benzylidene compounds

Summary

Summary: Compounds containing the PhCH= radical.

Top Publications

  1. ncbi Synthesis and anti-tyrosine kinase activity of 3-(substituted-benzylidene)-1, 3-dihydro-indolin derivatives: investigation of their role against p60c-Src receptor tyrosine kinase with the application of receptor docking studies
    Sureyya Olgen
    Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Ankara, Tandogan Ankara 06100, Turkey
    Farmaco 60:497-506. 2005
  2. ncbi Diphenyl difluoroketone: a curcumin derivative with potent in vivo anticancer activity
    Dharmalingam Subramaniam
    Section of Digestive Diseases and Nutrition, Department of Medicine, University of Oklahoma Health Sciences Center, Oklahoma City, OK 73126, USA
    Cancer Res 68:1962-9. 2008
  3. ncbi Biochemical properties of mammalian neutral sphingomyelinase 2 and its role in sphingolipid metabolism
    Norma Marchesini
    Department of Biochemistry and Molecular Biology, Medical University of South Carolina, Charleston 29425, USA
    J Biol Chem 278:13775-83. 2003
  4. ncbi Selective alpha7-nicotinic acetylcholine receptor agonist GTS-21 improves survival in murine endotoxemia and severe sepsis
    Valentin A Pavlov
    Laboratory of Biomedical Science, The Feinstein Institute for Medical Research, Manhasset, NY, USA
    Crit Care Med 35:1139-44. 2007
  5. pmc Cholinergic agonists regulate JAK2/STAT3 signaling to suppress endothelial cell activation
    Prodyot K Chatterjee
    The Center for Immunology and Inflammation, The Feinstein Institute for Medical Research, Manhasset, New York, USA
    Am J Physiol Cell Physiol 297:C1294-306. 2009
  6. ncbi EF24 induces G2/M arrest and apoptosis in cisplatin-resistant human ovarian cancer cells by increasing PTEN expression
    Karuppaiyah Selvendiran
    Department of Internal Medicine, Davis Heart and Lung Research Institute and Comprehensive Cancer Center, The Ohio State University, Columbus, Ohio 43210, USA
    J Biol Chem 282:28609-18. 2007
  7. ncbi BZYX, a novel acetylcholinesterase inhibitor, significantly improved chemicals-induced learning and memory impairments on rodents and protected PC12 cells from apoptosis induced by hydrogen peroxide
    Jing Zhang
    Institute of Pharmacology and Toxicology, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China
    Eur J Pharmacol 613:1-9. 2009
  8. ncbi Inhibition of tumor necrosis factor-induced cell death in MCF7 by a novel inhibitor of neutral sphingomyelinase
    Chiara Luberto
    Department of Biochemistry, Medical University of South Carolina, 173 Ashley Avenue, Charleston, SC 29425, USA
    J Biol Chem 277:41128-39. 2002
  9. pmc Diphenyl difluoroketone: a potent chemotherapy candidate for human hepatocellular carcinoma
    Yingjian Liang
    Key Laboratory of Hepatosplenic Surgery, Department of General Surgery, The First Affiliated Hospital of Harbin Medical University, Ministry of Education, Harbin, Heilongjiang Province, People s Republic of China
    PLoS ONE 6:e23908. 2011
  10. pmc Inhibition of IkappaB kinase-nuclear factor-kappaB signaling pathway by 3,5-bis(2-flurobenzylidene)piperidin-4-one (EF24), a novel monoketone analog of curcumin
    Andrea L Kasinski
    Emory University School of Medicine, Atlanta, GA 30322, USA
    Mol Pharmacol 74:654-61. 2008

Research Grants

  1. Lipid Raft Microdomains in Neutrophil Function
    ROBERT GARY SITRIN; Fiscal Year: 2010
  2. The Urokinase-CD87 System in Macrophage Activation
    Robert Sitrin; Fiscal Year: 2004
  3. MOLECULAR NEUROBIOLOGY OF SCHIZOPHRENIA
    Robert Freedman; Fiscal Year: 2008
  4. Asymmetric Synthesis of Amino Acids and Amino Phosphonic Acids
    FRANKLIN DAVIS; Fiscal Year: 2007
  5. ASYMMETRIC SYNTHESIS OF BIOACTIVE PRIMARY AMINES
    FRANKLIN DAVIS; Fiscal Year: 2006
  6. Mouse model of binge drinking-induced neurotoxicity
    CHRISTOPHER DE FIEBRE; Fiscal Year: 2006
  7. Opiate Bivalent Ligands:Structure/Function Studies
    PHILIP PORTOGHESE; Fiscal Year: 2006
  8. The Genetics of Endophenotypes and Schizophrenia
    Ann Olincy; Fiscal Year: 2007
  9. Syntheses of Amino Acids and Amino Phosphonic Acids
    FRANKLIN DAVIS; Fiscal Year: 2005
  10. ELECTROPHYSIOLOGY OF SENSORY GATING IN SCHIZOPHRENIA
    Robert Freedman; Fiscal Year: 2004

Detail Information

Publications180 found, 100 shown here

  1. ncbi Synthesis and anti-tyrosine kinase activity of 3-(substituted-benzylidene)-1, 3-dihydro-indolin derivatives: investigation of their role against p60c-Src receptor tyrosine kinase with the application of receptor docking studies
    Sureyya Olgen
    Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Ankara, Tandogan Ankara 06100, Turkey
    Farmaco 60:497-506. 2005
    ..Among all of the compounds, only (Z)-3-(2'-Chloro-benzylidene)-1, 3-dihydro-indolin-2-one (8) and (E)-3-(3'-Nitro-benzylidene)-1, 3-dihydro-indolin-2-thione (16) were docked at the active site where the PP1 was embedded...
  2. ncbi Diphenyl difluoroketone: a curcumin derivative with potent in vivo anticancer activity
    Dharmalingam Subramaniam
    Section of Digestive Diseases and Nutrition, Department of Medicine, University of Oklahoma Health Sciences Center, Oklahoma City, OK 73126, USA
    Cancer Res 68:1962-9. 2008
    ..Taken together, these data suggest that the novel curcumin-related compound EF24 is a potent antitumor agent that induces caspase-mediated apoptosis during mitosis and has significant therapeutic potential for gastrointestinal cancers...
  3. ncbi Biochemical properties of mammalian neutral sphingomyelinase 2 and its role in sphingolipid metabolism
    Norma Marchesini
    Department of Biochemistry and Molecular Biology, Medical University of South Carolina, Charleston 29425, USA
    J Biol Chem 278:13775-83. 2003
    ..In conclusion, these results 1) show that nSMase2 is a structural gene for nSMase, 2) suggest that nSMase2 acts as a bona fide N-SMase in cells, and 3) implicate nSMase2 in the regulation of cell growth and cell signaling...
  4. ncbi Selective alpha7-nicotinic acetylcholine receptor agonist GTS-21 improves survival in murine endotoxemia and severe sepsis
    Valentin A Pavlov
    Laboratory of Biomedical Science, The Feinstein Institute for Medical Research, Manhasset, NY, USA
    Crit Care Med 35:1139-44. 2007
    ..Here we studied whether GTS-21, a selective alpha7-nicotinic acetylcholine receptor agonist, inhibits proinflammatory cytokines in vitro and in vivo and improves survival in murine endotoxemia and severe sepsis...
  5. pmc Cholinergic agonists regulate JAK2/STAT3 signaling to suppress endothelial cell activation
    Prodyot K Chatterjee
    The Center for Immunology and Inflammation, The Feinstein Institute for Medical Research, Manhasset, New York, USA
    Am J Physiol Cell Physiol 297:C1294-306. 2009
    ..Our results have significant implications for better understanding the therapeutic potential of cholinergic agonists for treating IL-6 mediated inflammatory conditions...
  6. ncbi EF24 induces G2/M arrest and apoptosis in cisplatin-resistant human ovarian cancer cells by increasing PTEN expression
    Karuppaiyah Selvendiran
    Department of Internal Medicine, Davis Heart and Lung Research Institute and Comprehensive Cancer Center, The Ohio State University, Columbus, Ohio 43210, USA
    J Biol Chem 282:28609-18. 2007
    ..Therefore, EF24 appears to have a potential therapeutic role in human ovarian cancer through the activation of PTEN...
  7. ncbi BZYX, a novel acetylcholinesterase inhibitor, significantly improved chemicals-induced learning and memory impairments on rodents and protected PC12 cells from apoptosis induced by hydrogen peroxide
    Jing Zhang
    Institute of Pharmacology and Toxicology, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China
    Eur J Pharmacol 613:1-9. 2009
    ..It is hopeful that BZYX becomes a potential candidate for use in the intervention for neurodegenerative diseases...
  8. ncbi Inhibition of tumor necrosis factor-induced cell death in MCF7 by a novel inhibitor of neutral sphingomyelinase
    Chiara Luberto
    Department of Biochemistry, Medical University of South Carolina, 173 Ashley Avenue, Charleston, SC 29425, USA
    J Biol Chem 277:41128-39. 2002
    ..In conclusion, our results indicate that N-SMase activation is a necessary step for the full development of the cytotoxic program induced by TNF...
  9. pmc Diphenyl difluoroketone: a potent chemotherapy candidate for human hepatocellular carcinoma
    Yingjian Liang
    Key Laboratory of Hepatosplenic Surgery, Department of General Surgery, The First Affiliated Hospital of Harbin Medical University, Ministry of Education, Harbin, Heilongjiang Province, People s Republic of China
    PLoS ONE 6:e23908. 2011
    ..Our study has offered a strategy that EF24 being a therapeutic agent for hepatocellular carcinoma...
  10. pmc Inhibition of IkappaB kinase-nuclear factor-kappaB signaling pathway by 3,5-bis(2-flurobenzylidene)piperidin-4-one (EF24), a novel monoketone analog of curcumin
    Andrea L Kasinski
    Emory University School of Medicine, Atlanta, GA 30322, USA
    Mol Pharmacol 74:654-61. 2008
    ..The effective inhibition of TNF-alpha-induced NF-kappaB signaling by EF24 extends the therapeutic application of EF24 to other NF-kappaB-dependent diseases, including inflammatory diseases such as rheumatoid arthritis...
  11. ncbi Targeting tissue factor-expressing tumor angiogenesis and tumors with EF24 conjugated to factor VIIa
    Mamoru Shoji
    Winship Cancer Institute, Emory University, Atlanta, GA 30322, USA
    J Drug Target 16:185-97. 2008
    ..It may also prove to be useful for treating drug-resistant tumors and micro-metastases in addition to primary tumors...
  12. pmc Comparative pharmacology of rat and human alpha7 nAChR conducted with net charge analysis
    Roger L Papke
    Department of Pharmacology and Therapeutics, Box 100267 JHMHSC, University of Florida, Gainesville, Florida, FL 32610 0267, USA
    Br J Pharmacol 137:49-61. 2002
    ..Since these concentrations are relatively non-desensitizing, the contribution of choline-activated alpha7 receptor current may play a significant role in the regulation of calcium homeostasis in alpha7-expressing neurons...
  13. pmc EF24, a novel curcumin analog, disrupts the microtubule cytoskeleton and inhibits HIF-1
    Shala L Thomas
    Department of Pharmacology, Emory University School of Medicine, Atlanta, Georgia, USA
    Cell Cycle 7:2409-17. 2008
    ....
  14. pmc Activation of the p38 pathway by a novel monoketone curcumin analog, EF24, suggests a potential combination strategy
    Shala L Thomas
    Emory University, Atlanta, GA 30322, USA
    Biochem Pharmacol 80:1309-16. 2010
    ..These studies offer a novel strategy that combines the curcumin analog EF24 with a p38 inhibitor for potentially enhanced therapy in the treatment of lung cancer...
  15. ncbi Hydroxy metabolites of the Alzheimer's drug candidate 3-[(2,4-dimethoxy)benzylidene]-anabaseine dihydrochloride (GTS-21): their molecular properties, interactions with brain nicotinic receptors, and brain penetration
    William R Kem
    Department of Pharmacology and Therapeutics, College of Medicine, University of Florida, Gainesville, FL 32610 0267, USA
    Mol Pharmacol 65:56-67. 2004
    ..Benzylidene anabaseines pharmacologically similar to the hydroxy metabolites, but which enter the brain more readily, may provide greater stimulation of alpha7 receptors in the whole organism...
  16. ncbi Mecamylamine reversal by nicotine and by a partial alpha7 nicotinic acetylcholine receptor agonist (GTS-21) in rabbits tested with delay eyeblink classical conditioning
    Diana S Woodruff-Pak
    Research and Technology Development, Albert Einstein Healthcare Network, Korman Suite 100, 5501 Old York Road, Philadelphia, PA 19141, USA
    Behav Brain Res 143:159-67. 2003
    ..Reversal of mecamylamine-induced learning deficits by nicotine and GTS-21 suggests that nAChR agonists may have efficacy in ameliorating deficits caused by the loss of some types of nAChRs in diseases such as AD...
  17. ncbi DMXB, an alpha7 nicotinic agonist, normalizes auditory gating in isolation-reared rats
    Heidi C O'Neill
    Department of Psychiatry C268 71, University of Colorado Health Sciences Center, 4200 East 9th Avenue, Denver, CO 80262, USA
    Psychopharmacology (Berl) 169:332-9. 2003
    ..3-(2,4)-Dimethoxybenzylidine anabaseine (DMXB; also known as GTS-21) is such an agonist and has shown efficacy in mice both orally and intraperitoneally...
  18. ncbi Alpha-7 nicotinic receptor agonists: potential new candidates for the treatment of schizophrenia
    Laura F Martin
    Department of Psychiatry, Department of Veterans Affairs and University of Colorado Health Sciences Center, 4200 East Ninth Avenue, C268 71, Denver, CO 80262, USA
    Psychopharmacology (Berl) 174:54-64. 2004
    ..This inhibitory process, which involves the alpha(7) nicotinic receptor mediated release of gamma-aminobutyric acid (GABA) by hippocampal interneurons, represents a potential new target for therapeutic intervention in schizophrenia...
  19. ncbi The structural basis for GTS-21 selectivity between human and rat nicotinic alpha7 receptors
    Clare Stokes
    Department of Pharmacology and Therapeutics, P O Box 100267, 1600 SW Archer Rd, University of Florida, College of Medicine, Gainesville, FL 32610, USA
    Mol Pharmacol 66:14-24. 2004
    ..Specific features in the agonist molecule itself are also identified that interact with these structural features of the receptor agonist binding site...
  20. 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...
  21. ncbi Synthesis and biological evaluation of 3-(substituted-benzylidene)-1,3-dihydro-indolin derivatives as human protein kinase CK2 and p60(c-Src) tyrosine kinase inhibitors
    Sureyya Olgen
    University of Ankara, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Turkey
    Biol Pharm Bull 30:715-8. 2007
    ..It was found that 3-(substituted-benzylidene)-1,3-dihydro-indolin-2-thione derivatives are more effective than indolin-2-one congeners for the inhibition of CK2 and p60(c-Src) tyrosine kinase...
  22. ncbi Are we finally taming inflammation?
    Rafael Bojalil
    Crit Care Med 35:1215-6. 2007
  23. ncbi Reversal of agonist selectivity by mutations of conserved amino acids in the binding site of nicotinic acetylcholine receptors
    Nicole A Horenstein
    Department of Pharmacology and Therapeutics, University of Florida College of Medicine, Gainesville, Florida 32610, USA
    J Biol Chem 282:5899-909. 2007
    ....
  24. ncbi Stimulation of alpha 7 cholinergic receptors inhibits lipopolysaccharide-induced neutrophil recruitment by a tumor necrosis factor alpha-independent mechanism
    Ida A J Giebelen
    Center for Infection and Immunity Amsterdam CINIMA, University of Amsterdam, Amsterdam, The Netherlands
    Shock 27:443-7. 2007
    ..These data identify a novel anti-inflammatory effect of chemical alpha7 cholinergic receptor stimulation that is independent from its capacity to inhibit TNF-alpha production...
  25. ncbi The consequences of reducing expression of the alpha7 nicotinic receptor by RNA interference and of stimulating its activity with an alpha7 agonist in SH-SY5Y cells indicate that this receptor plays a neuroprotective role in connection with the pathogenes
    Xiao lan Qi
    Department of Pathology and Molecular Biology, Guiyang Medical University, Guiyang 550004, Guizhou, PR China
    Neurochem Int 51:377-83. 2007
    ....
  26. ncbi Distinct profiles of alpha7 nAChR positive allosteric modulation revealed by structurally diverse chemotypes
    Jens Halvard Grønlien
    Oslo Research Park, Oslo, Norway
    Mol Pharmacol 72:715-24. 2007
    ..In summary, our studies reveal two distinct alpha7 PAM profiles, which could offer unique opportunities for modulating alpha7 nAChRs in vivo and in the development of novel therapeutics for central nervous system indications...
  27. pmc Synthesis and positron emission tomography studies of C-11-labeled isotopomers and metabolites of GTS-21, a partial alpha7 nicotinic cholinergic agonist drug
    Sung Won Kim
    Medical Department, Brookhaven National Laboratory, Upton, NY 11973, USA
    Nucl Med Biol 34:541-51. 2007
    ..One of its two major demethylated metabolites, 4-OH-GTS-21, has been suggested to contribute to its therapeutic effects...
  28. ncbi Local stimulation of alpha7 cholinergic receptors inhibits LPS-induced TNF-alpha release in the mouse lung
    Ida A J Giebelen
    Center for Infection and Immunity Amsterdam CINIMA, Academic Medical Center, University of Amsterdam, Amsterdam, The Netherlands
    Shock 28:700-3. 2007
    ..These data indicate that local administration of GTS-21 inhibits TNF-alpha release in the lung during LPS-induced inflammation...
  29. ncbi alpha7 Nicotinic acetylcholine receptor as a target to rescue deficit in hippocampal LTP induction in beta-amyloid infused rats
    Ling Chen
    ICORP SORST Cell Mechanosensing, JST, Nagoya University Graduate School of Medicine, 65 Tsurumai Cho, Showa Ku, Nagoya 466 8550, Japan
    Neuropharmacology 50:254-68. 2006
    ..These results suggest that Abeta-impaired LTP and PPF arise as a consequence of dysfunctional alpha7nAChR, and that alpha7nAChR may be an important target to help ameliorate AD patient cognitive deficits...
  30. ncbi Theoretical studies of Alzheimer's disease drug candidate 3-[(2,4-dimethoxy)benzylidene]-anabaseine (GTS-21) and its derivatives
    Dong Qing Wei
    Tianjin Institute of Bioinformatics and Drug Discoveries, Tianjin Normal University, Tianjin 300074, China
    Biochem Biophys Res Commun 338:1059-64. 2005
    ..Our studies, in combination with experimental studies, will lead to a promising basis for practical drug design against Alzheimer's disease...
  31. ncbi A phase I pharmacokinetic study of HMN-214, a novel oral stilbene derivative with polo-like kinase-1-interacting properties, in patients with advanced solid tumors
    Linda L Garland
    Arizona Cancer Center, University of Arizona, Tucson, Arizona 85724, USA
    Clin Cancer Res 12:5182-9. 2006
    ..We conducted a dose escalation study of HMN-214 in patients with advanced cancer to assess the safety profile and pharmacokinetics of HMN-214 and to establish the maximum tolerated dose...
  32. ncbi Presynaptic modulation of synaptic transmission by pregnenolone sulfate as studied by optical recordings
    Ling Chen
    International Cooperative Research Project Solution Oriented Research for Science and Technology Cell Mechanosensing, Japan Science and Technology Agency, Nagoya
    J Neurophysiol 94:4131-44. 2005
    ....
  33. pmc Initial phase 2 trial of a nicotinic agonist in schizophrenia
    Robert Freedman
    Department of Psychiatry, Denver VA Medical Center and University of Colorado, Denver, CO 80262, USA
    Am J Psychiatry 165:1040-7. 2008
    ..The agent 3-(2,4-dimethoxybenzylidene) anabaseine (DMXB-A) is a partial alpha(7)-nicotinic agonist and can be taken orally. A phase 1 trial showed evidence for cognitive enhancement in schizophrenia...
  34. ncbi Relating neuronal nicotinic acetylcholine receptor subtypes defined by subunit composition and channel function
    Qiang Nai
    Department of Anatomy and Neurobiology, Medical College of Ohio, Toledo, Ohio 43614, USA
    Mol Pharmacol 63:311-24. 2003
    ..By linking structural to functional nAChR subtypes, the findings also illustrate a useful pharmacological strategy for selectively targeting nAChRs...
  35. ncbi Prediction of plasma concentration of GTS-21 in hairless rats following monolithic transdermal delivery
    Hideki Kawamata
    Department of Biochemical Science and Engineering, College of Computer Science and Systems Engineering, Kyusyu Institute of Technology, Kawazu, Iizuka, Japan
    Biol Pharm Bull 25:342-5. 2002
    ....
  36. ncbi Electronic excitations of green fluorescent proteins: protonation states of chromophore model compound in solutions
    Daiqian Xie
    Department of Chemistry, Institute of Theoretical and Computational Chemistry, Nanjing University, Nanjing, 210093, People s Republic of China
    J Comput Chem 26:1487-96. 2005
    ..Some technical problems related to the computation of electronic excitations within the HBMIA at the anionic state are also discussed...
  37. ncbi Alpha 7 nicotinic acetylcholine receptor-mediated protection against ethanol-induced neurotoxicity
    Nancyellen C de Fiebre
    Department of Pharmacology and Neuroscience, University of North Texas Health Science Center, 3500 Camp Bowie Boulevard, Fort Worth, TX 76107 2699, USA
    Alcohol 31:149-53. 2003
    ..These results support the suggestion that nicotinic partial agonists may be useful in treating binge drinking-induced neurotoxicity and may provide clues as to why heavy drinkers are usually smokers...
  38. ncbi Alpha7 nicotinic receptor activation inhibits ethanol-induced mitochondrial dysfunction, cytochrome c release and neurotoxicity in primary rat hippocampal neuronal cultures
    Yangxin Li
    Department of Internal Medicine, School of Medicine, Southern Illinois University, Springfield, IL 62707, USA
    J Neurochem 81:853-8. 2002
    ....
  39. ncbi Inverse agonists and neutral antagonists at mu opioid receptor (MOR): possible role of basal receptor signaling in narcotic dependence
    D Wang
    Department of Biopharmaceutical Sciences and Pharmaceutical Chemistry, and Wheeler Center for Neurobiology of Addiction, University of California San Francisco, 94143-0446, USA
    J Neurochem 77:1590-600. 2001
    ..Neutral antagonists have promise in treatment of narcotic addiction...
  40. ncbi Signal transduction of opioid-induced cardioprotection in ischemia-reperfusion
    B C McPherson
    Department of Anesthesia and Critical Care, The University of Chicago, Illinois, USA
    Anesthesiology 94:1082-8. 2001
    ..CONCLUSION: Stimulation of delta1-opioid receptors generates oxygen radicals via mitochondrial KATP channels. This signaling pathway attenuates oxidant stress and cell death in cardiomyocytes...
  41. ncbi Delta-opioid receptor-induced late preconditioning is mediated by cyclooxygenase-2 in conscious rabbits
    Eitaro Kodani
    Experimental Research Laboratory, Division of Cardiology, University of Louisville and Jewish Heart and Lung Institute, Louisville, KY 40292, USA
    Am J Physiol Heart Circ Physiol 283:H1943-57. 2002
    ..These results demonstrate that activation of delta-opioid receptors induces late PC against both stunning and infarction via a COX-2-dependent mechanism...
  42. ncbi Deltorphin II enhances extracellular levels of dopamine in the nucleus accumbens via opioid receptor-independent mechanisms
    Kaoru Murakawa
    Department of Pharmacology, Nihon University School of Dentistry, 1 8 13 Kanda Surugadai, Chiyoda, Tokyo, 101 8310, Japan
    Eur J Pharmacol 491:31-6. 2004
    ..These results suggest that deltorphin II enhances extracellular dopamine in the nucleus accumbens via opioid receptor-independent, tetrodotoxin-sensitive mechanisms...
  43. ncbi Screening for new agonists against Alzheimer's disease
    Huiqin Zheng
    College of Life Sciences and Technology, Shanghai Jiaotong University, Minhang District, Shanghai, China
    Med Chem 3:488-93. 2007
    ..Finally, it was found through an in-depth structural analysis that Mol 7235 might be a promising candidate for further modification by experiments to make it become an effective drug for treating Alzheimer's disease...
  44. ncbi Interactions among mu- and delta-opioid receptors, especially putative delta1- and delta2-opioid receptors, promote dopamine release in the nucleus accumbens
    N Hirose
    Department of Dental Anaesthesiology, Nihon University School of Dentistry, 1 8 13, Kanda Surugadai, Chiyoda ku, Tokyo 101 8310, Japan
    Neuroscience 135:213-25. 2005
    ....
  45. ncbi Repeated delta1-opioid receptor stimulation reduces delta2-opioid receptor responses in the SA node
    S H Deo
    Dept of Integrative Physiology, Univ of North Texas Health Science Center, 3500 Camp Bowie Blvd, Fort Worth TX 76107, USA
    Am J Physiol Heart Circ Physiol 291:H2246-54. 2006
    ....
  46. ncbi Immunosuppression by delta-opioid antagonist naltrindole: delta- and triple mu/delta/kappa-opioid receptor knockout mice reveal a nonopioid activity
    C Gaveriaux-Ruff
    CNRS UPR 9050, ESBS, Universite Louis Pasteur, Illkirch, France
    J Pharmacol Exp Ther 298:1193-8. 2001
    ..Therefore, the postulated inhibitory activity of naltrindole in the graft rejection process is mediated by a target, which remains to be discovered...
  47. ncbi BW373U86, a delta opioid agonist, partially mediates delayed cardioprotection via a free radical mechanism that is independent of opioid receptor stimulation
    H H Patel
    Medical College of Wisconsin, Department of Pharmacology and Toxicology, Milwaukee, WI 53226, USA
    J Mol Cell Cardiol 33:1455-65. 2001
    ..Furthermore, it is the early burst in OFRs that is crucial to initiating the protective effect...
  48. pmc Spectroscopic analysis of benzylidene anabaseine complexes with acetylcholine binding proteins as models for ligand-nicotinic receptor interactions
    Todd T Talley
    Department of Pharmacology, University of California, San Diego, La Jolla, California 92093 0636, USA
    Biochemistry 45:8894-902. 2006
    ....
  49. ncbi Cardiac enkephalins interrupt vagal bradycardia via delta 2-opioid receptors in sinoatrial node
    Martin Farias
    Department of Integrative Physiology, University of North Texas Health Science Center, 3500 Camp Bowie Boulevard, Fort Worth, TX 76107, USA
    Am J Physiol Heart Circ Physiol 284:H1693-701. 2003
    ..These data also support the existence of vagotonic delta(1)-opioid receptors also in the sinoatrial node...
  50. ncbi Methionine-enkephalin modulation of hydrogen peroxide (H2O2) release by rat peritoneal macrophages involves different types of opioid receptors
    Stanislava Stanojevic
    Institute of Virology, Vaccines and Sera Torlak, Immunology Research Centre Branislav Jankovic, Vojvode Stepe 458, 11152 Belgrade, Serbia
    Neuropeptides 42:147-58. 2008
    ....
  51. ncbi Comparison of receptor mechanisms and efficacy requirements for delta-agonist-induced convulsive activity and antinociception in mice
    Daniel C Broom
    Department of Pharmacology, University of Michigan Medical School, 1150 West Medical Center Drive, Ann Arbor, MI 48109 0632, USA
    J Pharmacol Exp Ther 303:723-9. 2002
    ....
  52. ncbi Selectivity of delta- and kappa-opioid ligands depends on the route of central administration in mice
    Mary M Lunzer
    Department of Medicinal Chemistry, University of Minnesota, 308 Harvard St S E, Minneapolis, MN 55455, USA
    J Pharmacol Exp Ther 322:166-71. 2007
    ..In view of the observed tissue-dependent selectivity, we suggest that multiple opioid antagonists be employed routinely in establishing agonist selectivity in vivo...
  53. ncbi Different effects of opioid antagonists on mu-, delta-, and kappa-opioid receptors with and without agonist pretreatment
    Danxin Wang
    Department of Pharmacology, School of Medicine and Public Health, The Ohio State University, 333 West 10th Ave, Columbus, OH 43210, USA
    J Pharmacol Exp Ther 321:544-52. 2007
    ..Activity profiles at the three opioid receptors under different conditions could lead to antagonists with optimal clinical properties in treatment of addiction and adverse opioid effects...
  54. ncbi Comparison of some 3-(substituted-benzylidene)-1,3-dihydroindolin derivatives as ligands of tyrosine kinase based on binding mode studies and biological assay
    Sureyya Olgen
    Department of Pharmaceutical Chemistry Faculty of Pharmacy, University of Ankara, 06100 Tandodan, Ankara, Turkey
    Arch Pharm Res 29:1006-17. 2006
    ....
  55. ncbi Reductive ring opening of o-nitrobenzylidene acetals of monosaccharides: synthesis and photolysis of some photolabile sugars
    S Watanabe
    Department of Biomolecular Science, Faculty of Science, Toho University, 2-2-1 Miyama, Funabashi, Chiba 274-8510, Japan
    Org Lett 3:255-7. 2001
    ..The photolabile sugars obtained were deprotected by irradiation at 350 nm to afford methylglycosides...
  56. ncbi Synthesis, structure, and bioactivity of N'-substituted benzylidene-3,4,5-trimethoxybenzohydrazide and 3-acetyl-2-substituted phenyl-5-(3,4,5-trimethoxyphenyl)-2,3-dihydro-1,3,4-oxadiazole derivatives
    Linhong Jin
    Center for Research and Development of Fine Chemicals, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Guiyang, Guizhou 550025, PR China
    Bioorg Med Chem Lett 16:5036-40. 2006
    ..The IC(50) values of high active compounds 2a, 2b, 2c, 2f, 3l, and 3m against PC3 cells were 0.2, 1.8, 0.2, 1.2, 1.7, and 0.3muM, respectively...
  57. ncbi [Color reactions for identification of nalidixic acid]
    K Görlitzer
    Institut fur Pharmazeutische Chemie, Technischen Universität Braunschweig, Germany
    Pharmazie 55:17-21. 2000
    ..The 7-methyl group of 1 condenses with vanillin (2) and Ehrlich's reagent (4) to the coloured (E)-benzylidene compounds 3 and 5...
  58. ncbi Studies on tellurium-containing heterocycles. Part 20. Reactions of 2-benzoselenopyrylium salts and 2-benzotelluropyrylium salts with nucleophiles: formation of 1-functionalized 1H-isoselenochromenes and 1H-isotellurochromenes
    Haruki Sashida
    Faculty of Pharmaceutical Sciences, Hokuriku University, Kanagawa machi, Kanazawa 920 1181, Japan
    Chem Pharm Bull (Tokyo) 52:57-62. 2004
    ..The 1-benzylselenopyrylium salts (19A) and 1-benzyltelluropyrylium salts (19B) exist in the solvent as an equilibrium mixture of the salts (19) and the corresponding (Z)-benzylidene compounds (20).
  59. ncbi (18)F-Labeled benzylideneaniline derivatives as new ligands for beta-amyloid plaque imaging in Alzheimer's disease
    Hak Jeong Lee
    Department of Nuclear Medicine, Seoul National University College of Medicine and Institute of Radiation Medicine, Jongno gu, Seoul 110 744, South Korea
    Nucl Med Biol 36:107-16. 2009
    ..We herein describe the synthesis of (18)F-labeled benzylideneaniline derivatives using a novel labeling approach for imaging Abeta plaques in AD patients...
  60. ncbi Enzyme-like effect of metmyoglobin on the thermal cis-trans isomerization of stilbazolium betaine
    A V Pastukhov
    Institute of Problems of Chemical Physics, Russian Academy of Sciences, Chernogolovka, Moscow Region
    J Biol Inorg Chem 5:307-12. 2000
    ..Possible mechanisms of the reaction acceleration are considered...
  61. ncbi Synthesis, spectroscopic characterization and crystal structure of novel NNNN-donor μ-bis(bidentate) tetraaza acyclic Schiff base ligands
    Mohammad Hossein Habibi
    Department of Chemistry, University of Isfahan, Isfahan 81746 73441, Islamic Republic of Iran
    Spectrochim Acta A Mol Biomol Spectrosc 98:396-404. 2012
    ..The synthesized ligands have been characterized on the basis of the results of cyclic voltammetry (CV) and spectroscopic studies viz. FT-IR spectroscopy (FT-IR), mass spectroscopy (MS) and UV-Vis spectroscopy (UV-Vis)...
  62. ncbi Tandem Ru-alkylidene-catalysed cross metathesis/hydrogenation: synthesis of lipophilic amino acids
    Zhen J Wang
    School of Chemistry, Monash University, Wellington Road, Melbourne, 3800, Victoria, Australia
    J Pept Sci 19:470-6. 2013
    ..The resultant unsaturated analogues can be then optionally hydrogenated under mild reaction conditions by using the spent metathesis catalyst...
  63. ncbi Inhibition of Candida albicans isocitrate lyase activity by cadiolides and synoilides from the ascidian Synoicum sp
    Chan Hong Ahn
    Department of Agricultural Biotechnology, College of Agriculture and Life Sciences, Seoul National University, 1 Gwanak ro, Gwanak Gu, Seoul 151 921, Republic of Korea
    Bioorg Med Chem Lett 23:4099-101. 2013
    ..62, 17.16, and 10.36 μM, respectively. Growth phenotype of ICL deletion mutants and Northern blot analysis data indicated that compound 1 inhibits the ICL expression in C. albicans under C2 carbon utilizing condition...
  64. ncbi Cholinergic receptors modulate immune complex-induced inflammation in vitro and in vivo
    Milena Vukelic
    Program in Inflammation and Autoimmunity, Hospital for Special Surgery, Weill Cornell Medical College, New York, NY 10021, USA
    J Immunol 191:1800-7. 2013
    ..Taken together, these findings suggest that cholinergic output has the potential to exert tonic inhibitory activity that dampens responses to ICs and C5a and thus may be a target to minimize tissue damage in autoimmune diseases. ..
  65. ncbi Synthesis and characterization of bis[N'-(4-carboxybenzylidene)]-pyridine-2,6-dicarbohydrazide: colorimetric and fluorometric modulation in presence of F- ions
    Priti Sinha
    Department of Chemistry, Faculty of Science, Banaras Hindu University, Varanasi 221 005, India
    Spectrochim Acta A Mol Biomol Spectrosc 116:286-94. 2013
    ..The theoretical calculations agreed to the experimental results...
  66. ncbi The monosialosyl ganglioside GM-1 reduces the vagolytic efficacy of delta2-opioid receptor stimulation
    Shavsha Davis
    Univ of North Texas Health Science Center, Dept of Integrative Physiology, 3500 Camp Bowie Boulevard, Fort Worth, TX 76107
    Am J Physiol Heart Circ Physiol 291:H2318-26. 2006
    ..The data support the hypothesis that delta(1)-receptor stimulation may reduce delta(2)-vagolytic responses by stimulating the GM-1 synthesis...
  67. ncbi FT-IR, FT-Raman and computational study of (E)-N-carbamimidoyl-4-((4-methoxybenzylidene)amino)benzenesulfonamide
    Asha Chandran
    Department of Chemistry, TKM College of Arts and Science, Kollam, Kerala, India
    Spectrochim Acta A Mol Biomol Spectrosc 92:84-90. 2012
    ..The geometrical parameters of the title compound are in agreement with that of reported similar derivatives...
  68. pmc Acute and chronic heroin dependence in mice: contribution of opioid and excitatory amino acid receptors
    Gad Klein
    Neuropsychology Doctoral Subprogram, Queens College, City University of New York, Flushing, NY 11367, USA
    Eur J Pharmacol 586:179-88. 2008
    ..Elucidating the substrates contributing to heroin dependence, and identifying their similarities and differences with those of other opioids such as morphine, may yield effective treatment strategies to the problem of heroin dependency...
  69. ncbi Glucocorticoid analogues: potential therapeutic alternatives for treating inflammatory muscle diseases
    Erica K M Reeves
    ReveraGen BioPharma, Inc, Rockville, MD, USA
    Endocr Metab Immune Disord Drug Targets 12:95-103. 2012
    ..In this review, we discuss molecular effects of currently prescribed GCs on skeletal muscle and also discuss the current state of development of GC analogues as alternative therapeutics for inflammatory muscle diseases...
  70. ncbi Near-infrared fluorescence amplified organic nanoparticles with aggregation-induced emission characteristics for in vivo imaging
    Junlong Geng
    Department of Chemical and Biomolecular Engineering, National University of Singapore, Singapore 117576
    Nanoscale 6:939-45. 2014
    ....
  71. ncbi Identity of the putative delta1-opioid receptor as a delta-kappa heteromer in the mouse spinal cord
    Philip S Portoghese
    Department of Medicinal Chemistry, College of Pharmacy, University of Minnesota, 308 Harvard Street, S E, Minneapolis, MN 55455, USA
    Eur J Pharmacol 467:233-4. 2003
    ..Studies with selective opioid receptor (ant)agonists support this conclusion...
  72. ncbi Neutral sphingomyelinase 2 induces dopamine uptake through regulation of intracellular calcium
    Seok Kyun Kim
    Department of Environmental and Health Chemistry, Chung Ang University, Dongjak Ku, Seoul, South Korea
    Cell Signal 22:865-70. 2010
    ..Taken together, these data suggest that nSMase2 may increase DA uptake through inducing ceramide production and thereby decreasing intracellular calcium levels...
  73. pmc Functional magnetic resonance imaging of effects of a nicotinic agonist in schizophrenia
    Jason R Tregellas
    Department of Psychiatry, Denver VA Medical Center VISN19 MIRECC and University of Colorado Denver, Aurora, CO 80045, USA
    Neuropsychopharmacology 35:938-42. 2010
    ..Imaging of drug response is useful in planning future clinical tests of this compound and other nicotinic agonists for schizophrenia...
  74. ncbi QSAR investigations on benzylideneamino and phenyliminomethyl scaffolds for selective COX-2 inhibiton: a Hansch approach
    E Manivannan
    School of Pharmacy, Devi Ahilya Vishwavidyalaya, Ring Road, Indore 452 017, M P, India
    Med Chem 5:440-5. 2009
    ..The derived results reveal the important structural features significant for improved COX-2 inhibitory activity and selectivity of these novel aryl sulfonamides...
  75. pmc Lewis acid-catalyzed diastereoselective hydroarylation of benzylidene malonic esters
    Shaofeng Duan
    Department of Chemistry, 1251 Wescoe Hall Drive, 2010 Malott Hall, and the KU Chemical Methodologies and Library Development Center of Excellence, The University of Kansas, Lawrence, Kansas 66045 7582, USA
    J Org Chem 74:4612-4. 2009
    ..Ultimately, 3,4-disubstituted dihydrocoumarins are obtained via a hydroarylation-lactonization sequence. Moreover, the dihydrocoumarins are formed with a high degree of diastereoselectivity favoring the trans stereoisomer...
  76. ncbi A novel bis-benzylidenecyclopentanone derivative, BPR0Y007, inducing a rapid caspase activation involving upregulation of Fas (CD95/APO-1) and wild-type p53 in human oral epidermoid carcinoma cells
    Shin Hun Juang
    Cancer Cooperative Ward in National Taiwan University Hospital, Division of Cancer Research, National Health Research Institutes, 7, Chung Shan Road, Taipei, Taiwan, ROC
    Biochem Pharmacol 68:293-303. 2004
    ..Overall, our results demonstrated that the BPR0Y007 could induce an early cytotoxic apoptosis through a caspase-8-dependent but mitochondrial-caspase-9 independent pathway, and involving upregulation of p53...
  77. ncbi An unexpected silver triflate-catalyzed tandem reaction of N'-(2-alkynylbenzylidene)hydrazide with ketene
    Gang Liu
    Department of Chemistry, Fudan University, 220 Handan Road, Shanghai 200433, China
    Chem Commun (Camb) 48:7049-51. 2012
    ..This reaction proceeds efficiently to generate the molecular complexity with the formation of four bonds in a one-pot procedure...
  78. ncbi Intragastric DMXB-A, an alpha7 nicotinic agonist, improves deficient sensory inhibition in DBA/2 mice
    J K Simosky
    Department of Pharmacology, University of Colorado Health Sciences Center, Denver, Colorado 80262, USA
    Biol Psychiatry 50:493-500. 2001
    ..These studies agree with results from previous studies with subcutaneously administered DMXB-A...
  79. ncbi Effects at a distance in alpha 7 nAChR selective agonists: benzylidene substitutions that regulate potency and efficacy
    Roger L Papke
    Department of Pharmacology and Therapeutics, University of Florida, PO Box 100267 JHMHSC, Gainesville, FL 32610 0267, USA
    Neuropharmacology 46:1023-38. 2004
    ....
  80. ncbi Tumor-specific cytotoxicity and type of cell death induced by sodium 5,6-benzylidene-L-ascorbate
    Kaori Kishino
    Division of Pharmacology, Meikai University School of Dentistry, Sakado, Saitama, Japan
    Anticancer Res 28:2577-84. 2008
    ..The present study suggests that SBA induces various degrees of autophagic cell death, followed by either necrosis or apoptosis at laters stage, depending on the cell type...
  81. ncbi 2-O-propargyl ethers: readily cleavable, minimally intrusive protecting groups for beta-mannosyl donors
    David Crich
    Department of Chemistry, University of Illinois at Chicago, 845 West Taylor Street, Chicago, Illinois 60607 7061, USA
    Org Lett 7:2277-80. 2005
    ..Deprotection is conducted by treatment with potassium tert-butoxide followed by catalytic osmium tetroxide and N-methylmorpholine N-oxide...
  82. ncbi Reductive openings of benzylidene acetals. Kinetic studies of borane and alane activation by Lewis acids
    Richard Johnsson
    Organic Chemistry, Lund University, PO Box 124, SE 221 00 Lund, Sweden
    Carbohydr Res 343:2997-3000. 2008
    ..These results correlate well with the concept of regioselectivity by activation of borane complexes...
  83. ncbi Synthesis of 3-azido-3-deoxy-beta-D-galactopyranosides
    Christopher T Oberg
    Organic Chemistry, Lund University, PO Box 124, SE 22100 Lund, Sweden
    Carbohydr Res 344:1282-4. 2009
    ....
  84. pmc Lipopolysaccharide upregulates α7 acetylcholine receptors: stimulation with GTS-21 mitigates growth arrest of macrophages and improves survival in burned mice
    Mohammed Abdul Sattar Khan
    Department of Anesthesia, Critical Care and Pain Medicine, Shriners Hospitals for Children, Massachusetts General Hospital and Harvard Medical School, Boston, Massachusetts, USA
    Shock 38:213-9. 2012
    ..The in vivo beneficial effects of GTS-21 in burn injury warrant further studies...
  85. pmc Domain structures in nematic liquid crystals on a polycarbonate surface
    Alexander M Parshin
    Kirensky Institute of Physics, Russian Academy of Sciences, Siberian Branch, Krasnoyarsk Scientific Center, Krasnoyarsk 660036, Russia
    Int J Mol Sci 14:16303-20. 2013
    ..The observed textures are compared with different combinations of the volume LC orientations and the radial distribution of the director field and the disclination lines at the polycarbonate surface. ..
  86. pmc Cardiopulmonary arrest and resuscitation disrupts cholinergic anti-inflammatory processes: a role for cholinergic α7 nicotinic receptors
    Greg J Norman
    Department of Psychology, The Ohio State University, Columbus, Ohio 43210, USA
    J Neurosci 31:3446-52. 2011
    ..Furthermore, we provide evidence that pharmacological activation of α7 nicotinic acetylcholine receptors provide significant protection against ischemia-related cell death and inflammation within a clinically relevant time frame...
  87. ncbi Discovery of novel benzylidene-1,3-thiazolidine-2,4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases
    Les A Dakin
    Oncology iMed Sciences Group, AstraZeneca R and D Boston, 35 Gatehouse Drive, Waltham, MA 02451, USA
    Bioorg Med Chem Lett 22:4599-604. 2012
    ..The synthesis and SAR of these compounds are described, along with X-ray crystallographic, anti-proliferative, and selectivity data...
  88. ncbi Opioid peptide deltorphin II simulates the cardioprotective effect of ischemic preconditioning: role of δ₂-opioid receptors, protein kinase C, and K(ATP) channels
    L N Maslov
    Institute of Cardiology, Siberian Division of the Russian Academy of Medical Sciences, Tomsk, Russia
    Bull Exp Biol Med 149:591-3. 2010
    ..The infarct-limiting effect of deltorphin II was not observed after inhibition of protein kinase C or blockade of mitochondrial K(ATP) channels...
  89. ncbi Structural conformations and density functional study on the intramolecular charge transfer based on vibrational spectra of 2,4-dihydroxy-N'-(4-methoxybenzylidene)benzohydrazide
    D M Suresh
    Government Arts College, Stone Hill House, Udhagamandalam, The Nilgiris 643 002, Tamilnadu, India
    Spectrochim Acta A Mol Biomol Spectrosc 110:157-68. 2013
    ..The broadening of the band at 1631 cm(-1) and the appearance of the band at 1556 cm(-1) strongly suggests the existence of proton equilibrium...
  90. pmc Withanolide D induces apoptosis in leukemia by targeting the activation of neutral sphingomyelinase-ceramide cascade mediated by synergistic activation of c-Jun N-terminal kinase and p38 mitogen-activated protein kinase
    Susmita Mondal
    Infectious Diseases and Immunology Division, Indian Institute of Chemical Biology, A Unit of Council of Scientific and Industrial Research, Govt, of India 4, Raja S, C, Mullick Road, Kolkata 700032, India
    Mol Cancer 9:239. 2010
    ..Manipulation in ceramide production by physiological and pharmacological modulators therefore will give additive effect in leukemia chemotherapy...
  91. pmc Anticancer activity of an imageable curcuminoid 1-[2-aminoethyl-(6-hydrazinopyridine-3-carbamidyl)-3,5-bis-(2-fluorobenzylidene)-4-piperidone (EFAH)
    Pallavi Lagisetty
    Department of Pharmaceutical Sciences and Small Animal Imaging Facility, University of Oklahoma Health Science Center, 1110 N, Stonewall Avenue, Oklahoma City, OK 73117, USA
    Chem Biol Drug Des 79:194-201. 2012
    ..For the first time, a visual biodisposition of EF24 in a live animal model has been demonstrated. Such knowledge could be of benefit in developing therapeutic curcuminoids, such as EF24...
  92. ncbi Synthesis of fluorescent analogues of the anticancer natural products 4-hydroxyphenylmethylene hydantoin and delta-tocotrienol
    Mudit Mudit
    Department of Basic Pharmaceutical Sciences, College of Pharmacy, 1800 Bienville Drive, University of Louisiana at Monroe, Monroe, Louisiana 71201, USA
    Nat Prod Commun 5:1623-6. 2010
    ..Both 2 and 4 retained good anti-migratory and antiproliferative activities, respectively. Fluorescent analogues 2 and 4 can be used for the identification of molecular targets of 1 and 3 in tumor cell cultures...
  93. ncbi Possible involvement of protein-tyrosine kinases such as p72syk in the disc-sphere change response of porcine platelets
    H Maeda
    Department of Biochemistry, Fukui Medical School
    J Biochem 117:1201-8. 1995
    ..These lines of evidence suggest that the activation of protein-tyrosine kinases such as p72syk may be involved in the disc-sphere change response in thromboxane A2-stimulated porcine platelets...
  94. ncbi Modulation of myofilament Ca2+ densitivity by delta- and kappa-opioid agonists in intact guinea pig hearts
    Yuri Nakae
    Department of Anesthesiology, Sapporo Medical University School of Medicine, Japan
    Anesth Analg 96:733-9, table of contents. 2003
    ..delta- and kappa-opioid agonists enhance myofilament Ca(2+) sensitivity despite decreasing available [Ca(2+)](i) in intact isolated guinea pig hearts, and these effects are mediated by delta- and kappa-opioid receptor stimulation...
  95. ncbi Structure-activity relationships of benzylidene anabaseines in nicotinic acetylcholine receptors of cockroach nerve cords
    Israt Sultana
    Department of Life Science and Biotechnology, Faculty of Life and Environmental Science, Shimane University, Matsue, Shimane 690 8504, Japan
    Bioorg Med Chem 10:2963-71. 2002
    ..High-affinity analogues of CBA might be suitable probes for use in classifying and characterizing insect nAChR subtypes...
  96. ncbi A total synthesis of hydroxylysine in protected form and investigations of the reductive opening of p-methoxybenzylidene acetals
    Tomas Gustafsson
    Organic Chemistry, Department of Chemistry, Umea University, SE 901 87 Umea, Sweden
    J Org Chem 69:8694-701. 2004
    ....
  97. ncbi Direct preconditioning of cardiac myocytes via opioid receptors and KATP channels
    B T Liang
    Department of Medicine, Cardiovascular Division, University of Pennsylvania Medical Center, Philadelphia, PA 19104, USA
    Circ Res 84:1396-400. 1999
    ..These results provide direct evidence that the preconditioning-like effect of morphine in the intact heart can be exerted at the level of cardiac myocytes and is most likely the result of mitochondrial KATP channel activation...
  98. ncbi Synthesis of aryl aldimines and their activity against fungi of clinical interest
    Cleiton M da Silva
    Grupo de Estudos em Química Orgânica e Biológica GEQOB, Departamento de Quimica, ICEx, Universidade Federal de Minas Gerais, Belo Horizonte, MG, 31270 901, Brazil
    Chem Biol Drug Des 78:810-5. 2011
    ..The aryl aldimines 2-(benzylideneamino)phenol (3) and 4-(benzylideneamino)phenol (8) were the most active compounds against the fungi studied. Compounds 3 and 8 efficiently inhibited the metabolism of C. neoformans mature biofilm...
  99. pmc Point-to-point ligand-receptor interactions across the subunit interface modulate the induction and stabilization of conformational states of alpha7 nAChR by benzylidene anabaseines
    Matthew D Isaacson
    Department of Pharmacology and Therapeutics, University of Florida College of Medicine, P O Box 100267, Gainesville, FL 32610, United States
    Biochem Pharmacol 85:817-28. 2013
    ..These results indicate that the fine-tuning of agonists for specific interaction with S36 can facilitate the development of therapeutics with targeted effects on ion channel desensitization properties and conformational state stability...
  100. ncbi 5-benzylidenerhodanine and 5-benzylidene-2-4-thiazolidinedione based antibacterials
    Ondrej Zvarec
    Department of Chemistry, The University of Adelaide, Adelaide, South Australia 5005, Australia
    Bioorg Med Chem Lett 22:2720-2. 2012
    ....
  101. ncbi Intermolecular C-H···O and C-H···X interactions in substituted spiroacenaphthylene structures
    J Suresh
    Department of Physics, Madura College, Madurai 625 011, India
    Acta Crystallogr C 68:o257-61. 2012
    ..In all three structures, molecules are linked through centrosymmetric ring motifs, further tailored through a relay of C-H···X [Cl in (I), Br in (II) and O in (III)] interactions...

Research Grants11

  1. Lipid Raft Microdomains in Neutrophil Function
    ROBERT GARY SITRIN; Fiscal Year: 2010
    ..Hopefully, targeting the function of lipid raft microdomains will engender new therapeutic strategies for enhancing antimicrobial defenses and suppressing the deleterious effects of acute inflammation. ..
  2. The Urokinase-CD87 System in Macrophage Activation
    Robert Sitrin; Fiscal Year: 2004
    ....
  3. MOLECULAR NEUROBIOLOGY OF SCHIZOPHRENIA
    Robert Freedman; Fiscal Year: 2008
    ..We present provocative new data that perinatal choline supplementation to mice with acra7 polymorphisms results in offspring with normal inhibition of the hippocampal response to repeated sounds. ..
  4. Asymmetric Synthesis of Amino Acids and Amino Phosphonic Acids
    FRANKLIN DAVIS; Fiscal Year: 2007
    ..The photodesulfmylation of sulfinamides represents an important new protocol, not requiring acids or bases, for the removal of the valuable amine N-sulfinyl protecting group. ..
  5. ASYMMETRIC SYNTHESIS OF BIOACTIVE PRIMARY AMINES
    FRANKLIN DAVIS; Fiscal Year: 2006
    ....
  6. Mouse model of binge drinking-induced neurotoxicity
    CHRISTOPHER DE FIEBRE; Fiscal Year: 2006
    ..Via the latter, the development of alpha7-selective agents as therapeutics to treat binge drinking-induced neurotoxicity may be fostered. ..
  7. Opiate Bivalent Ligands:Structure/Function Studies
    PHILIP PORTOGHESE; Fiscal Year: 2006
    ..Chronic testing of the target compounds will be carried out in mice to determine if there are in vivo correlates with the in vitro data obtained in projects 1 and 2. ..
  8. The Genetics of Endophenotypes and Schizophrenia
    Ann Olincy; Fiscal Year: 2007
    ..Findings of heritable deficits in specific measures will be used to guide the next generation of studies of the genetics of schizophrenia. ..
  9. Syntheses of Amino Acids and Amino Phosphonic Acids
    FRANKLIN DAVIS; Fiscal Year: 2005
    ..Targets include cyclic, unsaturated, and, beta substituted derivatives (beta amino, beta hydroxy, and beta fluoro). ..
  10. ELECTROPHYSIOLOGY OF SENSORY GATING IN SCHIZOPHRENIA
    Robert Freedman; Fiscal Year: 2004
    ..Schizophrenia and bipolar disorder are complex illnesses with multiple genetic and non-genetic elements. The goal of this project is elucidate one of these elements as they are discovered. ..
  11. NICOTINIC SYNAPTIC TRANSMISSION IN THE HIPPOCAMPUS
    Robert Freedman; Fiscal Year: 2002
    ....