Zobrazeno 1 - 10
of 19
pro vyhledávání: '"William F. Holt"'
Autor:
Mark R. Hellberg, Bryon S. Severns, William F. Holt, Richard Young, Richard A. Glennon, Thomas R. Dean, Najam A. Sharif, Hwang-Hsing Chen, Curtis R. Kelly, Marsha A. McLaughlin, Jesse A. May
Publikováno v:
Journal of medicinal chemistry. 58(22)
Recently, it has been reported that 5-HT2 receptor agonists effectively reduce intraocular pressure (IOP) in a nonhuman primate model of glaucoma. Although 1-[(2S)-2-aminopropyl]indazol-6-ol (AL-34662) was shown to have good efficacy in this nonhuman
Publikováno v:
Survey of Ophthalmology. 50:S46-S54
Topical treatment of ocular bacterial infection is practiced widely, and the choice of the antibacterial agent depends on the nature of the infection, including the susceptibility of the organism, the tissue affected, and the safety profile of the ag
Autor:
Graham J. Durant, Lu Zhang, Michael E. Perlman, Suchitra Chari, Teresa Wolcott, Ruth C. Lavin, Cassandra Kirk, Robert N. McBurney, Seetharamaiyer Padmanabhan, William F. Holt, James B. Fischer, Paresh Thakker, Deborah Daly, David Berlove, Jinqing Guo, Kathy J Burke-Howie, Deke Moore
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:3151-3155
Solution-phase synthesis of various acylguanidine derivatives and the evaluation of a small library of compounds as potential sodium channel blockers are described.
Autor:
Irene M. Purcell, Teresa M. Schelhorn, William F. Holt, S S Ellery, Wester Ronald Thure, William R. Murphy, Michael L. Mangiapane, Kelly A. Simpson, Andrew H. Smith
Publikováno v:
Drug Development Research. 34:361-368
Human and monkey renin are very similar, but differ from the renin of species commonly used in screening antihypertensive agents (i.e., dog and rat). This has necessitated the evaluation of renin inhibitors (Rls) in primate models. We have found that
Autor:
William F. Holt, M.A. Ravi Kiron, Robert L. Rosati, Kleinman Edward F, Andrew H. Fray, Irene M. Purcell, William R. Murphy
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:589-592
CP-71,362 (Boc-Phe-His-hexahydroPhe[OH]Leu-Lys-Phe) has been identified as the most potent inhibitor of rat plasma renin (IC50 = 3 nM) and dog plasma renin (IC50 = 3 pM) to date and thus can be used as an important experimental tool in the study of t
Autor:
Joseph T. MacAndrew, William F. Holt, S S Ellery, William R. Murphy, Irene M. Purcell, Kleinman Edward F, Andrew H. Smith, Michael L. Mangiapane
Publikováno v:
Clinical and Experimental Hypertension. 16:507-533
Most renin inhibitors are primate-specific. In the present paper, we describe the effects of CP-71,362, a pentapeptide which preferentially inhibits canine (and to a lesser extent, rat) plasma renin. Vs. the canine enzyme, its affinity (IC50 = 3.3 x
Publikováno v:
Journal of Cardiovascular Pharmacology. 21:791-796
Renal and systemic hemodynamics were studied in rats 1 month after induction of myocardial infarction by ligation of the left coronary artery. The mean arterial pressure, heart rate, and cardiac index were not different from controls, but there were
Publikováno v:
Hypertension. 19:668-671
Oral administration of the angiotensin II receptor subtype 1 (AT1) antagonist DuP 753 causes long-lasting lowering of mean arterial pressure in spontaneously hypertensive rats. We examined whether the antihypertensive action of DuP 753 is a result of
Autor:
Peter J. Oates, John P. Hakkinen, William F. Holt, William R. Murphy, Lawrence A. Reiter, James J. Maciejko, Goddard Carl Joseph
Publikováno v:
Digestive Diseases and Sciences. 36:1721-1728
CP-66,948 is a histamine H2-receptor antagonist with gastric antisecretory activity and mucosal protective properties. The affinity of CP-66,948 for the guinea pig atria histamine H2-receptor is 15 times greater than that of cimetidine and seven time
Publikováno v:
Journal of Medicinal Chemistry. 33:543-552
A series of 4-substituted 2-guanidinothiazoles has been found to inhibit the gastric proton-pump enzyme H+,K(+)-ATPase. In general, these compounds were reversible inhibitors of canine gastric H+,K(+)-ATPase, competitive at the K+ site, and selective