P. Jacobson

发表

Discovery of adamantane ethers as inhibitors of 11beta-HSD-1: Synthesis and biological evaluation.

K. Longenecker, Jyoti R. Patel, H. Sham, 2007, Bioorganic & medicinal chemistry letters.

Distinctions and contradistinctions between antiobesity histamine H3 receptor (H3R) antagonists compared to cognition-enhancing H3 receptor antagonists

E. Bush, A. Hancock, R. Bitner, 2006, Inflammation Research.

Adamantane 11-beta-HSD-1 inhibitors: Application of an isocyanide multicomponent reaction.

Deanne F. Stolarik, S. Fung, Katina Monzon, 2006, Bioorganic & medicinal chemistry letters.

Selective antagonism of the hepatic glucocorticoid receptor reduces hepatic glucose production.

D. Edgerton, A. Cherrington, D. Beno, 2006, Metabolism: clinical and experimental.

Effect of 11 beta-hydroxysteroid dehydrogenase-1 inhibition on hepatic glucose metabolism in the conscious dog.

R. Rizza, R. Basu, D. Edgerton, 2010, American journal of physiology. Endocrinology and metabolism.

Discovery of potent and selective inhibitors of 11beta-HSD1 for the treatment of metabolic syndrome.

H. Sham, S. Richards, M. Winn, 2006, Bioorganic & medicinal chemistry letters.

Delayed administration of elezanumab, a human anti-RGMa neutralizing monoclonal antibody, promotes recovery following cervical spinal cord injury

M. Fehlings, Charles Tator, Lili Huang, 2022, Neurobiology of Disease.

Intrathecal amyloid‐beta oligomer administration increases tau phosphorylation in the medial temporal lobe in the African green monkey: A nonhuman primate model of Alzheimer's disease

E. Mufson, W. Klein, S. Perez, 2022, Neuropathology and applied neurobiology.

Anti-inflammatory properties of the protein kinase C inhibitor, 3-[1-[3-(dimethylamino)propyl]-1H-indol-3-yl]-4(1H-indol-3-yl)-1H-pyrrole-2,5-dione monohydrochloride (GF109203X) in the PMA-mouse ear edema model

D. Schrier, P. Jacobson, A. Metz, 2005, Agents and Actions.

Hepatic knockdown of mitochondrial GPAT1 in ob/ob mice improves metabolic profile.

Haiyan Xu, R. Gimeno, C. Collins, 2006, Biochemical and biophysical research communications.

Pharmacological Studies of Novel Marine Metabolites

R. Jacobs, P. Jacobson, M. D. Carvalho, 1993 .

Liver-selective glucocorticoid receptor antagonism decreases glucose production and increases glucose disposal, ameliorating insulin resistance.

P. Jacobson, D. Wilcox, B. Zinker, 2007, Metabolism: clinical and experimental.

Hepatic Glucocorticoid Receptor Antagonism Is Sufficient to Reduce Elevated Hepatic Glucose Output and Improve Glucose Control in Animal Models of Type 2 Diabetes

L. Öhman, D. Edgerton, A. Cherrington, 2005, Journal of Pharmacology and Experimental Therapeutics.

Effects of 11β-hydroxysteroid dehydrogenase-1 inhibition on hepatic glycogenolysis and gluconeogenesis.

V. Saraswathi, R. Basu, D. Edgerton, 2013, American journal of physiology. Endocrinology and metabolism.

Anti-inflammatory properties of Gö 6850: a selective inhibitor of protein kinase C.

C. Schächtele, D. Schrier, P. Jacobson, 1995, The Journal of pharmacology and experimental therapeutics.

Peripheral and central nervous system inhibition of 11β-hydroxysteroid dehydrogenase type 1 in man by the novel inhibitor ABT-384

G. Marek, D. Barnes, L. Ereshefsky, 2013, Translational Psychiatry.

Liver Is the Site of Splanchnic Cortisol Production in Obese Nondiabetic Humans

R. Rizza, A. Basu, P. Jung, 2009, Diabetes.

Basu R, Basu A, Grudzien M, Jung P, Jacobson P, Johnson M, Singh R, Sarr M, Rizza RA. Liver is the site of splanchnic cortisol production in obese nondiabetic humans. Diabetes 2009;58:39-45

R. Rizza, A. Basu, P. Jung, 2009 .

Acute Inhibition of 11β-Hydroxysteroid Dehydrogenase Type-1 Improves Memory in Rodent Models of Cognition

K. Browman, E. Mohler, L. Rueter, 2011, The Journal of Neuroscience.

Pharmacological characterization of the pseudopterosins: novel anti-inflammatory natural products isolated from the Caribbean soft coral, Pseudopterogorgia elisabethae.

K. Glaser, R. Jacobs, A. Mayer, 1998, Life sciences.

Regulation of CD11b/CD18 expression in human neutrophils by phospholipase A2.

D. Schrier, P. Jacobson, 1993, Journal of immunology.

Inactivation of human synovial fluid phospholipase A2 by the marine natural product, manoalide.

L. Marshall, R. Jacobs, P. Jacobson, 1990, Biochemical pharmacology.

Antiobesity effects of A-331440, a novel non-imidazole histamine H3 receptor antagonist.

E. Bush, G. Fox, A. Hancock, 2004, European journal of pharmacology.

Discovery and pharmacological evaluation of growth hormone secretagogue receptor antagonists.

E. Bush, H. Sham, D. Beno, 2006, Journal of medicinal chemistry.

2,4-diaminopyrimidine derivatives as potent growth hormone secretagogue receptor antagonists.

E. Bush, H. Sham, D. Beno, 2006, Journal of medicinal chemistry.

The effects of the phospholipase A2 inhibitor, manoalide, on cartilage degradation, stromelysin expression, and synovial fluid cell count induced by intraarticular injection of human recombinant interleukin-1 alpha in the rabbit.

C. Flory, D. Schrier, P. Jacobson, 1996, Arthritis and rheumatism.

Adamantane sulfone and sulfonamide 11-β-HSD1 Inhibitors

K. Longenecker, R. Judge, Deanne F. Stolarik, 2007 .

Parallel strategies for the preparation and selection of liver-targeted glucocorticoid receptor antagonists.

G. L. Hamilton, B. J. Backes, S. Fung, 2007, Bioorganic & medicinal chemistry letters.

Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists.

S. Richards, S. Fung, Jiahong Wang, 2006, Bioorganic & medicinal chemistry letters.

Delivery of RNAi reagents in murine models of obesity and diabetes

E. Bush, P. Jung, C. Rondinone, 2006, Journal of RNAi and gene silencing : an international journal of RNA and gene targeting research.

Synthesis and characterization of non-steroidal ligands for the glucocorticoid receptor: selective quinoline derivatives with prednisolone-equivalent functional activity.

M. Nakane, S. Elmore, P. Kym, 2001, Journal of medicinal chemistry.

Streptococcal cell wall-induced arthritis. Requirements for neutrophils, P-selectin, intercellular adhesion molecule-1, and macrophage-inflammatory protein-2.

P. Ward, J. Dykens, C. Flory, 1997, Journal of immunology.

Discovery and metabolic stabilization of potent and selective 2-amino-N-(adamant-2-yl) acetamide 11beta-hydroxysteroid dehydrogenase type 1 inhibitors.

R. Henry, H. Sham, D. Beno, 2007, Journal of medicinal chemistry.

ABT-963 [2-(3,4-Difluoro-phenyl)-4-(3-hydroxy-3-methyl-butoxy)-5-(4-methanesulfonyl-phenyl)-2H-pyridazin-3-one], A Highly Potent and Selective Disubstituted Pyridazinone Cyclooxgenase-2 Inhibitor

G. Carter, S. Surapaneni, K. Marsh, 2004, Journal of Pharmacology and Experimental Therapeutics.

Nonsteroidal selective glucocorticoid modulators: the effect of C-10 substitution on receptor selectivity and functional potency of 5-allyl-2,5-dihydro-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.

S. Elmore, M. Nakane, J. Miner, 2003, Journal of medicinal chemistry.

Discovery of orally active butyrolactam 11β-HSD1 inhibitors

E. Bush, Deanne F. Stolarik, S. Fung, 2006 .

Nonsteroidal selective glucocorticoid modulators: the effect of C-5 alkyl substitution on the transcriptional activation/repression profile of 2,5-dihydro-10-methoxy-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.

S. Elmore, D. Anderson, B. Green, 2001, Journal of medicinal chemistry.

PTP1B antisense oligonucleotide lowers PTP1B protein, normalizes blood glucose, and improves insulin sensitivity in diabetic mice

J. Waring, R. Ulrich, S. Crosby, 2002, Proceedings of the National Academy of Sciences of the United States of America.

Synthesis and structural activity relationship of 11beta-HSD1 inhibitors with novel adamantane replacements.

Jyoti R. Patel, H. Sham, S. Fung, 2006, Bioorganic & medicinal chemistry letters.

Histamine H3 antagonists in models of obesity

E. Bush, A. Hancock, P. Jacobson, 2004, Inflammation Research.

A novel antiinflammatory maintains glucocorticoid efficacy with reduced side effects.

M. Nakane, S. Elmore, R. Turner, 2003, Molecular endocrinology.

Effect of analgesic therapy on clinical outcome measures in a randomized controlled trial using client-owned dogs with hip osteoarthritis

S. Schaefer, E. Cozzi, P. Muir, 2012, BMC Veterinary Research.

A new spin on an old model: in vivo evaluation of disease progression by magnetic resonance imaging with respect to standard inflammatory parameters and histopathology in the adjuvant arthritic rat.

D. Wilcox, P. Jacobson, R. Harris, 1999, Arthritis and rheumatism.

Chronic treatment with either dexfenfluramine or sibutramine in diet-switched diet-induced obese mice

Thomas Fey, Robin Shapiro, E. Bush, 2006, Endocrine.

Differential Effects of Domoic Acid and E. coli Lipopolysaccharide on Tumor Necrosis Factor-α, Transforming Growth Factor-β1 and Matrix Metalloproteinase-9 Release by Rat Neonatal Microglia: Evaluation of the Direct Activation Hypothesis

A. Mayer, S. Gunasekera, P. Jacobson, 2007, Marine drugs.

Effect of a short-term in vitro exposure to the marine toxin domoic acid on viability, tumor necrosis factor-alpha, matrix metalloproteinase-9 and superoxide anion release by rat neonatal microglia

H. Manev, A. Mayer, T. Uz, 2001, BMC pharmacology.

Potentiation of analgesic efficacy but not side effects: co-administration of an α4β2 neuronal nicotinic acetylcholine receptor agonist and its positive allosteric modulator in experimental models of pain in rats.

M. Decker, G. Fox, Chih-Liang Chin, 2011, Biochemical pharmacology.

Liver-specific Knockdown of JNK1 Up-regulates Proliferator-activated Receptor γ Coactivator 1β and Increases Plasma Triglyceride despite Reduced Glucose and Insulin Levels in Diet-induced Obese Mice*

E. Bush, P. Jung, C. Rondinone, 2007, Journal of Biological Chemistry.

Comparison of adjuvant and streptococcal cell wall-induced arthritis in the rat

P. Jacobson, R. Carlson, 1999 .

Fuscoside: an anti-inflammatory marine natural product which selectively inhibits 5-lipoxygenase. Part I: Physiological and biochemical studies in murine inflammatory models.

R. Jacobs, P. Jacobson, 1992, The Journal of pharmacology and experimental therapeutics.

Escherichia coli lipopolysaccharide potentiation and inhibition of rat neonatal microglia superoxide anion generation: correlation with prior lactic dehydrogenase, nitric oxide, tumor necrosis factor-alpha, thromboxane B2, and metalloprotease release.

K. Glaser, A. Mayer, P. Jacobson, 1999, Shock.

Elezanumab, a human anti-RGMa monoclonal antibody, promotes neuroprotection, neuroplasticity, and neurorecovery following a thoracic hemicompression spinal cord injury in non-human primates

Q. Barraud, G. Courtine, J. Guest, 2021, Neurobiology of Disease.

Delayed administration of the human anti-RGMa monoclonal antibody elezanumab promotes functional recovery including spontaneous voiding after spinal cord injury in rats

Charles Tator, B. Mueller, P. Monnier, 2020, Neurobiology of Disease.

Estimating efficacy and drug ED50's using von Frey thresholds: impact of weber's law and log transformation.

Michael Decker, David Leblond, M. Decker, 2012, The journal of pain : official journal of the American Pain Society.

The Vasopressin 1b Receptor Antagonist A-988315 Blocks Stress Effects on the Retrieval of Object-Recognition Memory

B. Roozendaal, M. M. Gaalen, Areg Barsegyan, 2015, Neuropsychopharmacology.

Synthesis and biological evaluation of heterocycle containing adamantane 11beta-HSD1 inhibitors.

Jyoti R. Patel, H. Sham, D. Beno, 2006, Bioorganic & medicinal chemistry letters.

Antiobesity evaluation of histamine H3 receptor (H3R) antagonist analogs of A-331440 with improved safety and efficacy

E. Bush, A. Hancock, P. Jacobson, 2005, Inflammation Research.

In vitro optimization of structure activity relationships of analogues of A-331440 combining radioligand receptor binding assays and micronucleus assays of potential antiobesity histamine H3 receptor antagonists.

E. Bush, A. Hancock, P. Jacobson, 2004, Basic & clinical pharmacology & toxicology.

Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.

Jyoti R. Patel, T. Reisch, Z. Tian, 2005, Journal of medicinal chemistry.

Rapamycin analogs with reduced systemic exposure.

P. Wiedeman, J. Trevillyan, G. Carter, 2005, Bioorganic & medicinal chemistry letters.

Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.

K. Koehler, L. Hagberg, C. Jakob, 2004, Journal of medicinal chemistry.

Hepatic knockdown of stearoyl-CoA desaturase 1 via RNA interference in obese mice decreases lipid content and changes fatty acid composition.

Haiyan Xu, Harriet T. Smith, R. Reilly, 2007, Frontiers in bioscience : a journal and virtual library.

ABT-963, A Highly Potent and Selective Disubstituted Pyridazinone COX-2 Inhibitor

G. Carter, S. Surapaneni, M. Jarvis, 2004 .

Effects of 11β-hydroxysteroid dehydrogenase-1 inhibition on hepatic glycogenolysis and gluconeogenesis.

V. Saraswathi, R. Basu, D. Edgerton, 2013, American journal of physiology. Endocrinology and metabolism.

Adamantane sulfone and sulfonamide 11-beta-HSD1 Inhibitors.

K. Longenecker, R. Judge, Deanne F. Stolarik, 2007, Bioorganic & medicinal chemistry letters.

Discovery of orally active butyrolactam 11beta-HSD1 inhibitors.

E. Bush, Deanne F. Stolarik, S. Fung, 2006, Bioorganic & medicinal chemistry letters.

Treatment of zucker diabetic fatty rats with antisense oligonucleotide to phosphotyrosine phosphatase-1B for 5 weeks halts development of diabetes

E. Bush, J. Trevillyan, P. Jacobson, 2001 .

Neutralizing RGMa with Elezanumab Promotes Cerebroprotection and Recovery in Rabbit Middle Cerebral Artery Occlusion

Charles Tator, G. Fox, V. Nimmrich, 2023, Translational stroke research.