11C]methylated mercaptoimidazole piperazinyl derivatives as potential radioligands for imaging 5‐HT1A receptors by positron emission tomography (PET)

  2005cites this paper
• Improvement of intestinal motility using S-methylisothiourea in postoperative ileus.

  2004cites this paper
• Determination of lipophilicity and its use as a predictor of blood-brain barrier penetration of molecular imaging agents.

  2003cites this paper
• Versatile solid-phase synthesis of s-arylisothioureas.

  2002cites this paper
• Radiosynthesis, in vitro validation, and in vivo evaluation of 18F-labeled COX-1 and COX-2 inhibitors.

  2002cites this paper
• N-functionalized benzotriazole-1-carboximidoyl chlorides: synthetic equivalents for isocyanide dichlorides.

  2001cites this paper
• Synthesis, (18)F-labeling, and biological evaluation of piperidyl and pyrrolidyl benzilates as in vivo ligands for muscarinic acetylcholine receptors.

  2000cites this paper
• Radiolabeled neuronal nitric oxide synthase inhibitors: synthesis, in vivo evaluation, and primate PET studies.

  2000cites this paper
• Design of isoform-selective inhibitors of nitric oxide synthase.

  1998cites this paper
• Measurement of upregulation of inducible nitric oxide synthase in the experimental autoimmune encephalomyelitis model using a positron emitting radiopharmaceutical.

  1997cites this paper
• Achieving Balanced Resolution in Radiopharmacological Studies: Tc-Labeled BMS 194,796

  1997cites this paper
• Synthesis, in vivo evaluation and PET study of a carbon-11-labeled neuronal nitric oxide synthase (nNOS) inhibitor S-methyl-L-thiocitrulline.

  1997cites this paper