bicyclo compounds

Summary

Top Publications

  1. ncbi Synthesis of polyprenylated acylphloroglucinols using bridgehead lithiation: the total synthesis of racemic clusianone and a formal synthesis of racemic garsubellin A
    Nadia M Ahmad
    School of Chemistry, The University of Nottingham, University Park, Nottingham NG7 2RD, UK
    J Org Chem 72:4803-15. 2007
  2. ncbi Frontal cortical alpha7 and alpha4beta2 nicotinic acetylcholine receptors in working and reference memory
    Wai Kit Chan
    Department of Biological Sciences, National University of Singapore, 14 Science Drive 4, Singapore 117543, Singapore
    Neuropharmacology 52:1641-9. 2007
  3. ncbi Volatile components of peel and leaf oils of lemon and lime species
    Marie Laure Lota
    Université de Corse, Equipe Chimie et Biomasse, UMR CNRS 6134, Route des Sanguinaires, 20000 Ajaccio, France
    J Agric Food Chem 50:796-805. 2002
  4. pmc Activation of the α7 nicotinic ACh receptor induces anxiogenic effects in rats which is blocked by a 5-HT₁a receptor antagonist
    Anshul A Pandya
    Laboratory of Neurobiology, National Institute of Environmental Health Sciences, National Institutes of Health, Department of Health and Human Services, Research Triangle Park, MD F2 08, PO Box 12233, NC 27709, USA
    Neuropharmacology 70:35-42. 2013
  5. pmc Effects of nicotinic acetylcholine receptor agonists on cognition in rhesus monkeys with a chronic cocaine self-administration history
    Robert W Gould
    Department of Physiology and Pharmacology, Wake Forest University School of Medicine, Winston Salem, NC 27157, USA
    Neuropharmacology 64:479-88. 2013
  6. ncbi Behavioral effects of PNU-282987, an alpha7 nicotinic receptor agonist, in mice
    Paloma Vicens
    Department of Psychology, IISPV, Universitat Rovira i Virgili, 43007 Tarragona, Spain
    Behav Brain Res 216:341-8. 2011
  7. ncbi Group II and III mGluRs-mediated presynaptic inhibition of EPSCs recorded from hippocampal interneurons of CA1 stratum lacunosum moleculare
    Christopher J Price
    Medical Research Council, Anatomical Neuropharmacology Unit, Mansfield Road, Oxford OX1 3TH, UK
    Neuropharmacology 49:45-56. 2005
  8. ncbi Activation of alpha7 acetylcholine receptors augments stimulation-induced hippocampal theta oscillation
    C J Siok
    Department of Neuroscience, Pfizer Global Research and Development, Eastern Point Road, Groton, CT 06340, USA
    Eur J Neurosci 23:570-4. 2006
  9. ncbi Hyperforin acts as an angiogenesis inhibitor
    Christoph M Schempp
    Department of Dermatology, University of Freiburg, Germany
    Planta Med 71:999-1004. 2005
  10. ncbi The combined effects of vinclozolin and procymidone do not deviate from expected additivity in vitro and in vivo
    Christine Nellemann
    Institute of Food Safety and Nutrition, Danish Veterinary and Food Administration, Mørkhøj Bygade 19, DK 2860 Søborg, Denmark
    Toxicol Sci 71:251-62. 2003

Research Grants

Detail Information

Publications209 found, 100 shown here

  1. ncbi Synthesis of polyprenylated acylphloroglucinols using bridgehead lithiation: the total synthesis of racemic clusianone and a formal synthesis of racemic garsubellin A
    Nadia M Ahmad
    School of Chemistry, The University of Nottingham, University Park, Nottingham NG7 2RD, UK
    J Org Chem 72:4803-15. 2007
    ..This enabled a formal synthesis of racemic garsubellin A by accessing one of the late intermediates in the Danishefsky synthesis...
  2. ncbi Frontal cortical alpha7 and alpha4beta2 nicotinic acetylcholine receptors in working and reference memory
    Wai Kit Chan
    Department of Biological Sciences, National University of Singapore, 14 Science Drive 4, Singapore 117543, Singapore
    Neuropharmacology 52:1641-9. 2007
    ..Our data thus sheds further light on the frontal cortex as an important anatomical locus for nAchR-mediated memory function in the brain, and highlights the differing role of alpha7 and alpha4beta2 nAchRs in long and short term memory...
  3. ncbi Volatile components of peel and leaf oils of lemon and lime species
    Marie Laure Lota
    Université de Corse, Equipe Chimie et Biomasse, UMR CNRS 6134, Route des Sanguinaires, 20000 Ajaccio, France
    J Agric Food Chem 50:796-805. 2002
    ..Four others were identified for lime leaf oils: beta-pinene/limonene; limonene/geranial/neral; limonene/linalool/citronellal; and limonene/sabinene/citronellal/linalool. These results were interpreted using principal component analysis...
  4. pmc Activation of the α7 nicotinic ACh receptor induces anxiogenic effects in rats which is blocked by a 5-HT₁a receptor antagonist
    Anshul A Pandya
    Laboratory of Neurobiology, National Institute of Environmental Health Sciences, National Institutes of Health, Department of Health and Human Services, Research Triangle Park, MD F2 08, PO Box 12233, NC 27709, USA
    Neuropharmacology 70:35-42. 2013
    ..These results suggest that α7 nAChR PAMs are pharmacologically advantageous over agonists, and should be considered for further development as therapeutic drugs targeting the α7 receptors...
  5. pmc Effects of nicotinic acetylcholine receptor agonists on cognition in rhesus monkeys with a chronic cocaine self-administration history
    Robert W Gould
    Department of Physiology and Pharmacology, Wake Forest University School of Medicine, Winston Salem, NC 27157, USA
    Neuropharmacology 64:479-88. 2013
    ..The cognitive enhancing effects of nAChR agonists may be beneficial in combination with behavioral treatments for cocaine addiction. This article is part of a Special Issue entitled 'Cognitive Enhancers'...
  6. ncbi Behavioral effects of PNU-282987, an alpha7 nicotinic receptor agonist, in mice
    Paloma Vicens
    Department of Psychology, IISPV, Universitat Rovira i Virgili, 43007 Tarragona, Spain
    Behav Brain Res 216:341-8. 2011
    ....
  7. ncbi Group II and III mGluRs-mediated presynaptic inhibition of EPSCs recorded from hippocampal interneurons of CA1 stratum lacunosum moleculare
    Christopher J Price
    Medical Research Council, Anatomical Neuropharmacology Unit, Mansfield Road, Oxford OX1 3TH, UK
    Neuropharmacology 49:45-56. 2005
    ..Our results show powerful modulation of excitatory transmission impinging on interneurons of CA1 SLM by presynaptic group II or III mGluRs...
  8. ncbi Activation of alpha7 acetylcholine receptors augments stimulation-induced hippocampal theta oscillation
    C J Siok
    Department of Neuroscience, Pfizer Global Research and Development, Eastern Point Road, Groton, CT 06340, USA
    Eur J Neurosci 23:570-4. 2006
    ..Given the connection between hippocampal theta oscillation and cognitive processes, it is proposed that precognitive actions of alpha7 nAChR agonists could be mediated, at least in part, by modulation of hippocampal oscillatory activity...
  9. ncbi Hyperforin acts as an angiogenesis inhibitor
    Christoph M Schempp
    Department of Dermatology, University of Freiburg, Germany
    Planta Med 71:999-1004. 2005
    ..These data suggest that, in addition to the induction of tumor cell apoptosis, hyperforin can also suppress angiogenesis by a direct, non-toxic effect on endothelial cells...
  10. ncbi The combined effects of vinclozolin and procymidone do not deviate from expected additivity in vitro and in vivo
    Christine Nellemann
    Institute of Food Safety and Nutrition, Danish Veterinary and Food Administration, Mørkhøj Bygade 19, DK 2860 Søborg, Denmark
    Toxicol Sci 71:251-62. 2003
    ....
  11. ncbi Hyperforin and its analogues inhibit CYP3A4 enzyme activity
    Ju Young Lee
    Pharmaceutical Chemistry, Faculty of Pharmacy, University of Sydney, Building A15, Science Road, Sydney, NSW 2006, Australia
    Phytochemistry 67:2550-60. 2006
    ..63 microM) and furohyperforin (IC(50) 1.3 microM). As the acylphloroglucinols are potent inhibitors of the CYP3A4 enzyme, their modulation of the enzyme activity is unlikely to be involved in increased drug metabolism by St. John's wort...
  12. ncbi The selective alpha7 nicotinic acetylcholine receptor agonist PNU-282987 [N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-4-chlorobenzamide hydrochloride] enhances GABAergic synaptic activity in brain slices and restores auditory gating deficits in anesthetized rats
    M Hajos
    Department of Neuroscience, Pfizer Global Research and Development, Eastern Point Rd, Groton, CT 06340, USA
    J Pharmacol Exp Ther 312:1213-22. 2005
    ..These results provide further support for the concept that drugs that selectively activate alpha7 nAChRs may offer a novel, potential pharmacotherapy in treatment of schizophrenia...
  13. ncbi Chemopreventive effects of ONO-8711, a selective prostaglandin E receptor EP(1) antagonist, on breast cancer development
    T Kawamori
    Cancer Prevention Division, National Cancer Center Research Institute, 1 1 Tsukiji 5 chome, Chuo Ku, Tokyo 104 0045
    Carcinogenesis 22:2001-4. 2001
    ..These results suggest that EP(1) receptor is associated with breast cancer development and selective PGE receptor EP(1) antagonists may possess chemopreventive effects through the induction of apoptosis without any side effects...
  14. ncbi Prostaglandin E2 receptor EP1 transactivates EGFR/MET receptor tyrosine kinases and enhances invasiveness in human hepatocellular carcinoma cells
    Chang Han
    Department of Pathology, University of Pittsburgh School of Medicine, Pennsylvania 15213, USA
    J Cell Physiol 207:261-70. 2006
    ..These findings disclose a cross-talk between the COX-2/PGE(2)/EP(1) and EGFR/c-Met signaling pathways that coordinately regulate human HCC cell invasion...
  15. ncbi Halicyclamine A, a marine spongean alkaloid as a lead for anti-tuberculosis agent
    Masayoshi Arai
    Graduate School of Pharmaceutical Sciences, Osaka University, Yamada oka 1 6, Suita, Osaka 565 0871, Japan
    Bioorg Med Chem 16:6732-6. 2008
    ..smegmatis. However, IMPDH was not target for halicyclamine A, because halicyclamine A showed same MIC value against the wild-type M. smegmatis and IMPDH over-expressing strains...
  16. pmc Activation of the alpha7 nAChR reduces acid-induced acute lung injury in mice and rats
    Xiao Su
    Cardiovascular Research Institute, University of California San Francisco, HSW 825, 505 Parnassus Ave, San Francisco, CA 94143 0130, USA
    Am J Respir Cell Mol Biol 37:186-92. 2007
    ..These results indicate that activation of alpha7 nAChR may provide a new therapeutic pathway for the treatment of acute lung injury...
  17. ncbi Hyperforin: more than an antidepressant bioactive compound?
    Miguel A Medina
    Department of Molecular Biology and Biochemistry, Faculty of Sciences, University of Malaga, E 29071 Malaga, Spain
    Life Sci 79:105-11. 2006
    ..They include other neurological effects, effects on inflammation, as well as antibacterial, antitumoral and antiangiogenic effects...
  18. ncbi Mapping protein interfaces with a fluorogenic cross-linker and mass spectrometry: application to nebulin-calmodulin complexes
    A Sinz
    Laboratory of Physical Biology, National Institute of Arthritis and Musculoskeletal and Skin Diseases, National Institutes of Health, Bethesda, Maryland 20892, USA
    Biochemistry 40:7903-13. 2001
    ..The cross-linking of amino acids 1-6 (MKTPEM) with amino acids 114-129 (YKENVGKATATPVTPE) and 115-129 (KENVGKATATPVTPE) in ND66 hints at an association of noncontiguous nebulin modules in solution...
  19. ncbi Hyperforin and aristoforin inhibit lymphatic endothelial cell proliferation in vitro and suppress tumor-induced lymphangiogenesis in vivo
    Melanie Rothley
    Forschungszentrum Karlsruhe, Institut für Toxikologie und Genetik, Postfach 3640, Karlsruhe, Germany
    Int J Cancer 125:34-42. 2009
    ....
  20. ncbi In vitro antimalarial activity of hyperforin, a prenylated acylphloroglucinol. A structure-activity study
    Luisella Verotta
    Dipartimento di Chimica Organica e Industriale, via Venezian 21, 20133 Milan, Italy
    Bioorg Med Chem Lett 17:1544-8. 2007
    ..Related phloroglucinols like the hop beta-acids and the enantiomers of usnic acid showed only marginal activity, suggesting that hyperforin is a new antimalarial chemotype...
  21. ncbi The antidepressant mechanism of Hypericum perforatum
    Tiziana Mennini
    Istituto di Ricerche Farmacologiche Mario Negri, Via Eritrea 62, 20157, Milano, Italy
    Life Sci 75:1021-7. 2004
    ..In the rat, Hypericum extract might indirectly activate sigma receptors in vivo (through the formation of an unknown metabolite or production of an endogenous ligand), suggesting a new target for its antidepressant effects...
  22. ncbi The fungicide procymidone alters sexual differentiation in the male rat by acting as an androgen-receptor antagonist in vivo and in vitro
    J Ostby
    Endocrinology Branch, National Health and Environmental Effects Research Laboratory, US EPA, Research Triangle Park, NC 27711, USA
    Toxicol Ind Health 15:80-93. 1999
    ....
  23. ncbi Increased cell proliferation in the adult mouse hippocampus following chronic administration of group II metabotropic glutamate receptor antagonist, MGS0039
    Takao Yoshimizu
    Psychiatric Diseases and Pain Research, Medicinal Pharmacology Laboratory, Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    Biochem Biophys Res Commun 315:493-6. 2004
    ..These findings raise the possibility that MGS0039 may exert antidepressant-like effects by modulating cell proliferation in the hippocampus...
  24. ncbi Group II mGlu receptor agonists inhibit behavioural and electrophysiological effects of DOI in mice
    Aleksandra Kłodzińska
    Institute of Pharmacology, Polish Academy of Sciences, 31 343 Cracow, Smetna 12, Poland
    Pharmacol Biochem Behav 73:327-32. 2002
    ..The data indicate that Group II mGlu receptor agonists may counteract the effects of hallucinogenic drugs...
  25. ncbi Enantioselective synthesis of bicyclo[3.1.0]hexane carbocyclic nucleosides via a lipase-catalyzed asymmetric acetylation. Characterization of an unusual acetal byproduct
    Yuichi Yoshimura
    Laboratory of Medicinal Chemistry, Center for Cancer Research, National Cancer Institute Frederick, 376 Boyles St, Frederick, Maryland 21702, USA
    J Org Chem 67:5938-45. 2002
    ..This side reaction was also enzyme-catalyzed and was triggered by the byproduct acetaldehyde generated during the reaction...
  26. ncbi An mGluR2/3 antagonist, MGS0039, exerts antidepressant and anxiolytic effects in behavioral models in rats
    Takao Yoshimizu
    Psychiatric Diseases and Pain Research, Medicinal Pharmacology Laboratory, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    Psychopharmacology (Berl) 186:587-93. 2006
    ..1.0]hexane-2,6-dicarboxylic acid (MGS0039) is a selective antagonist for group II metabotropic glutamate receptors (mGluR2/3), and that it exerted antidepressant effects in some animal behavioral tests...
  27. ncbi Neuropharmacological profiles of antagonists of group II metabotropic glutamate receptors
    Naoya Kawashima
    Research Strategy Group, Pharmaceutical Business Division, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    Neurosci Lett 378:131-4. 2005
    ..These findings suggest that modulation of serotonergic neuron might be, at least in part, responsible for the antidepressant-like effects of group II mGluR antagonists...
  28. ncbi AMPA receptor stimulation mediates the antidepressant-like effect of a group II metabotropic glutamate receptor antagonist
    Jun Ichi Karasawa
    Medicinal Pharmacology Laboratory, Taisho Pharmaceutical Co, Ltd, Kita ku, Saitama 331 9530, Japan
    Brain Res 1042:92-8. 2005
    ..Pretreatment with NBQX significantly attenuated the increase in serotonin release by MGS0039. These findings suggest that stimulation of postsynaptic AMPA receptors plays a role in mediating the pharmacological effects of MGS0039...
  29. ncbi Hypericum perforatum, a source of neuroactive lead structures
    Luisella Verotta
    Dipartimento di Chimica Organica e Industriale, Universita degli Studi di Milano, via Venezian 21, 20133 Milano, Italy
    Curr Top Med Chem 3:187-201. 2003
    ..One clinical trial carried out using two extracts with different hyperforin content indicate this constituent as (one of) the main active principle responsible for the antidepressant activity...
  30. ncbi Hyperforin blocks neutrophil activation of matrix metalloproteinase-9, motility and recruitment, and restrains inflammation-triggered angiogenesis and lung fibrosis
    Raffaele Niero
    Department of Experimental Biomedical Sciences, Medical School, Padova, Italy
    J Pharmacol Exp Ther 321:492-500. 2007
    ..These results indicate that Hyp is a powerful anti-inflammatory compound with therapeutic potential, and they elucidate mechanistic keys...
  31. ncbi Hyperforin down-regulates effector function of activated T lymphocytes and shows efficacy against Th1-triggered CNS inflammatory-demyelinating disease
    Anna Cabrelle
    Department of Clinical and Experiment Medicine, Medical School, Padova, Italy
    J Leukoc Biol 83:212-9. 2008
    ..Together, these properties qualify Hyp as a putative, therapeutic molecule for the treatment of autoimmune inflammatory disease sustained by Th1 cells, including EAE...
  32. ncbi St John's wort: Prozac from the plant kingdom
    G Di Carlo
    Department of Experimental Pharmacology, University of Naples Federico II, via D Montesano 49, 80131 Naples, Italy
    Trends Pharmacol Sci 22:292-7. 2001
    ..However, important herb--drug interactions have been described. In view of its efficacy and safety records, St John's wort should be considered for the first-line treatment of mild to moderate depression...
  33. ncbi Synthesis and biological evaluation of hyperforin analogues. Part I. Modification of the enolized cyclohexanedione moiety
    Luisella Verotta
    Dipartimento di Chimica Organica e Industriale, Universita di Milano, via Venezian 21, 20133 Milano, Italy
    J Nat Prod 65:433-8. 2002
    ....
  34. ncbi Structural investigations of isomeric oxidised forms of hyperforin by HPLC-NMR and HPLC-MSn
    J L Wolfender
    Institut de Pharmacognosie et Phytochimie, Universite de Lausanne, CH 1015 Lausanne, Switzerland
    Phytochem Anal 14:290-7. 2003
    ..The strategy followed for the on-line identification of these constituents is discussed...
  35. ncbi Hyperforin analogues from St. John's wort (Hypericum perforatum)
    L Verotta
    Dipartimento di Chimica Organica e Industriale, via Venezian 21, 20133 Milano, Italy
    J Nat Prod 63:412-5. 2000
    ..Three oxygenated analogues of the prenylated phloroglucinol hyperforin (3-5) were isolated from the aerial parts of Hypericum perforatum and their structures elucidated by spectroscopic methods...
  36. ncbi MGS0039: a potent and selective group II metabotropic glutamate receptor antagonist with antidepressant-like activity
    Shigeyuki Chaki
    Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, Saitama 331 9530, Japan
    Neuropharmacology 46:457-67. 2004
    ..These results indicate that MGS0039 is a potent and selective antagonist of group II mGluR, and that group II mGluR antagonists, like MGS0039, have an antidepressant-like potential in experimental animal models...
  37. ncbi Modulation of chemoselectivity by protein additives. Remarkable effects in the oxidation of hyperforin
    Luisella Verotta
    Dipartimento di Chimica Organica e Industriale, via Venezian 21, 20133 Milano, Italy
    J Org Chem 69:7869-74. 2004
    ..The use of protein additives allows a straightforward and multigram preparation of the enollactone 6, an interesting multifunctionalized scaffold for bioactivity induction and/or modulation...
  38. ncbi Evaluation of hyperforin analogues for inhibition of 5-lipoxygenase
    Christian Feisst
    Institute of Pharmaceutical Chemistry, University of Frankfurt, Marie Curie Str 9, D 60439 Frankfurt, Germany
    Med Chem 1:287-91. 2005
    ..Our data show that some of the oxidised hyperforin derivatives possess even improved efficacy, whereas alkylation and acylation have detrimental effects...
  39. ncbi Hyperforin inhibits cancer invasion and metastasis
    Massimo Dona
    Department of Experimental Biomedical Sciences, Medical School of Padova, Italy
    Cancer Res 64:6225-32. 2004
    ..These observations qualify Hyp-DCHA as an interesting lead compound to prevent and contrast cancer spread and metastatic growth...
  40. ncbi Physiological antagonism between 5-hydroxytryptamine(2A) and group II metabotropic glutamate receptors in prefrontal cortex
    G J Marek
    Department of Psychiatry and Pharmacology, Yale University School of Medicine, Ribicoff Research Facilities of the Connecticut Mental Health Center, New Haven, CT 06508, USA
    J Pharmacol Exp Ther 292:76-87. 2000
    ....
  41. ncbi Instability of St. John's wort (Hypericum perforatum L.) and degradation of hyperforin in aqueous solutions and functional beverage
    Catharina Y W Ang
    National Center for Toxicological Research, U S Food and Drug Administration, 3900 NCTR Road, Jefferson, AR 72079, USA
    J Agric Food Chem 52:6156-64. 2004
    ..The latter was also found in the drink product containing SJW as an ingredient. Biological activities and potential quality and safety implications of these chemical changes are yet to be evaluated...
  42. ncbi Protective effects of St. John's wort extract and its component hyperforin against cytokine-induced cytotoxicity in a pancreatic beta-cell line
    Marta Menegazzi
    Dipartimento di Scienze Morfologiche e Biomediche, University of Verona, Strada Le Grazie 8, 37134 Verona, Italy
    Int J Biochem Cell Biol 40:1509-21. 2008
    ..Thus, they are potentially valuable for the prevention or limitation of beta-cell loss in diabetes...
  43. ncbi Construction of highly functionalized medium-sized rings: synthesis of hyperforin and perforatumone model systems
    K C Nicolaou
    Department of Chemistry and Skaggs Institute for Chemical Biology, Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    Angew Chem Int Ed Engl 44:3895-9. 2005
  44. ncbi Effects of the antidepressant St. John's wort (Hypericum perforatum) on rat and human vas deferens contractility
    Raffaele Capasso
    Departments of Experimental Pharmacology and Urology, University of Naples Federico II, Naples Italy
    J Urol 173:2194-7. 2005
    ..John's wort (SJW) (Hypericum perforatum) we evaluated the effect of this herbal antidepressant on rat and human vas deferens contractility...
  45. ncbi Pseudohypericin and hyperforin in Hypericum perforatum from Northern Turkey: variation among populations, plant parts and phenological stages
    Cuneyt Cirak
    Department of Agronomy, Faculty of Agriculture, University of Ondokuz Mayis, 55139 Kurupelit, Samsun, Turkey
    J Integr Plant Biol 50:575-80. 2008
    ..The present findings might be useful to optimize the processing methodology of wild-harvested plant material and obtain increased concentrations of these secondary metabolites...
  46. ncbi Hypericum perforatum extract in burning mouth syndrome: a randomized placebo-controlled study
    Andrea Sardella
    Unit of Oral Pathology and Medicine, School of Dentistry, University of Milan, Milan, Italy
    J Oral Pathol Med 37:395-401. 2008
    ..perforatum extract taken three times a day for 12 weeks improved the pain of BMS patients, although the general reduction in the number of sites with reported burning sensation, a less accurate and objective score, was significant...
  47. ncbi Investigation of the bioavailability of hypericin, pseudohypericin, hyperforin and the flavonoids quercetin and isorhamnetin following single and multiple oral dosing of a hypericum extract containing tablet
    Hans Ulrich Schulz
    LAFAA Laboratory for Contract Research in Clinical Pharmacology and Biopharmaceutical Analytics GmbH, Bad Schwartau Germany
    Arzneimittelforschung 55:15-22. 2005
    ..The kinetic characteristics of the hypericum flavonoids are reported here for the first time. The trial preparation was well tolerated...
  48. ncbi Biosynthesis of the hyperforin skeleton in Hypericum calycinum cell cultures
    Petra Klingauf
    Institut fur Pharmazeutische Biologie, Technische Universitat Braunschweig, Mendelssohnstrasse 1, D 38106 Braunschweig, Germany
    Phytochemistry 66:139-45. 2005
    ..The three type III polyketide synthases were separated by anion exchange chromatography...
  49. ncbi The first prenylation step in hyperforin biosynthesis
    Zakia Boubakir
    Institut fuer Pharmazeutische Biologie, Technische Universitaet Braunschweig, Mendelssohnstr 1, D 38106 Braunschweig, Germany
    Phytochemistry 66:51-7. 2005
    ..The formation of hyperforins in H. calycinum cell cultures was preceded by an increase in dimethylallyltransferase activity, with the maximum specific activity being 3.6 microkat/kg protein...
  50. ncbi Bioactive constituent production in St. John's Wort in vitro hairy roots. Regenerated plant lines
    Alessandra Bertoli
    Dipartimento di Chimica Bioorganica e Biofarmacia DCBB, Universita di Pisa, Via Bonanno 33, 56126 Pisa, Italy
    J Agric Food Chem 56:5078-82. 2008
    ..25 mg/gdw) than that reported for the in vitro shoots in the literature. Morphological and phytochemical features were determined in order to select H. perforatum genotypes enriched in valuable bioactive compounds...
  51. ncbi Functional induction and de-induction of P-glycoprotein by St. John's wort and its ingredients in a human colon adenocarcinoma cell line
    Run Tian
    Department of Medico Pharmaceutical Sciences, Graduate School of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan
    Drug Metab Dispos 33:547-54. 2005
    ..Hyperforin is considered to be a primary cause of the inductive effect of St. John's wort. Long-term administration of St. John's wort may cause clinically significant decrease in the plasma concentrations of P-glycoprotein substrates...
  52. ncbi A mechanistic study on altered pharmacokinetics of irinotecan by St. John's wort
    Ze Ping Hu
    Department of Pharmacy, Faculty of Science, National University of Singapore, Science Drive 4, 117543, Singapore
    Curr Drug Metab 8:157-71. 2007
    ..Further studies are needed to explore the role of both pharmacokinetic and pharmacodynamic components in the protective effect of SJW against the toxicities of CPT-11...
  53. ncbi Biosynthesis of hyperforin and adhyperforin from amino acid precursors in shoot cultures of Hypericum perforatum
    Katja Karppinen
    Department of Biology, University of Oulu, P O Box 3000, FIN 90014 Oulu, Finland
    Phytochemistry 68:1038-45. 2007
    ..0-fold increase in the accumulation of adhyperforin. The administration of L-valine at concentrations of 0-5mM had no stimulating effect on the hyperforin production in H. perforatum shoot cultures...
  54. pmc Hyperforin accumulates in the translucent glands of Hypericum perforatum
    Jens Soelberg
    Biological Institute, Department of Evolutionary Biology, University of Copenhagen, Botanical Laboratory, Gothersgade 140, 1123 Copenhagen, Denmark
    Ann Bot 99:1097-100. 2007
    ..Hypericum perforatum contains the therapeutically important compounds hypericin and hyperforin. Hypericin is known to accumulate in the dark glands. This investigation aimed to determine the accumulation site of hyperforin...
  55. ncbi Hypericin and hyperforin production in St. John's wort in vitro culture: influence of saccharose, polyethylene glycol, methyl jasmonate, and Agrobacterium tumefaciens
    M Pavlik
    University of Veterinary and Pharmaceutical Sciences, Palackeho 1 3, CZ 61242 Brno, Czech Republic
    J Agric Food Chem 55:6147-53. 2007
    ..The obtained results will be applied in experimental botany and in the technology of H. perforatum cultivation for pharmaceutical applications...
  56. ncbi Simultaneous determination of total hypericin and hyperforin in St. John's wort extracts by HPLC with electrochemical detection
    Ulla Rückert
    Institut für Pharmazeutische Wissenschaften, Karl Franzens Universitat Graz, Schubertstrasse 1, A 8010 Graz, Austria
    Phytochem Anal 18:204-8. 2007
    ..For quantification, an HPLC method with electrochemical detection was applied. As an example of the application of the principle, two preparations containing St. John's wort were assayed...
  57. ncbi Topical anti-inflammatory activity of extracts and compounds from Hypericum perforatum L
    Silvio Sosa
    Dipartimento dei Materiali e delle Risorse Naturali, Universita di Trieste, Trieste, Italy
    J Pharm Pharmacol 59:703-9. 2007
    ..The pharmacological activity and phytochemical profile of the tested extracts and fraction suggest that different constituents are involved in the topical antiphlogistic property of H. perforatum in-vivo...
  58. ncbi Mass spectral characterization of phloroglucinol derivatives hyperforin and adhyperforin
    Lekha Sleno
    Institute for Marine Biosciences, 1411 Oxford Street, Halifax, Nova Scotia B3H 3Z1, Canada
    Rapid Commun Mass Spectrom 20:2641-8. 2006
    ..This information is expected to be especially valuable for the characterization of related compounds, such as degradation products, metabolites and novel synthetic analogs of hyperforin...
  59. ncbi Hypericum perforatum: a 'modern' herbal antidepressant: pharmacokinetics of active ingredients
    Mario Wurglics
    Institute of Pharmaceutical Chemistry, ZAFES, J W Goethe University, Frankfurt am Main, Germany
    Clin Pharmacokinet 45:449-68. 2006
    ..perforatum extract has been investigated in only one study. More data are available for rutin and the aglycone quercetin after administration of pure substances or other flavonoid sources...
  60. ncbi Effect of eluent pH on the HPLC-UV analysis of hyperforin from St. John's Wort (Hypericum perforatum L.)
    Jean Dominique Fourneron
    Laboratory of Galenic and Industrial Pharmacy, Faculty of Pharmacy, 27 Boulevard Jean Moulin, 13385 Marseille, France
    Phytochem Anal 17:71-7. 2006
    ....
  61. ncbi [Hypericin and hyperforin: bioactive components of St. John's Wort (Hypericum perforatum). Their isolation, analysis and study of physiological effect]
    J Vacek
    Akademie ved Ceské republiky, Biofyzikální ústav, Brno
    Ceska Slov Farm 56:62-6. 2007
    ..The review paper surveys the present knowledge of chemical and analytical methods for their identification and quantification, physiological activity, and pharmacological and biomedical applications of hypericin and hyperforin...
  62. ncbi Differential accumulation of hyperforin and secohyperforin in Hypericum perforatum tissue cultures
    Armen Charchoglyan
    Yerevan State University, Faculty of Biology, Alex Manoogian Street 1, Yerevan, Armenia
    Phytochemistry 68:2670-7. 2007
    ..No differential stimulation was observed after elicitor treatment. Hyperforin and secohyperforin are proposed to arise from a branch point in the biosynthetic pathway...
  63. pmc Inhibition of prostaglandin E(2) production by anti-inflammatory hypericum perforatum extracts and constituents in RAW264.7 Mouse Macrophage Cells
    Kimberly D P Hammer
    The Center for Research on Botanical Dietary Supplements, Interdepartmental Genetics Graduate Program, Iowa State University, Ames, Iowa 50011, USA
    J Agric Food Chem 55:7323-31. 2007
    ....
  64. ncbi St. John's wort: role of active compounds for its mechanism of action and efficacy
    Veronika Butterweck
    Department of Pharmaceutics, College of Pharmacy, University of Florida, Gainesville, FL 32608, USA
    Wien Med Wochenschr 157:356-61. 2007
    ..Although there are some open questions, the bulk of data suggests that several groups of active compounds are contributing to the antidepressant efficacy of the plant extract...
  65. ncbi St. John's wort
    Silvana Lawvere
    Department of Clinical Prevention, Roswell Park Cancer Institute, Buffalo, New York 14263, USA
    Am Fam Physician 72:2249-54. 2005
    ..Studies of St. John's wort for the treatment of major depression have had conflicting results. St. John's wort is generally well tolerated, although it may potentially reduce the effectiveness of several pharmaceutical drugs...
  66. ncbi Investigation of pharmacokinetic data of hypericin, pseudohypericin, hyperforin and the flavonoids quercetin and isorhamnetin revealed from single and multiple oral dose studies with a hypericum extract containing tablet in healthy male volunteers
    Hans Ulrich Schulz
    LAFAA Laboratory for Contract Research in Clinical Pharmacology and Biopharmaceutical Analytics GmbH, Bad Schwartau, Germany
    Arzneimittelforschung 55:561-8. 2005
    ..The data obtained for the five consitituents generally corresponded well with values previously published. The trial preparation was well tolerated...
  67. pmc Undeclared exposure to St. John's Wort in hospitalized patients
    Meret Martin-Facklam
    Department of Internal Medicine VI, Clinical Pharmacology and Pharmacoepidemiology, University of Heidelberg, Heidelberg, Germany
    Br J Clin Pharmacol 58:437-41. 2004
    ....
  68. ncbi The production of hypericins and hyperforin by in vitro cultures of St. John's wort (Hypericum perforatum)
    Ara Kirakosyan
    Department of Molecular, Cellular and Developmental Biology, University of Michigan, Ann Arbor, MI 48109 1048, USA
    Biotechnol Appl Biochem 39:71-81. 2004
    ..Additionally, factors optimizing compound production--particularly in in vitro cultures--are presented and reviewed...
  69. ncbi Researching the antidepressant actions of Hypericum perforatum (St. John's wort) in animals and man
    M Franklin
    University of Oxford Department of Psychiatry, Warneford Hospital, UK
    Pharmacopsychiatry 34:S29-37. 2001
    ..The data also suggests that hyperforin may be more important than hypericin for effecting these changes following acute treatment. Further studies investigating both acute and sub-chronic effects of these compounds are necessary...
  70. ncbi Biosynthesis of hyperforin in Hypericum perforatum
    Petra Adam
    Lehrstuhl fur Organische Chemie und Biochemie, Technische Universitat Munchen, Lichtenbergstrasse 4, D 85747 Garching, Germany
    J Med Chem 45:4786-93. 2002
    ..The phloroglucinol moiety is generated via a polyketide type mechanism...
  71. ncbi Evaluation of synaptosomal uptake inhibition of most relevant constituents of St. John's wort
    M Wonnemann
    Department of Pharmacology, Biocenter Niederursel, University of Frankfurt, Frankfurt/Main, Germany
    Pharmacopsychiatry 34:S148-51. 2001
    ..Further investigations would have to clarify any possible contribution of these two constituents to the antidepressive effects of SJW extract seen in animal experiments and clinical trials...
  72. ncbi Effects of two different extracts of St. John's wort and some of their constituents on cytochrome P450 activities in rat liver microsomes
    M Nöldner
    Department of Pharmacology, Dr Willmar Schwabe GmbH and Co, Karlsruhe, FRG
    Pharmacopsychiatry 34:S108-10. 2001
    ..Our results demonstrated that the reported interactions between St. John's Wort and various other drugs are not mediated by CYP 450 isoforms present in rat liver...
  73. ncbi Hyperforin a constituent of St John's wort (Hypericum perforatum L.) extract induces apoptosis by triggering activation of caspases and with hypericin synergistically exerts cytotoxicity towards human malignant cell lines
    Katarina Hostanska
    Department of Internal Medicine, University Hospital Zurich, Zurich, Switzerland
    Eur J Pharm Biopharm 56:121-32. 2003
    ..Cytocidal effects of HP and its cooperation with HY on tumor growth inhibition in a synergistic manner make the St John's wort an interesting option in cancer warranting further in vitro and in vivo investigation...
  74. ncbi [Formulation of St. John's wort extract. A medicinal obstacle course]
    Peter Christian Schmidt
    Universität Tübingen Pharmazeutisches Institut Lehrstuhl Pharmazeutische Technologie Auf der Morgenstelle 8 72076 Tübingen
    Pharm Unserer Zeit 32:203-11. 2003
  75. ncbi Step by step removal of hyperforin and hypericin: activity profile of different Hypericum preparations in behavioral models
    Veronika Butterweck
    Institute of Pharmacology and Toxicology, Universitätsklinikum Muenster, Domagkstrasse 12, 48149 Muenster, Germany
    Life Sci 73:627-39. 2003
    ..We also could show that hyperforin contributes to the beneficial properties of SJW extract, confirming the hypothesis that the crude SJW extract contains several constituents with antidepressant activity...
  76. ncbi Role of hyperforin in the antidepressant-like activity of Hypericum perforatum extracts
    Luigi Cervo
    Istituto di Ricerche Farmacologiche Mario Negri, Via Eritrea 62, 20157 Milan, Italy
    Psychopharmacology (Berl) 164:423-8. 2002
    ..Hyperforin has been identified as an active constituent of Hypericum perforatum but its importance in the antidepressant effect of this plant's extracts is not really known...
  77. ncbi An in vitro and hydroponic growing system for hypericin, pseudohypericin, and hyperforin production of St. John's wort (Hypericum perforatum CV new stem)
    Susan J Murch
    Department of Plant Agriculture, University of Guelph, Guelph, Ontario, Canada
    Planta Med 68:1108-12. 2002
    ..These data provide evidence that greenhouse hydroponic systems can be effectively used for the efficient production of St. John's wort and other medicinal plants...
  78. ncbi 2.1 A crystal structure of human PXR in complex with the St. John's wort compound hyperforin
    Ryan E Watkins
    Department of Chemistry, The University of North Carolina at Chapel Hill, North Carolina 27599, USA
    Biochemistry 42:1430-8. 2003
    ....
  79. ncbi Simultaneous determination of hypericin and hyperforin in human plasma and serum using liquid-liquid extraction, high-performance liquid chromatography and liquid chromatography-tandem mass spectrometry
    R Pirker
    Institute of Analytical Chemistry and Radiochemistry, Leopold Franzens University, Innrain 52a, 6020, Innsbruck, Austria
    J Chromatogr B Analyt Technol Biomed Life Sci 777:147-53. 2002
    ..John's Wort extract capsules. Blood samples were taken 2, 4, and 6 h after ingestion. Finally, this method proved to be highly suitable for clinical and pharmacologically relevant studies...
  80. ncbi In vitro binding studies with two hypericum perforatum extracts--hyperforin, hypericin and biapigenin--on 5-HT6, 5-HT7, GABA(A)/benzodiazepine, sigma, NPY-Y1/Y2 receptors and dopamine transporters
    M Gobbi
    Istituto di Ricerche Farmacologiche Mario Negri, Milan, Italy
    Pharmacopsychiatry 34:S45-8. 2001
    ....
  81. ncbi Fast high-performance liquid chromatographic analysis of naphthodianthrones and phloroglucinols from Hypericum perforatum extracts
    Ari Tolonen
    Department of Chemistry, University of Oulu, PO Box 3000, 90014 Oulu, Finland
    Phytochem Anal 14:306-9. 2003
    ..1 to 17% within these ranges. Lower levels of quantitative determination were 2 microg/mL for hyperforin and 0.5 microg/mL for hypericin, while detection limits were 0.1 and 0.02 microg/mL, respectively...
  82. ncbi Inhibitory effect of the antidepressant St. John's wort (hypericum perforatum) on rat bladder contractility in vitro
    Raffaele Capasso
    Department of Experimental Pharmacology, University of Naples Federico II, Naples, Italy
    Urology 64:168-72. 2004
    ..To evaluate the effect of St. John's wort (SJW), an effective and safe herbal antidepressant, on rat bladder contractility. Recent data have suggested a strong association between depression and urinary incontinence...
  83. ncbi Quantitative characterization of direct P-glycoprotein inhibition by St John's wort constituents hypericin and hyperforin
    Er jia Wang
    Drug Metabolism and Pharmacokinetics, Schering Plough Research Institute, Lafayette, NJ 07848, USA
    J Pharm Pharmacol 56:123-8. 2004
    ....
  84. ncbi Induction of hypericins and hyperforins in Hypericum perforatum in response to damage by herbivores
    Tara M Sirvent
    Department of Plant Pathology, Cornell University, Ithaca, New York, USA
    J Chem Ecol 29:2667-81. 2003
    ..Although the leaf damage index of the specialist feeding was 2.7 times greater, C. quadrigemina had little effect on H. perforatum chemical defenses in response to feeding damage in comparison to generalist feeding...
  85. ncbi A preliminary approach to nonenolizable beta,beta-tricarbonyls: assembly of a hyperevolutin prototype
    David G J Young
    Department of Chemistry, University of Tennessee, Knoxville, Knoxville, Tennessee 37996, USA
    J Org Chem 67:3134-7. 2002
    ..Treatment of 20 with Raney nickel and hydrogen gas produced primary enamine 21 which contains a nonenolizable beta,beta-tricarbonyl group in latent form...
  86. ncbi Quantitative analysis of the active components and the by-products of eight dry extracts of Hypericum perforatum L. (St John's Wort)
    S G von Eggelkraut-Gottanka
    Department of Pharmaceutical Technology, Auf der Morgenstelle 8, D 72076 Tubingen, Germany
    Phytochem Anal 13:170-6. 2002
    ..9-8.3%) was estimated by elemental analysis. Thus, 60-70% of the compounds of the H. perforatum dry extracts have been quantified...
  87. ncbi Extracts of St. John's wort and various constituents affect beta-adrenergic binding in rat frontal cortex
    K Simbrey
    Institute of Pharmacology and Toxicology, Universitatsklinikum Munster, Domagkstrasse 12, 48149 Munster, Germany
    Life Sci 74:1027-38. 2004
    ..Compared to the SJW extracts and single compounds the effect of imipramine on beta-AR-binding was more pronounced in both treatment paradigms...
  88. ncbi Determining hyperforin and hypericin content in eight brands of St. John's wort
    Gerlie C de los Reyes
    School of Pharmacy, University of Southern California, 1985 Zonal Avenue, Los Angeles, CA 90089 9121, USA
    Am J Health Syst Pharm 59:545-7. 2002
  89. ncbi Short term treatment with St. John's wort, hypericin or hyperforin fails to induce CYP450 isoforms in the Swiss Webster mouse
    B J Bray
    Department of Pharmacology, University of Otago, Dunedin, New Zealand
    Life Sci 70:1325-35. 2002
    ..These results indicate that four days of treatment with moderate to high doses of SJW, hyperforin or hypericin fails to induce these CYP450 isoforms in the male Swiss Webster mouse...
  90. ncbi Effect of St. John's wort on free radical production
    E J Hunt
    University of Georgia College of Pharmacy, Department of Clinical and Administrative Sciences, Athens 30602, USA
    Life Sci 69:181-90. 2001
    ..The results of this study suggest that St. John's wort inhibits free radical production in both cell-free and human vascular tissue...
  91. ncbi Separation of hypericins and hyperforins in extracts of Hypericum perforatum L. using non-aqueous capillary electrophoresis with reversed electro-osmotic flow
    Anette Gemal Jensen
    Department of Analytical and Pharmaceutical Chemistry, The Royal Danish School of Pharmacy, Universitetsparken 2, DK 2100, Copenhagen, Denmark
    J Pharm Biomed Anal 27:167-76. 2002
    ..The technique of non-aqueous capillary electrophoresis with reversed electro-osmotic flow provides a very fast technique to evaluate the composition of hypericins and hyperforins in extracts of Hypericum perforatum L...
  92. ncbi St John's wort, a herbal antidepressant, activates the steroid X receptor
    J M Wentworth
    Department of Medicine, University of Cambridge, Addenbrooke's Hospital, Cambridge, CB2 2QQ, UK
    J Endocrinol 166:R11-6. 2000
    ..Future development of SJW derivatives lacking SXR activation, may enable its antidepressant and drug-metabolising properties to be dissociated...
  93. ncbi Xenobiotic organic compounds in leachates from ten Danish MSW landfills--chemical analysis and toxicity tests
    A Baun
    Environment and Resources DTU, Technical University of Denmark, Bygningstorvet, Building 115, DK 2800 Kongens Lyngby, Denmark
    Water Res 38:3845-58. 2004
    ..The compounds belong to the following groups: BTEX, C3-benzenes, bicyclo compounds, napthalenes, chlorinated aliphatics, phenols (chloro-, methyl-, dimethyl, nonyl-), pesticides, and ..
  94. ncbi Synthesis and in vitro muscarinic activities of a series of 3-(pyrazol-3-yl)-1-azabicyclo[2.2.2]octanes
    R Plate
    Department of Medicinal Chemistry, N V Organon, Oss, The Netherlands
    Bioorg Med Chem 8:449-54. 2000
    ..Preferential inhibition of OXO-M binding was used as an indicator for potential muscarinic agonistic properties; this potential was confirmed in functional studies on isolated organs...
  95. ncbi Removal of the 2.2.2 cryptand (Kryptofix 2.2.2) from 18FDG by cation exchange
    D L Alexoff
    Department of Chemistry, Brookhaven National Laboratory, Upton, NY 11973
    Int J Rad Appl Instrum A 42:1189-93. 1991
    ..Quality assurance tests including apyrogenicity, sterility, radiochemical purity, carbohydrate composition and pH were not compromised by the incorporation of the cryptand removal cartridge...
  96. ncbi Characterisation of an mGlu8 receptor-selective agonist and antagonist in the lateral and medial perforant path inputs to the dentate gyrus
    Marion S Mercier
    MRC Centre for Synaptic Plasticity, School of Physiology and Pharmacology, University of Bristol, Dorothy Hodgkin Building, Bristol BS1 3NY, UK
    Neuropharmacology 67:294-303. 2013
    ..MDCPG may be a useful tool in determining whether observable DCPG effects are attributable to mGlu8, versus mGlu2, receptor activation...
  97. ncbi Reagent-based DOS: developing a diastereoselective methodology to access spirocyclic- and fused heterocyclic ring systems
    V Surendra Babu Damerla
    GVK Biosciences Pvt Ltd, Department of Medicinal Chemistry, 28 A IDA Nacharam, Hyderabad, India
    Chem Asian J 7:2351-60. 2012
    ..In summary, our DOS methodology affords new, diverse scaffolds, thereby resulting in compounds that may have significance in medicinal chemistry...
  98. ncbi Synthesis of 2-aminomethyl-4-phenyl-1-azabicyclo[2.2.1]heptanes via LiAlH₄-induced reductive cyclization of 2-(4-chloro-2-cyano-2-phenylbutyl)aziridines and evaluation of their antimalarial activity
    Matthias D'hooghe
    Department of Sustainable Organic Chemistry and Technology, Faculty of Bioscience Engineering, Ghent University, Coupure Links 653, B 9000 Ghent, Belgium
    Bioorg Med Chem Lett 23:1507-10. 2013
    ..Furthermore, the proposed mode of action was supported by ligand docking studies, pointing to a strong binding interaction with the enzyme plasmepsin II...
  99. ncbi Ozonolysis of beta-pinene: temperature dependence of secondary organic aerosol mass fraction
    Ravikant Pathak
    Center for Atmospheric Particle Studies, Carnegie Mellon University, Pittsburgh, PA, USA
    Environ Sci Technol 42:5081-6. 2008
    ..The parametrization predicts much higher SOA production for beta-pinene ozonolysis for typical atmospheric conditions than the values that have been suggested by previous studies...
  100. pmc Asymmetric total synthesis of (+)- and (-)-clusianone and (+)- and (-)-clusianone methyl enol ether via ACC alkylation and evaluation of their anti-HIV activity
    Michelle R Garnsey
    Department of Chemistry, Duke University, Durham, NC 27705, USA
    Bioorg Med Chem Lett 21:2406-9. 2011
    ..The four synthetic compounds were evaluated for their anti-HIV activity. Both (+)- and (-)-clusianone displayed significant anti-HIV activity...
  101. ncbi The role of nicotinic acetylcholine receptor (nAChR) α7 subtype in the functional interaction between nicotine and ethanol in mouse cerebellum
    Najla Taslim
    Department of Pharmacology and Toxicology, Brody School of Medicine, East Carolina University, Greenville, North Carolina 27834, USA
    Alcohol Clin Exp Res 35:540-9. 2011
    ..This study, an extension of earlier work, was intended to investigate the possible role of nAChR subtype α(7) in mitigating ethanol ataxia...

Research Grants49

  1. Synthesis of Macrolides, Steroids, Cyclopentanoids, etc.
    BARRY TROST; Fiscal Year: 2009
    ..These new synthetic methods apply to many structural types beyond those illustrated and constitutes a significant to gain access to complex molecular targets more easily. ..
  2. TUMOR REMISSION--TAXOL AND CLOSE ANALOGS VIA SYNTHESIS
    LEO PAQUETTE; Fiscal Year: 2003
    ..These include, but are not limited to, the 1-deoxy, D-homo-, 2-desmethyl, and 12-methylene derivatives, in addition to the D-ring invertomer and the C-nor isomer. ..
  3. Discovery of Novel Pharmacotherapies: Cocaine Dependence
    PETER MELTZER; Fiscal Year: 2008
    ..vi) analogues of pyrovalerone. ..
  4. Allenic [2 + 2 + 1] Reactions Enabling Syntheses of Natural Products with 7-Membe
    Kay M Brummond; Fiscal Year: 2010
    ..Grayanotoxin is an important molecular tool for deciphering the mechanism for gating functions of the sodium ion channels. ..
  5. TOTAL SYNTHESIS OF AZADIRACHTIN
    K Nicolaou; Fiscal Year: 2008
    ..The proposed work is expected to impact the general areas of pharmaceutical and agricultural research, and infectious diseases in particular, through discoveries in synthetic organic chemistry and chemical biology. ..
  6. Enabling Technologies for Combinatorial Chemistry
    K Nicolaou; Fiscal Year: 2005
    ..abstract_text> ..
  7. Tandem Cycloaddition Chemistry of 2-Azoniaheterodienes
    SCOTT DENMARK; Fiscal Year: 2007
    ..abstract_text> ..
  8. TOTAL SYNTHESIS OF APOPTOLIDIN
    K Nicolaou; Fiscal Year: 2004
    ..The proposed work is expected to have significant impact in the area of cancer chemotherapy and should provide enabling technologies and tools for biology and medicine. ..
  9. INTERESTING BIOACTIVE SUBSTANCES
    David Williams; Fiscal Year: 2006
    ..The selective synthesis of contiguous stereotriads will advance basic methodology for asymmetric conjugate additions. ..
  10. SYNTHESIS OF ANTICANCER AGENTS
    K C Nicolaou; Fiscal Year: 2010
    ..abstract_text> ..
  11. CHEMICAL SYNTHESIS OF NOVEL NATURAL PRODUCTS
    David Williams; Fiscal Year: 2009
    ..Daphnicyclidin A. This recent discovery has revealed a new molecular architecture which exhibits significant antitumor activity. Our research will investigate strategies for chemical synthesis of these complex polycyclic systems. ..
  12. Cross-Coupling Reactions of Organosilanols
    SCOTT DENMARK; Fiscal Year: 2009
    ..Synthetic approaches to isodomoic acid H, hepatitis C viral inihibiting indole alkaloids, the salicylihalimide macrolactone oximidine II, and polyene antiviral antibiotic viridenomycin are detailed. ..
  13. TOTAL SYNTHESIS OF NATURAL PRODUCTS
    K Nicolaou; Fiscal Year: 2002
    ..3] sigmatropic rearrangement and a radical based ring closure to form the bicyclic skeleton. ..
  14. NEW RHODIUM-CATALYZED ALLYLIC ALKYLATION REACTIONS
    P Evans; Fiscal Year: 2006
    ..The development of a temporary silicon-tethered (TST) rhodium-catalyzed [4+2+2] carbocyclization approach to the diterpene, epoxydictymene. ..
  15. PHYSIOLOGICALLY ACTIVE NATURAL PRODUCTS
    Douglass Taber; Fiscal Year: 2007
    ..In the course of these investigations, new molecular reactivity will be developed that will substantially shorten current routes to polycyclic natural products and drug candidates. ..
  16. Novel Glutamatergic Detoxification Strategies
    John Krystal; Fiscal Year: 2006
    ..abstract_text> ..
  17. Symposium on Neuroimaging in Alcoholism
    John Krystal; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  18. CYTOTOXIC NITROGEN HETEROCYCLES
    Edwin Vedejs; Fiscal Year: 2008
    ..abstract_text> ..
  19. AMINO ACID NEUROTRANSMITTER DYSREGULATION IN ALCOHOLISM
    John Krystal; Fiscal Year: 2008
    ..abstract_text> ..
  20. Development of PET radioligands for cerebral cannabinoid receptor (CB1)
    ANDREW HORTI; Fiscal Year: 2008
    ....
  21. High Throughput Screening for Potassium Channel Modulators
    ELENA MAKHINA; Fiscal Year: 2008
    ..Identified compounds will serve both for basic study of K+ channel physiology and as a basis for development of clinical K+ channel drugs. [unreadable] [unreadable] [unreadable]..
  22. Symposium on Neuroimaging in Alcoholism
    John Krystal; Fiscal Year: 2003
    ..A call for abstracts also will bring forward names and ideas from other groups that might be added to the main program. Young Investigator travel scholarships will be considered. ..
  23. Chemistry and Biology of 5-HT2C Receptor Ligands for Drug Abuse
    ALAN PAUL KOZIKOWSKI; Fiscal Year: 2010
    ....
  24. DESIGN AND SYNTHESIS OF NONPEPTIDE PROTEASE INHIBITORS
    Arun K Ghosh; Fiscal Year: 2010
    ..This research integrates organic synthesis, protein-ligand x-ray crystallography, molecular modeling and in-depth virus and cell-biological studies to design the next generation of HIV-1 protease inhibitors. ..
  25. ASYMMETRIC SYNTHESIS OF ANTITUMOR AGENTS
    MICHAEL CRIMMINS; Fiscal Year: 2005
    ..Laulimalide stimulates tubulin polymerization more effectively than paclitaxel. Laulimalide is a representative of a new class of microtubule stabilizing agents with promise for therapeutic potential. ..
  26. Asymmetric Synthesis of Bioactive Chiral Amines
    GREGORY FRIESTAD; Fiscal Year: 2006
    ..In the long term, these endeavors will advance the art and science of synthetic organic chemistry toward the ideal of efficiency, a long-term goal which remains mostly inaccessible in syntheses of complex natural products. ..
  27. STEREOSELECTIVE SYNTHESIS OF CYCLIC ETHERS
    P Evans; Fiscal Year: 2006
    ..Finally, we will examine a series bismuth-catalyzed bis-reductive etherification reactions for the construction of linear fused polycyclic ethers. ..
  28. SYNTHESIS OF THE TEDANOLIDES, CYTOTOXIC POLYPROPIONATES
    Michael Jung; Fiscal Year: 2003
    ....
  29. CHEMICAL AND PHARMACOLOGICAL STUDIES OF COCAINE ANALOGS
    Alan Kozikowski; Fiscal Year: 2004
    ....
  30. Micromass LCT Mass Spectrometer
    MICHAEL CRIMMINS; Fiscal Year: 2004
    ..The major users group is highly dependent on rapid turn around mass spectral data. Since there is currently no Departmental mass spectrometry facility, the research programs of the major users have been seriously hampered for some time. ..
  31. ARENE ACTIVATION BY TRANSITION METALS
    ANTHONY PEARSON; Fiscal Year: 2004
    ....
  32. AMINO ACID NEUROTRANSMITTER DYSREGULATION IN ALCOHOLISM
    John Krystal; Fiscal Year: 2003
    ..In summary, this K02 award would foster my academic development and enable me to better contribute to the building of pathophysiologic models of alcoholism that can guide medications development for this disorder. ..
  33. NALTREXONE BLOCKADE OF NMDA
    John Krystal; Fiscal Year: 2002
    ..Thus, the blockade of the rewarding effects of ketamine by naltrexone may provide insight into an important mechanism underlying the psychopharmacology of ethanol and the treatment of alcoholism. ..
  34. Agilent 5973 GC/MS System
    GARY MOLANDER; Fiscal Year: 2002
    ..Our current lack of such instrumentation negatively affects the ability to carry out many of these studies. This critical capability, in the form of an instrument for everyday analysis, is urgently needed. ..
  35. BIOLOGICAL STUDIES OF PIPERIDINE ANALOGS OF COCAINE
    Alan Kozikowski; Fiscal Year: 2001
    ..4. For compounds meeting set criteria, to further evaluate their behavioral pharmacological profile in animals using intravenous drug self-administration and drug discrimination procedures. ..
  36. Catalytic Processes for Selective Organic Synthesis
    GARY MOLANDER; Fiscal Year: 2005
    ..4) Carbometalation/cyclization reactions will be explored utilizing organochromium species. 5) Ligands and catalytic systems designed for asymmetric synthesis will be explored. ..
  37. DESIGN OF LIGANDS SELECTIVE FOR THE DAG SUPERFAMILY
    Alan Kozikowski; Fiscal Year: 2002
    ..To assess the effect of alterations in the ligand's hydrophobic side chain on its tumor promoting activity, studies of skin hyperplasia will be conducted. ..
  38. ASYMMETRIC SYNTHESIS OF NOVEL NATURAL PRODUCTS
    MICHAEL CRIMMINS; Fiscal Year: 2006
    ..Synthesis of the biologically active agents guanacastepene, and SCH 351448 will also be pursued. ..
  39. MOLECULAR MECHANISMS OF 5-HT RECEPTOR ACTIONS
    Bryan Roth; Fiscal Year: 2005
    ..A full molecular pharmacologic characterization of these compounds is essential prior to their use in humans. ..
  40. Selenium Prevention of Tobacco Smoke-Induced Lung Cancer
    Teresa Fan; Fiscal Year: 2005
    ..Biomarker characterization should reveal whether synergism is mediated via apoptosis. ..
  41. COBALT COMPLEXES OF MODIFIED NUCLEOSIDES, DINUCLEOSIDES
    Roman Dembinski; Fiscal Year: 2005
    ..Pursuing the leading structures of hexacarbonyl dicobalt complexes that exhibit activity against human mammary tumor cells, we will synthesize a library of new metallonucleosides and conduct structure-activity relationship studies. ..
  42. Yeast-Based Screening for Mammalian K Channel Modulators
    ELENA MAKINA; Fiscal Year: 2005
    ..It will also provide leads for future search for highly specific and potent K+ channel modulators for use as neuropharmacological agents. ..
  43. DEVELOPMENT OF LIGAND ASSISTED ASYMMETRIC SYNTHESES
    Arun Ghosh; Fiscal Year: 2001
    ..Besides the broad range of scope and generality, this line of research will provide excellent opportunities to teach and train graduate and undergraduate students in the laboratory. ..
  44. Assay Development for Identification of ER-NFkB Pathway Selective Agents
    KENDALL NETTLES; Fiscal Year: 2006
    ..Optimized chemical probes will be used for structural biology experiments to understand the mechanisms through which ER suppresses NFkB. ..
  45. PKC Modulators for the Treatment of Alzheimer's disease
    Alan Kozikowski; Fiscal Year: 2008
    ..For the best compounds from Aim 2, perform studies in triple transgenic mice to ascertain effects on Abeta and sAPPalpha levels and plaque formation in vivo. ..
  46. Chemistry and Pharmacology of a New Nicotine Ligands
    Alan Kozikowski; Fiscal Year: 2007
    ..Functional activity will be evaluated using established 86RbC1 efflux assays and/or whole cell patch clamp measurements. ..
  47. NEW DEVELOPMENTS IN ORGANOCOPPER CHEMISTRY
    R Dieter; Fiscal Year: 2004
    ..The proposed synthetic routes to pyrrolidine aza sugars will develop the potential synthetic power of alpha-aminoalkylcuprate chemistry. ..
  48. Prostanoid Modulation of Neuronal Death
    Noel Carlson; Fiscal Year: 2005
    ..abstract_text> ..