Zobrazeno 1 - 10
of 83
pro vyhledávání: '"D E MacIntyre"'
Since its inception the research area of platelet pharmacology has always been a vigorous one and it is a characteristic that new approaches to the understanding of platelet function are rapidly and thoroughly investigated. The intensity of this acti
Autor:
Lawrence F. Colwell, William P. Feeney, Liping Deng, Michael J. Forrest, Randy R. Miller, Ralph A. Stearns, Ann E. Weber, Mari R. Candelore, Gary J Hom, D. E. Macintyre, Mathew J. Wyvratt, Dawn Chitty, Robert J. Mathvink, Tolman Js, Laurie Tota, Margaret A. Cascieri, M. H. Fisher
Publikováno v:
Journal of Medicinal Chemistry. 43:3832-3836
As part of our investigation into the development of orally bioavailable beta(3) adrenergic receptor agonists, we have identified a series of pyridylethanolamine analogues possessing a substituted thiazole benzenesulfonamide pharmacophore that are po
Autor:
Richard Hargreaves, D. E. Macintyre, G Mason, S Tye, E. Ber, F.D. Tattersall, Michael J Cumberbatch, J. J. Hale, Malcolm MacCoss, Margaret A. Cascieri, W. Rycroft, Paul E. Finke, Raymond G. Hill, Sharon Sadowski, David J. Williamson, Sander G. Mills
Publikováno v:
Neuropharmacology. 39:652-663
The anti-emetic profile of the novel brain penetrant tachykinin NK1 receptor antagonist MK-0869 (L-754,030) 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluor o)phenyl-4-(3-oxo-1,2,4-triazol-5-yl)methylmorpholine and its water soluble
Autor:
Donald J. Marsh, D. E. Macintyre, Xiao-Ming Guan, Michael J. Forrest, Easter G. Frazier, Airu S. Chen, Theodore N. Mellin, Ramon E. Camacho, Hong Yu, Jill K. Fisher, Van der Ploeg Lh, Joe Metzger, Alison M. Strack, Myrna E. Trumbauer, Howard Y. Chen, Shobhna Gopal-Truter
Publikováno v:
Transgenic Research. 9:145-154
We evaluated the role of the melanocortin-4 receptor (MC-4R) in the control of metabolic rate and food intake in mice. Intraperitoneal administration of the non-selective MC-R agonist melanotan II (MT-II; a cyclic heptapeptide) increases metabolic ra
Publikováno v:
Inflammation. 23:51-62
A model of acute lung injury induced by intravenous phorbol myristate acetate (PMA) is described. The model is characterized by the accumulation of polymorphonuclear leukocytes (PMNs) and a hemorrhagic edema in bronchoalveolar lavage (BAL) fluid when
Autor:
Jeffrey P Varnerin, T. Smith, Aurawan Vongs, Patricia J. Hey, M. Chou, Joseph J. King, Theodore N. Mellin, Easter G. Frazier, Michael R. Tota, D. E. Macintyre, Beth Junker, Beth Ann Murphy, Charles Rosenblum, Christian N. Nunes, B. W. Burgess, L. H. T. Van Der Ploeg
Publikováno v:
Protein Expression and Purification. 14:335-342
A procedure is described for gram-scale refolding of Escherichia coli-derived human leptin inclusion bodies. Refolding was achieved by gradually reducing denaturant using a diafiltration method. Refolded leptin is characterized by in vivo modulation
Autor:
P. E. Finke, Gary G. Chicchi, Nadia M.J. Rupniak, George J. Eiermann, Nancy N. Tsou, E. Ber, Angela Williams, W. Rycroft, Margaret A. Cascieri, Sander G. Mills, Richard Hargreaves, M. Maccoss, Joe Metzger, D. E. Macintyre, Myra B. Kurtz, Sharon Sadowski, J. J. Hale, F.D. Tattersall
Publikováno v:
Journal of Medicinal Chemistry. 41:4607-4614
Structural modifications requiring novel synthetic chemistry were made to the morpholine acetal human neurokinin-1 (hNK-1) receptor antagonist 4, and this resulted in the discovery of 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluor
Autor:
Catherine D. Strader, M J Forrest, Jennifer E. Hutchins, R R Miller, Shuet Hing L Chiu, D. E. Macintyre, G J Hom, R A Stearns, T J Bach, Margaret A. Cascieri, Linda J. Kelly, A M Amend, Joseph M. Metzger, D Carroll, Mari R. Candelore, Xiao-Ming Guan, B Hegarty-Friscino, E R Parmee, Edward J. Brady, Liping Deng, Robert J. Mathvink, Richard Saperstein, M. H. Fisher, J M Barker, H O Ok
Publikováno v:
Journal of Clinical Investigation. 101:2387-2393
Activation of beta3 adrenergic receptors on the surface of adipocytes leads to increases in intracellular cAMP and stimulation of lipolysis. In brown adipose tissue, this serves to up-regulate and activate the mitochondrial uncoupling protein 1, whic
Autor:
Joe Metzger, Gary G. Chicchi, Linda Elizabeth Keown, R. Baker, Margaret A. Cascieri, Simon C. Morton, Christopher John Swain, A. P. Watt, Silvi Luell, Sharon Sadowski, Andrew Pate Owens, D. E. Macintyre, Michael J. Forrest, Richard H. Herbert, Brian John Williams, T. Ladduwahetty
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:2959-2962
In vitro metabolism studies on a series of 3,5-bis(trifluoromethyl)benzyl ethers have identified 3,5-bis(trifluoromethyl)benzoic acid as a significant metabolite possibly arising via oxidation of the benzylic position. A methyl group was introduced i
Autor:
F.D. Tattersall, D. E. Macintyre, D. W. Williamson, Karen Elizabeth Haworth, Raymond Baker, Alan P. Watt, Margaret A. Cascieri, Tamara Ladduwahetty, Joseph M. Metzger, Eileen Mary Seward, Simon Neil Owen, Linda Elizabeth Keown, W. Rycroft, Richard Hargreaves, Christopher John Swain, S. L. Shepheard, Sharon Sadowski, Mark Stuart Chambers
Publikováno v:
Journal of Medicinal Chemistry. 39:2907-2914
The preparation of a series of N-heteroarylpiperidine ether-based human NK1 antagonists is described. Two of the compounds 3-[-(2S,3S)-3-(((3,5-bis(trifluoromethyl)phenyl)methyl)oxy)- 2-phenylpiperidino}methyl]-1,2,4-triazole (11) and 5-[¿(2S,3S)-3-