benzothiadiazines

Summary

Summary: Heterocyclic compounds of a ring with SULFUR and two NITROGEN atoms fused to a BENZENE ring. Members inhibit SODIUM-POTASSIUM-CHLORIDE SYMPORTERS and are used as DIURETICS.

Top Publications

  1. ncbi Substituted benzothiadizine inhibitors of Hepatitis C virus polymerase
    Antony N Shaw
    Department of Medicinal Chemistry, GlaxoSmithKline, Collegeville, PA 19426, USA
    Bioorg Med Chem Lett 19:4350-3. 2009
  2. ncbi Rational Prescribing in Primary Care (RaPP-trial). A randomised trial of a tailored intervention to improve prescribing of antihypertensive and cholesterol-lowering drugs in general practice [ISRCTN48751230]
    Atle Fretheim
    Department of Health Services Research, Norwegian Directorate for Health and Social Affairs, N 0031 Oslo, Norway
    BMC Health Serv Res 3:5. 2003
  3. ncbi The potential savings of using thiazides as the first choice antihypertensive drug: cost-minimisation analysis
    Atle Fretheim
    Department of Health Services Research, Norwegian Directorate for Health and Social Affairs, N 0031 Oslo, Norway
    BMC Health Serv Res 3:18. 2003
  4. ncbi Characterization of the inhibition of hepatitis C virus RNA replication by nonnucleosides
    Licia Tomei
    Department of Biochemistry, Istituto di Ricerche di Biologia Molecolare P. Angeletti (IRBM, Pomezia, Italy
    J Virol 78:938-46. 2004
  5. ncbi Influences of educational interventions and adverse news about calcium-channel blockers on first-line prescribing of antihypertensive drugs to elderly people in British Columbia
    M Maclure
    PharmaCare, British Columbia Ministry of Health, Victoria, Canada
    Lancet 352:943-8. 1998
  6. ncbi Choosing a first-line drug in the management of elevated blood pressure: what is the evidence? 1: Thiazide diuretics
    J M Wright
    Department of Medicine, University of British Columbia, Vancouver
    CMAJ 163:57-60. 2000
  7. ncbi Changes in the phamacologic treatment of hypertension in the Department of Veterans Affairs 1997-1999: decreased use of calcium antagonists and increased use of beta-blockers and thiazide diuretics
    D Siegel
    Medical Service, Department of Veterans Affairs, Northern California Health Care System, Mather 95655, USA
    Am J Hypertens 14:957-62. 2001
  8. ncbi [Tax payers have payed billions for the "blood pressure maffia's" actions]
    Bengt Järhult
    Lakartidningen 100:1917-8. 2003
  9. ncbi The ANBP2 and ALLHAT: conflicting or consistent?
    Jeffrey A Cutler
    National Heart, Lung, and Blood Institute, Bethesda, MD 20892 7936, USA
    J Clin Hypertens (Greenwich) 5:192-5. 2003
  10. ncbi [Thiazides or ACE inhibitors? A drug-economic analysis]
    Ivar Aursnes
    Tidsskr Nor Laegeforen 124:1668. 2004

Research Grants

Detail Information

Publications135 found, 100 shown here

  1. ncbi Substituted benzothiadizine inhibitors of Hepatitis C virus polymerase
    Antony N Shaw
    Department of Medicinal Chemistry, GlaxoSmithKline, Collegeville, PA 19426, USA
    Bioorg Med Chem Lett 19:4350-3. 2009
    ..Substitution in the benzothiadiazine portion of the molecule, furnishing improvement in potency in the high protein Replicon assay, is highlighted, culminating in the discovery of 12h, a highly potent oxyacetamide derivative...
  2. ncbi Rational Prescribing in Primary Care (RaPP-trial). A randomised trial of a tailored intervention to improve prescribing of antihypertensive and cholesterol-lowering drugs in general practice [ISRCTN48751230]
    Atle Fretheim
    Department of Health Services Research, Norwegian Directorate for Health and Social Affairs, N 0031 Oslo, Norway
    BMC Health Serv Res 3:5. 2003
    ....
  3. ncbi The potential savings of using thiazides as the first choice antihypertensive drug: cost-minimisation analysis
    Atle Fretheim
    Department of Health Services Research, Norwegian Directorate for Health and Social Affairs, N 0031 Oslo, Norway
    BMC Health Serv Res 3:18. 2003
    ..Despite this, the use of thiazides is much lower than that of other drug-classes. We wanted to estimate the potential for savings if thiazides were used as the first choice drug for the management of uncomplicated hypertension...
  4. ncbi Characterization of the inhibition of hepatitis C virus RNA replication by nonnucleosides
    Licia Tomei
    Department of Biochemistry, Istituto di Ricerche di Biologia Molecolare P. Angeletti (IRBM, Pomezia, Italy
    J Virol 78:938-46. 2004
    ..The mutations (M414T, C451R, G558R, and H95R) render the HCV replicons resistant to inhibition by benzothiadiazines, though the mutant replicons remain sensitive to inhibition by other nucleoside and NNIs of the HCV RNA ..
  5. ncbi Influences of educational interventions and adverse news about calcium-channel blockers on first-line prescribing of antihypertensive drugs to elderly people in British Columbia
    M Maclure
    PharmaCare, British Columbia Ministry of Health, Victoria, Canada
    Lancet 352:943-8. 1998
    ....
  6. ncbi Choosing a first-line drug in the management of elevated blood pressure: what is the evidence? 1: Thiazide diuretics
    J M Wright
    Department of Medicine, University of British Columbia, Vancouver
    CMAJ 163:57-60. 2000
    ..The evidence indicates that low-dose thiazides are preferable to high-dose thiazides and that low-dose thiazides are better than or equivalent to other antihypertensive drugs for each of the goals of therapy...
  7. ncbi Changes in the phamacologic treatment of hypertension in the Department of Veterans Affairs 1997-1999: decreased use of calcium antagonists and increased use of beta-blockers and thiazide diuretics
    D Siegel
    Medical Service, Department of Veterans Affairs, Northern California Health Care System, Mather 95655, USA
    Am J Hypertens 14:957-62. 2001
    ..These changes were consistent with improved compliance with VA national guidelines. The cost implications of these changes in practice patterns were considerable...
  8. ncbi [Tax payers have payed billions for the "blood pressure maffia's" actions]
    Bengt Järhult
    Lakartidningen 100:1917-8. 2003
  9. ncbi The ANBP2 and ALLHAT: conflicting or consistent?
    Jeffrey A Cutler
    National Heart, Lung, and Blood Institute, Bethesda, MD 20892 7936, USA
    J Clin Hypertens (Greenwich) 5:192-5. 2003
  10. ncbi [Thiazides or ACE inhibitors? A drug-economic analysis]
    Ivar Aursnes
    Tidsskr Nor Laegeforen 124:1668. 2004
  11. ncbi Angiotensin-converting enzyme inhibitors and diuretics: optimal combination therapy
    Mori J Krantz
    Ann Intern Med 141:893; author reply 893. 2004
  12. ncbi Distinguishing between presynaptic and postsynaptic mechanisms of short-term depression during action potential trains
    Adrian Y C Wong
    Department of Cell Physiology and Pharmacology, University of Leicester, Leicester, LE1 9HN, United Kingdom
    J Neurosci 23:4868-77. 2003
    ....
  13. ncbi Diuretics for cardiovascular prevention in the elderly
    O Hanon
    Department of Geriatrics, Hopital Broca, rue Pascal, Paris, France
    J Hum Hypertens 18:S15-22. 2004
    ....
  14. ncbi AMPA receptors on developing medial septum/diagonal band neurons are sensitive to early postnatal binge-like ethanol exposure
    Shu-Huei Hsiao
    Department of Medical Pharmacology and Toxicology, Texas A and M University System Health Science Center, College of Medicine MS 1114, College Station, TX 77843-1114, USA
    Brain Res Dev Brain Res 142:89-99. 2003
    ..Repeating this inhibition during early postnatal binge-like intoxication can augment normal development of AMPAR function...
  15. ncbi Hypertension, anti-hypertensive drug therapy and erectile dysfunction in diabetes
    P K Moulik
    Department of Medicine, Whiston Hospital, Prescot, UK
    Diabet Med 20:290-3. 2003
    ..The risk factors for ED were studied with particular reference to hypertension and anti-hypertensive drugs...
  16. ncbi Treatment of hypertension in type 2 diabetes mellitus: blood pressure goals, choice of agents, and setting priorities in diabetes care
    Sandeep Vijan
    Veterans Affairs Health Services Research, Development Center for Practice Management and Outcomes Research, P O Box 130170, Ann Arbor, Michigan 48113 0170, USA
    Ann Intern Med 138:593-602. 2003
    ..Hypertension in patients with type 2 diabetes mellitus is a prevalent condition that leads to substantial morbidity and mortality...
  17. ncbi The evidence base for tight blood pressure control in the management of type 2 diabetes mellitus
    Vincenza Snow
    American College of Physicians, 190 N. Independence Mall West, Philadelphia, Pennsylvannia 19106, USA
    Ann Intern Med 138:587-92. 2003
  18. ncbi [Established blood pressure drug wins out in a comparative study. In hypertension, a diuretic first!]
    Ulrike Wepner
    MMW Fortschr Med 145:10-2. 2003
  19. ncbi [Consequences of ALLHAT: Thiazides rehabilitated--time to change prescription patterns]
    Anders Hernborg
    , Universitetssjukhuset MAS, Malm
    Lakartidningen 100:408-10. 2003
  20. ncbi Shifting trends in the pharmacologic treatment of hypertension in a Nigerian tertiary hospital: a real-world evaluation of the efficacy, safety, rationality and pharmaco-economics of old and newer antihypertensive drugs
    A Q Adigun
    Department of Medicine, Division of Clinical Pharmacology, Indiana University School of Medicine, Indianapolis, USA
    J Hum Hypertens 17:277-85. 2003
    ....
  21. ncbi [ALLHAT=other leading physicians have alternative interpretations]
    Alan Charles
    Lakartidningen 100:2073-4. 2003
  22. ncbi Comparison of candesartan with lisinopril on ambulatory blood pressure and morning surge in patients with systemic hypertension
    Kazuo Eguchi
    Department of Cardiology, Jichi Medical School, Tochigi, Japan
    Am J Cardiol 92:621-4. 2003
    ....
  23. ncbi [ALLHAT trial--antithesis to the overuse of vasodilating antihypertensive drugs]
    Iwao Kuwajima
    Division of Internal Medicine, Tokyo Metropolitan Geriatric Hospital
    Nippon Rinsho 62:648-53. 2004
  24. ncbi [Risk factors to be considered at the beginning of antihypertensive therapy in diabetes mellitus]
    Gyorgy Jermendy
    Bajcsy Zsilinszky Kórház III Belgyógyászati Osztály, Budapest
    Orv Hetil 145:949-56. 2004
    ..It is reasonable to initiate antihypertensive therapy primarily with a low dose combination of two agents in diabetic patients with hypertension...
  25. ncbi [Revival of antihypertensive therapy: use of thiazide diuretics]
    Viktor Nagy
    Semmelweis Egyetem, Általános Orvostudományi Kar, II Belgyógyászai Klinika, Budapest
    Orv Hetil 145:669-76. 2004
    ..The newer diuretics--with fewer side effects--have very likely extrarenal way of effects, so their long time application seems very favourable...
  26. ncbi Properties of quantal transmission at CA1 synapses
    Sridhar Raghavachari
    Dept. of Biology and Volen Center for Complex Systems, Brandeis University MS 008, 415 South S, Waltham, MA 02454, USA
    J Neurophysiol 92:2456-67. 2004
    ....
  27. ncbi Following evidence-based prescribing guidelines for antihypertensives could save big bucks
    Gina Rollins
    Rep Med Guidel Outcomes Res 15:1, 6-7. 2004
  28. ncbi Treating high blood pressure in Africans with type 2 diabetes
    E O Okoro
    Ethn Dis 14:160-1. 2004
  29. ncbi [Modern strategies of infarction prevention in hypertensives and diabetics. Salt and sugar -- both are risky for the heart]
    Sonja Böhm
    MMW Fortschr Med 145:10. 2003
  30. ncbi Improving prescribing of antihypertensive and cholesterol-lowering drugs: a method for identifying and addressing barriers to change
    Atle Fretheim
    Informed Choice Research Department, Norwegian Health Services Research Centre, P, O, Box 7004, St, Olavs plass, Oslo, Norway
    BMC Health Serv Res 4:23. 2004
    ..We also report the results of a post hoc exercise and survey we carried out to evaluate our approach for identifying barriers and tailoring interventions...
  31. ncbi [Diabetes and drug treatment of hypertension]
    Andrea Siebenhofer
    Diabetes und Stoffwechselambulanz, Medizinische Universitätsklinik Graz, Auenbruggerplatz 15, 8036 Graz, Osterreich
    Wien Med Wochenschr 153:464-8. 2003
    ..To achieve an effective blood pressure reduction, a combination of different antihypertensive agents is necessary for most patients. Specially structured patient education programmes are another effective means of achieving this goal...
  32. ncbi The return on INVEST
    Michael H Alderman
    JAMA 290:2859-61. 2003
  33. ncbi Use of beta-blockers and risk of fractures
    Raymond G Schlienger
    Basel Pharmacoepidemiology Unit, Division of Clinical Pharmacology and Toxicology, University Hospital, Basel, Switzerland
    JAMA 292:1326-32. 2004
    ..Many elderly patients with hypertension who are at risk of developing osteoporosis may potentially benefit from combined therapy with beta-blockers and thiazides...
  34. ncbi Risk of congestive heart failure in an elderly population treated with peripheral alpha-1 antagonists
    Chris L Bryson
    VA Puget Sound Health Services Research and Development, VAMC, Seattle, Washington 98108, USA
    J Am Geriatr Soc 52:1648-54. 2004
    ....
  35. ncbi Antihypertensive therapy and incidence of type 2 diabetes in an elderly cohort
    Raj Padwal
    Division of General Internal Medicine, University of Alberta, Edmonton, Canada
    Diabetes Care 27:2458-63. 2004
    ..The aim of this study was to determine whether the incidence of type 2 diabetes differed among elderly users of four major antihypertensive drug classes...
  36. ncbi [Thiaside diuretics in combination with inhibitors of angiotensin-converting enzyme in patients with diabetes mellitus type 2 comorbid with arterial hypertension]
    I E Chazova
    Ter Arkh 76:28-32. 2004
    ..CONCLUSION: Co-renitek is effective and safe antihypertensive drug for treatment of arterial hypertension in patients with diabetes mellitus type 2...
  37. ncbi The thiazide-sensitive na-cl cotransporter and human disease: reemergence of an old player
    David H Ellison
    J Am Soc Nephrol 14:538-40. 2003
  38. ncbi [Policy of antihypertensive therapy in arterial hypertension in the elderly. II]
    M A Gurevich
    Klin Med (Mosk) 80:9-13. 2002
  39. ncbi [Comrades! There must be some blood order in the field of hypertension!]
    Arne Melander
    NEPI,
    Lakartidningen 102:1068-70. 2005
  40. ncbi Fixed dose combination therapy in the treatment of hypertension
    T Stanton
    Department of Medicine and Therapeutics, University of Glasgow, Glasgow, Scotland, UK
    J Hum Hypertens 16:75-8. 2002
  41. ncbi Prescribing patterns and therapeutic implications for diabetic hypertension in Bahrain
    K A Al Khaja
    Department of Pharmacology and Therapeutics, College of Medicine and Medical Sciences, Arabian Gulf University, Bahrain
    Ann Pharmacother 35:1350-9. 2001
    ..To determine drug prescription patterns and the extent of conformity with World Health Organization/international Society of Hypertension (WHO/ISH) guidelines in diabetic hypertension...
  42. ncbi Cyclothiazide prolongs low [Mg2+]-induced seizure-like events
    Bálint Lasztóczi
    Department of Neurochemistry, Institute of Biomolecular Chemistry, Chemical Research Center, Hungarian Academy of Sciences, Pusztaszeri ut 59 67, Budapest H 1025, Hungary
    J Neurophysiol 96:3538-44. 2006
    ..In contrast, the self-similar slow-down of low [Mg(2+)]-induced SLE dynamics by CTZ indicate AMPA receptor desensitization as a parameter shaping SLEs...
  43. ncbi Relative roles of different mechanisms of depression at the mouse endbulb of Held
    Hua Yang
    University of Buffalo, Department of Biological Sciences, State University of New York, Buffalo, NY 14260, USA
    J Neurophysiol 99:2510-21. 2008
    ..Furthermore, calcium-dependent recovery at the endbulb is critical to prevent complete rundown during high activity and to preserve the reliability of information transmission...
  44. ncbi Correlation of AMPA receptor subunit composition with synaptic input in the mammalian cochlear nuclei
    S M Gardner
    Department of Physiology, University of Wisconsin Medical School-Madison, Madison, Wisconsin 53706, USA
    J Neurosci 21:7428-37. 2001
    ....
  45. ncbi Blocking AMPA receptor desensitization prolongs spontaneous EPSC decay times and depolarizes H1 horizontal cells in carp retinal slices
    H Hirasawa
    Supermolecular Division, Electrotechnical Laboratory, Tsukuba, Ibaraki 305-8568, Japan
    Neurosci Res 40:217-25. 2001
    ..The desensitization of glutamate receptors may function to extend the dynamic range of H1 HC light responses...
  46. ncbi [Recent intervention studies with antihypertensive drugs and their influence on guidelines]
    Karl Heinz Rahn
    Medizinische Klinik und Poliklinik D, Universitatsklinikum, Muenster
    Med Klin (Munich) 98:771-5. 2003
    ..Both groups of experts emphasize that the main benefits of antihypertensive therapy are due to decreasing blood pressure per se...
  47. ncbi ALLHAT: a critical assessment
    Ake Sjoholm
    Karolinska Institutet, Internal Medicine, South Stockholm General Hospital, Stockholm, Sweden
    Blood Press 13:75-9. 2004
    ..Thus, the ALLHAT study suffers from several major shortcomings and there is a huge body of evidence that contradicts the ALLHAT interpretations...
  48. ncbi Hypertension: treatment--now & tomorrow
    Chike M Nzerue
    Ethn Dis 12:S2-43-5. 2002
  49. ncbi Effect of 14 years of antihypertensive treatment on renal function and urinary albumin excretion in primary hypertension
    A Siewert-Delle
    Department of Nephrology, Sahlgrenska University Hospital, University of Gothenburg, Sweden
    Am J Hypertens 9:841-9. 1996
    ..The increase in RVR and the decrease in RBF seen during 14 years of antihypertensive treatment was of the same magnitude as that seen with normal aging...
  50. ncbi Clinical inquiries. What is the best regimen for newly diagnosed hypertension?
    Joseph J Saseen
    University of Colorado Health Sciences Center, University of Colorado Family Medicine Residency Program, 4200 E 9th Ave Box C238, Denver, CO 80218 USA
    J Fam Pract 54:281-2. 2005
  51. ncbi [Reflexion of French experts on the key points of the symposium]
    J M Mallion
    Presse Med 31:S27-30. 2002
    ..Professor O. Dubourg recalled the beneficial effect of indapamid SR on LVH demonstrated in the LIVE study. Likewise, Professor M. Marre emphasized its important impact on microalbuminuria as shown in the NESTOR study...
  52. ncbi C-terminal truncation affects kinetic properties of GluR1 receptors
    Erika Suzuki
    Department of Pharmacology, Southern Illinois University School of Medicine, MC 9629, 801 N Rutledge, Room 3275, Springfield, IL 62702, USA
    Mol Cell Neurosci 29:1-10. 2005
    ..The lowered affinity and faster inactivation of these receptors suggests that their presence does not represent a risk for neuronal viability...
  53. ncbi Quality of life and antihypertensive drug therapy
    Joel Handler
    Kaiser Permanente, Anaheim, CA 92807, USA
    J Clin Hypertens (Greenwich) 7:274-85. 2005
    ..Medication compliance requires a multi-tiered strategy. Low-dose thiazide is well tolerated...
  54. ncbi Long-term potentiation alters the modulator pharmacology of AMPA-type glutamate receptors
    Bin Lin
    Department of Psychiatry, University of California, Irvine, California 92697, USA
    J Neurophysiol 87:2790-800. 2002
    ..Candidates for the changes responsible for the observed effects of LTP were evaluated using a model of AMPA receptor kinetics; a simple increase in the channel opening rate provided the most satisfactory match with the LTP data...
  55. ncbi Activity-dependent change in AMPA receptor properties in cerebellar stellate cells
    Siqiong June Liu
    Department of Pharmacology, University College London, London WC1E 6BT, United Kingdom
    J Neurosci 22:3881-9. 2002
    ..The activity-induced expression of GluR2-containing receptors significantly reduced the Ca(2+) permeability of AMPARs in stellate cells but did not slow the decay time course of synaptic currents...
  56. ncbi Diuretics: from classical carbonic anhydrase inhibitors to novel applications of the sulfonamides
    Claudiu T Supuran
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino Firenze, Italy
    Curr Pharm Des 14:641-8. 2008
    The widely clinically used benzothiadiazines and high ceiling diuretics, such as hydrochlorothiazide, hydroflumethiazide, quinethazone, metolazone, chlorthalidone, indapamide, furosemide and bumetanide, contain SO(2)NH(2) moieties acting ..
  57. ncbi ATP-sensitive potassium channel openers and 2,3-dimethyl-2-butylamine derivatives
    Hai Wang
    Department of Cardiovascularl Pharmacology, Beijing Institute of Pharmacology and Toxicology, Beijing, 100850, Peoples Republic of China
    Curr Med Chem 14:133-55. 2007
    ..2) cyanoguanidines, (3) thioformamides, (4) pyrimidine derivatives, (5) pyridine derivatives, (6) benzothiadiazines, (7) dihydropyridines, (8) nicotinamide derivatives, and (9) aliphatic amines...
  58. ncbi Studies of benzothiadiazine derivatives as hepatitis C virus NS5B polymerase inhibitors using 3D-QSAR, molecular docking and molecular dynamics
    X Wang
    Center of Bioinformatics, Northwest A and F University, Yangling, Shaanxi, China
    Curr Med Chem 17:2788-803. 2010
    ..with similar size of benzo group like isosteres are preferential at positions 1 and 2 (ring B of benzothiadiazines)...
  59. ncbi Novel 2,2-dioxide-4,4-disubstituted-1,3-H-2,1,3-benzothiadiazines as non-nucleoside reverse transcriptase inhibitors
    J W Corbett
    DuPont Pharmaceuticals Company, Experimental Station, Wilmington, DE 19880 0500, USA
    Bioorg Med Chem Lett 10:193-5. 2000
    ..The 2,2-dioxide-1H-2,1,3-benzothiadiazine ring system was constructed in one step from 2-amino-5-chlorobenzonitrile...
  60. ncbi Regulation of SULT2B1a (pregnenolone sulfotransferase) expression in rat C6 glioma cells: relevance of AMPA receptor-mediated NO signaling
    Atsushi Kohjitani
    Section on Steroid Regulation, Endocrinology and Reproduction Research Branch, National Institute of Child Health and Human Development, National Institutes of Health, Bethesda, MD, USA
    Neurosci Lett 430:75-80. 2008
    ..These findings suggest that expression of SULT2B1a, which catalyzes PREGS production, is inhibited by activation of excitatory amino acid receptors of the AMPA subtype, via facilitation of intracellular NO signaling...
  61. ncbi Satellite NG2 progenitor cells share common glutamatergic inputs with associated interneurons in the mouse dentate gyrus
    Jean Marie Mangin
    Department of Neurology, Center for Neuroscience Research, Children s National Medical Center, Washington, DC 20010, USA
    J Neurosci 28:7610-23. 2008
    ..The finding that NG2(+) cells are sensing patterns of activity arising in closely associated neurons suggests that NG2(+) cell function is finely regulated by the local network...
  62. ncbi [Current therapy guidelines for elderly hypertensive patients]
    Peter Fasching
    3. Interne Abteilung, Geriatriezentrum der Stadt Wien-Baumgarten, Wien, Osterreich
    Wien Med Wochenschr 154:2-3. 2004
  63. ncbi Simultaneous determination of enantiomerization and hydrolysis kinetic parameters of chiral N-alkylbenzothiadiazine derivatives
    Marina M Carrozzo
    Dipartimento di Scienze Farmaceutiche, Universita degli Studi di Modena e Reggio Emilia, Modena, Italy
    Chirality 22:389-97. 2010
    ..Hydrolysis rates are quite similar for the two benzothiadiazines methyl substituted to nitrogen at 2- and 4-positions...
  64. ncbi Dysnatremias in the critical care setting
    Michael L Moritz
    Division of Nephrology, Department of Pediatrics, Children's Hospital of Pittsburgh, University of Pittsburgh School of Medicine, Pittsburgh, PA, USA
    Contrib Nephrol 144:132-57. 2004
  65. ncbi Development of circulatory-renal limitations to angiotensin-converting enzyme inhibitors identifies patients with severe heart failure and early mortality
    Michelle Kittleson
    Departments of Medicine and Cardiology, Brigham and Women's Hospital, 75 Francis Street, Boston, MA 02115, USA
    J Am Coll Cardiol 41:2029-35. 2003
    ..New treatment strategies should be targeted to this population...
  66. ncbi In silico studies of urease inhibitors to explore ligand-enzyme interactions
    Farzana Latif Ansari
    Department of Chemistry, Quaid i Azam University, Islamabad, 45320, Pakistan
    J Enzyme Inhib Med Chem 24:151-6. 2009
    ..This may be ascribed mainly to the difference in the orientation of ring B of the two stereoisomers and the extent of their interaction with Asp224 and Cys322 present in the catalytic core of the enzyme...
  67. ncbi Activity of a potent hepatitis C virus polymerase inhibitor in the chimpanzee model
    Chih Ming Chen
    Abbott Laboratories, Global Pharmaceutical Research and Development, Abbott Park, IL 60064, USA
    Antimicrob Agents Chemother 51:4290-6. 2007
    ..These findings validate the antiviral efficacy and resistance development of benzothiadiazine HCV polymerase inhibitors in vivo...
  68. ncbi Both N-methyl-D-aspartate (NMDA) and non-NMDA receptors mediate glutamate-induced cleavage of the cyclin-dependent kinase 5 (cdk5) activator p35 in cultured rat hippocampal neurons
    Petri Kerokoski
    Department of Neuroscience and Neurology, University of Kuopio, P O Box 1627, 70211 Kuopio, Finland
    Neurosci Lett 368:181-5. 2004
    ..Different factors, such as maturation state of neurons or desensitization properties of non-NMDA receptors, may determine which receptor predominantly mediates the effect of glutamate on p35 cleavage...
  69. ncbi Better Prescribing Project: a randomized controlled trial of the impact of case-based educational modules and personal prescribing feedback on prescribing for hypertension in primary care
    Carol P Herbert
    University of Western Ontario, Faculty of Medicine and Dentistry, Health Sciences Addition, London, Ontario N6A 5C1, Canada
    Fam Pract 21:575-81. 2004
    ..The purpose of this study was to assess the impacts of individualized prescribing feedback and interactive small group education aimed at encouraging evidence-based prescribing in family/general practice...
  70. ncbi Physicochemical evaluation of PVP-thiazide diuretic interactions in co-spray-dried composites--analysis of glass transition composition relationships
    Lidia Tajber
    School of Pharmacy, The University of Dublin, Trinity College, Dublin 2, Ireland
    Eur J Pharm Sci 24:553-63. 2005
    ..The Schneider equation may be successfully applied to fit the Tg-composition profiles obtained, where other models fail to give good predictions...
  71. ncbi AMPA receptor desensitization as a determinant of vulnerability to focally evoked status epilepticus
    Francesco Fornai
    Department of Pharmacology, W215 Research Bldg, 3970 Reservoir Road NW, Georgetown University, Washington, DC 20057, USA
    Eur J Neurosci 21:455-63. 2005
    ....
  72. ncbi 3-(1,1-dioxo-2H-(1,2,4)-benzothiadiazin-3-yl)-4-hydroxy-2(1H)-quinolinones, potent inhibitors of hepatitis C virus RNA-dependent RNA polymerase
    Rosanna Tedesco
    Department of Medicinal Chemistry and Drug Metabolism, The Musculoskeletal, Microbial and Proliferative Diseases Center of Excellence for Drug Discovery, GlaxoSmithKline Pharmaceuticals, Collegeville, PA 19426, USA
    J Med Chem 49:971-83. 2006
    ..The potential for development and safety assessment profile of compound 130 will also be discussed...
  73. ncbi The place of diuretics in preventing cardiovascular events
    N M Kaplan
    The University of Texas Southwestern Medical Center, Dallas, TX 75235 8899, USA
    J Hum Hypertens 18:S29-32. 2004
    ..As lower blood pressure goals of therapy have been found to be needed, diuretic enhancement of other agents' efficacy has become even more essential. With such low doses, side effects are minimal in degree and infrequent in appearance...
  74. ncbi Long-term adaptation of renal ion transporters to chronic diuretic treatment
    Gheun Ho Kim
    Department of Internal Medicine and Institute of Biomedical Sciences, Hanyang University College of Medicine, Seoul, Korea
    Am J Nephrol 24:595-605. 2004
    ..This upregulation of OAT1 seems to be induced by substrate stimulation, lessening diuretic tolerance associated with long-term diuretic use...
  75. ncbi Adsorption of bentazon and propanil from aqueous solutions at the high area activated carbon-cloth
    Erol Ayranci
    Department of Chemistry, Akdeniz University, 07058 Antalya, Turkey
    Chemosphere 57:755-62. 2004
    ..Monolayer capacities determined from Langmuir isotherms of pesticides showed that bentazon has greater monolayer capacity than propanil. This conclusion was also confirmed through the 1/n parameter of Freundlich equation...
  76. ncbi Sodium disorders in the elderly
    Naureen Tareen
    Department of Medicine at the West Los Angeles, Veteran Administration Medical Center, CA, USA
    J Natl Med Assoc 97:217-24. 2005
    ..In this update, we have summarized age-related homeostatic changes that impair sodium balance, medications that alter salt and water handling, and the recognition and management of sodium disorders in elderly patients...
  77. ncbi Cyclothiazide selectively inhibits mGluR1 receptors interacting with a common allosteric site for non-competitive antagonists
    Alexander Surin
    Department of Pharmacology, Georgetown University Medical Center, 3900 Reservoir Road NW, Washington, DC 20057, USA
    Neuropharmacology 52:744-54. 2007
    ....
  78. ncbi Targeting AMPA receptor gating processes with allosteric modulators and mutations
    Nicholas A Mitchell
    Center for Neuropharmacology and Neuroscience, Albany Medical College, Albany, New York 12208, USA
    Biophys J 92:2392-402. 2007
    ....
  79. ncbi Paired-pulse depression at photoreceptor synapses
    Katalin Rabl
    Department of Ophthalmology and Visual Sciences, University of Nebraska Medical Center, Omaha, Nebraska 68198-5840, USA
    J Neurosci 26:2555-63. 2006
    ..Thus, depression of release is not likely to contribute to differences in the kinetics of transmission from rods and cones...
  80. ncbi 3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists
    Yonghui Wang
    Discovery Medicinal Chemistry, Molecular Discovery Research, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, PA 19426, USA
    Bioorg Med Chem Lett 17:3864-7. 2007
    ..Synthesis, structure and activity relationships, selectivity, and some developability properties are described...
  81. ncbi Combination therapy in the management of hypertension: focus on angiotensin receptor blockers combined with diuretics
    Paolo Palatini
    University of Padova, Padova, Italy
    J Clin Hypertens (Greenwich) 7:96-101. 2005
    ..Recent studies have shown that angiotensin II receptor blockers, given alone or combined with a diuretic, may prevent some cardiovascular outcomes independent of their blood pressure-lowering efficacy...
  82. ncbi Chronic magnesium administration enhances oxidative glucose metabolism in thiazide treated hypertensive patients
    G Paolisso
    Department of Geriatric Medicine and Metabolic Diseases, 1st Medical School, University of Naples, Italy
    Am J Hypertens 5:681-6. 1992
    ..In the multiple linear regression analysis of the pooled basal data (n = 42), erythrocyte magnesium content displayed an independent correlation with basal plasma insulin levels (t = -2.08, P < .05).(ABSTRACT TRUNCATED AT 250 WORDS)..
  83. ncbi Fixed combinations of delapril plus indapamide vs fosinopril plus hydrochlorothiazide in mild to moderate essential hypertension
    G Cremonesi
    Chiesi Farmaceutici, Parma, Italy
    Adv Ther 19:129-37. 2002
    ..Four patients in the F + H group dropped out because of adverse events. In this study, the efficacy and safety of D + I were comparable to those of F + H in patients with mild to moderate essential hypertension...
  84. ncbi A desensitization-selective potentiator of AMPA-type glutamate receptors
    Masayuki Sekiguchi
    Department of Degenerative Neurological Diseases, National Institute of Neuroscience, National Center of Neurology and Psychiatry 4 1 1 Ogawahigashi, Kodaira, Tokyo 187 8502, Japan
    Br J Pharmacol 136:1033-41. 2002
    ....
  85. ncbi Hypertension guidelines in elderly patients: is anybody listening?
    Karen Tu
    Institute for Clinical Evaluative Services, G106 2075 Bayview Avenue, Toronto, Ontario M4N 3M5, Canada
    Am J Med 113:52-8. 2002
    ....
  86. ncbi AMPA and NMDA currents show different short-term depression in the dorsal lateral geniculate nucleus of the rat
    Anders Kielland
    University of Oslo, Institute of Basic Medical Sciences, Department of Physiology, P O Box 1103 Blindern, N 0317 Oslo, Norway
    J Physiol 542:99-106. 2002
    ....
  87. ncbi Chloride increases adrenergic receptor-mediated platelet and vascular responses
    Henrikas Vaitkevicius
    Wayne State University School of Medicine, Detroit, Michigan, USA
    Am J Hypertens 15:492-8. 2002
    ..The ensuing reduction in [Cl-]i that is induced by diuretics in these tissues could play a role in reducing the effect of catecholamines on precipitating thrombotic stroke or myocardial infarction...
  88. ncbi The expression of cerebellar LTD in culture is not associated with changes in AMPA-receptor kinetics, agonist affinity, or unitary conductance
    D J Linden
    Department of Neuroscience, Johns Hopkins University School of Medicine, 725 North Wolfe Street, Baltimore, MD 21205, USA
    Proc Natl Acad Sci U S A 98:14066-71. 2001
    ..These results suggest that cerebellar LTD may be expressed solely as a reduction in the number of functional AMPA receptors in the postsynaptic density [Wang, Y.-T. & Linden, D. J. (2000) Neuron 25, 635-664]...
  89. ncbi Determination of bentazone, dichlorprop, and MCPA in different soils by sodium hydroxide extraction in combination with solid-phase preconcentration
    C W Thorstensen
    The Norwegian Crop Research Institute, Plant Protection, Høgskoleveien 7, N 1432 As, Norway
    J Agric Food Chem 49:4199-202. 2001
    ..4 (Hole), 2.5 (Kroer), and 37.8% (Froland) organic carbon, respectively. Limits of quantification using GC-MS were 0.0003 microg/g of wet soil for bentazone and 0.0001 microg/g of wet soil for both dichlorprop and MCPA...
  90. ncbi Laboratory degradation studies of bentazone, dichlorprop, MCPA, and propiconazole in Norwegian soils
    C W Thorstensen
    The Norwegian Crop Research Institute, Plant Protection, As, Norway
    J Environ Qual 30:947-53. 2001
    ..Pesticide degradation was approximated to first-order kinetics. Slow rates of degradation, where more than 50% of the pesticide remained in the soil after the 84-d duration of the experiment, did not fit well with first-order kinetics...
  91. ncbi Mechanisms underlying presynaptic facilitatory effect of cyclothiazide at the calyx of Held of juvenile rats
    T Ishikawa
    Department of Neurophysiology, University of Tokyo, Faculty of Medicine, Hongo 7-3-1, Bunkyo-ku, Tokyo 113-0033, Japan
    J Physiol 533:423-31. 2001
    ..6. We conclude that CTZ facilitates transmitter release through suppression of presynaptic potassium conductance and stimulation of exocytotic machinery downstream of Ca(2+) influx...
  92. ncbi Positive allosteric modulators of AMPA receptors reduce proton-induced receptor desensitization in rat hippocampal neurons
    S Lei
    Departments of Physiology and Pharmacology and Anaesthesia, University of Toronto, Toronto M5S 1A8, Ontario K7L 3N6, Canada
    J Neurophysiol 85:2030-8. 2001
    ..These results demonstrate that a reduction in the proton sensitivity of receptor desensitization contributes to the mechanism of action of some positive modulators of AMPA receptors...
  93. ncbi Studies of enantiomerization of chiral 3,4-dihydro-1,2,4-benzothiadiazine 1,1-dioxide type compounds
    G Cannazza
    Dipartimento di Scienze Farmaceutiche, Universita degli Studi di Modena e Reggio Emilia, Modena, Italy
    Chirality 13:94-101. 2001
    ....
  94. ncbi Is there a preferred antihypertensive therapy for isolated systolic hypertension and reduced arterial compliance?
    S S Franklin
    UCI Heart Disease Prevention Program, C240 Medical Sciences, University of California, Irvine, CA 92697, USA
    Curr Hypertens Rep 2:253-9. 2000
    ....
  95. ncbi Effects of S 18986-1, a novel cognitive enhancer, on memory performances in an object recognition task in rats
    C Lebrun
    Division of Cerebral Pathology, Institut de Recherches Servier, 125, Chemin de Ronde, 78290 Croissy sur Seine, France
    Eur J Pharmacol 401:205-12. 2000
    ..Furthermore, S 18986-1 was long-acting and demonstrated a good oral bioavailability. These data confer on S 18986-1, a potential role in improving episodic memory impaired in neurodegenerative diseases and during aging...
  96. ncbi Role of non-NMDA receptors in osmotic and glutamate stimulation of vasopressin release: effect of rapid receptor desensitization
    C D Sladek
    Department of Physiology and Biophysics, Finch University of Health Sciences The Chicago Medical School, IL 60064, USA
    J Neuroendocrinol 10:897-903. 1998
    ..These results support a role for non-NMDA receptor activation in osmotic regulation of VP release...
  97. ncbi Association of a mutation in thiazide-sensitive Na-Cl cotransporter with familial Gitelman's syndrome
    K Takeuchi
    Second Department of Internal Medicine, Tohoku University School of Medicine, Sendai, Japan
    J Clin Endocrinol Metab 81:4496-9. 1996
    ....
  98. ncbi Efficacy and safety of cilazapril, a new angiotensin-converting enzyme inhibitor
    R C Goldszer
    Department of Internal Medicine, Brigham and Women's Hospital, Boston, Massachusetts
    Am J Hypertens 1:300S-302S. 1988
    ..There was no change in standing or sitting heart rate, white blood cell count, creatinine clearance, urine protein levels. This is the first long-term data on this new converting enzyme inhibitor in human beings...
  99. ncbi Angiotensin-converting enzyme inhibitors in the treatment of mild to moderate essential hypertension
    A Salvetti
    Cattedra di Terapia Medica Sistematica, Clinica Medica I, University of Pisa, Italy
    Am J Hypertens 2:94S-99S. 1989
    ..However, although available data suggest that ACEIs can be considered a further advance in the treatment of hypertension, more extensive information is needed to confirm these promising results...
  100. ncbi Medicaid prescriber compliance with Joint National Committee VI Hypertension Treatment Guidelines
    Steven L Clause
    Albany College of Pharmacy, Albany, NY 12208, USA
    Ann Pharmacother 36:1505-11. 2002
    ..CONCLUSIONS: Single-drug therapy of hypertension in a nonhospitalized New York state Medicaid population from 1994 through 1999 did not closely follow JNC recommendations for the single-agent treatment of hypertension...
  101. ncbi AMPA receptor potentiators for the treatment of CNS disorders
    MICHAEL J O'NEILL
    Eli Lilly and Co Ltd, Lilly Research Centre, Erl Wood Manor, Windlesham, Surrey GU20 6PH, UK
    Curr Drug Targets CNS Neurol Disord 3:181-94. 2004
    ....

Research Grants98

  1. Differential effects of TARPs on AMPA receptor subunits
    AMY ARAI; Fiscal Year: 2007
    ....
  2. DIFFERENCES IN SYNAPTIC VS NONSYNAPTIC AMPA RECEPTORS
    AMY ARAI; Fiscal Year: 2004
    ..Determining which cellular factor stabilizes the low-affinity receptors will constitute the Fifth Aim of this application. ..
  3. Seizures & Amydala-Based Socioemotional Dysfunction
    Ludise Malkova; Fiscal Year: 2007
    ..The team is ideally suited to approach the analysis of comorbidity of seizures and autistic-like symptoms evoked from amygdala and to permit a translationally meaningful analysis of the animal data. ..
  4. Control of Synaptic Glutamate Release
    Steven Mennerick; Fiscal Year: 2007
    ....
  5. Synaptic Pathways in the Mammalian Retina
    EDMUND TREXLER; Fiscal Year: 2007
    ..abstract_text> ..
  6. Neural Substrates of Socioemotional Development
    Ludise Malkova; Fiscal Year: 2007
    ..Structured activities and short courses will guide the development of expertise in these areas necessary for the proposed studies as well as for the long-term career advancement of the candidate as a versatile neuroscientist. ..
  7. Home Automatic external Defibrillator Training
    Thomas Rea; Fiscal Year: 2007
    ..Alternatively, if nominal video-based approaches achieve comparable outcomes, training efforts can be streamlined at considerable cost savings with fewer impediments for distribution and dissemination. ..
  8. In Vitro Mechanisms of Ethanol Induced Neuronal Death.
    Steven Mennerick; Fiscal Year: 2005
    ..The proposed experiments should lead to a better fundamental understanding of the mechanisms by which forebrain neurons are susceptible to ethanol-induced death. ..
  9. Synaptic Transmission in the Mammalian Inner Retina
    JOSHUA SINGER; Fiscal Year: 2007
    ..abstract_text> ..
  10. Glutamate Receptor Desensitization and its Modulation
    KATHRYN PARTIN; Fiscal Year: 2005
    ....
  11. Pseudopteroxazole and Related Antitubercular Agents
    Michael Harmata; Fiscal Year: 2007
    ..More generally, the methodology to be developed should have extremely broad impact, as it can be applied to the generation of stereogenic centers in a large number of compounds of biological and medicinal interest. ..
  12. EFFECTS OF ACID ON BONE
    David A Bushinsky; Fiscal Year: 2010
    ..The current proposal is aimed at understanding the first steps by which acid is detected by bone cells. Understanding the process by which the bone detects and neutralizes the acid can lead to an improvement in bone health. ..
  13. Axonal Signaling in the Hippocampus
    Steven J Mennerick; Fiscal Year: 2010
    ..Our results will also lead to cellular insights into the mechanism of brain stimulation techniques currently used in the treatment of movement disorders and neuropsychiatric disease. ..
  14. Synaptic transmission in the rod pathway of the mammalian retina
    Joshua H Singer; Fiscal Year: 2010
    ..4 are responsible for X-linked incomplete congenital stationary night blindness, understanding the role that these channels play normally in synaptic transmission may provide insight into this disease. ..
  15. Contribution of increased VDR and CaR to Hypercalciuria in the GHS Rat
    David A Bushinsky; Fiscal Year: 2010
    ..These studies will advance research on hypercalciuria and may ultimately lead to improved care of patients with kidney stones. ..
  16. Glutamate Receptor Desensitization and its Modulation
    KATHRYN MCKAY PARTIN; Fiscal Year: 2010
    ..A biophysical approach to study modulation of deactivation and desensitization using drugs that have intrinsically different modes of action may better direct future efforts to design AMPA-selective, cognition-enhancing drugs. ..
  17. Use-dependent intrinsic plasticity in the cerebellum
    David Linden; Fiscal Year: 2009
    ..Because these cellular and molecular processes are not only involved in memory storage, this work has implications for other brain diseases as well, including epilepsy and addiction. ..
  18. EFFECTS OF ACID ON BONE
    David Bushinsky; Fiscal Year: 2009
    ..The current proposal is aimed at understanding the first steps by which acid is detected by bone cells. Understanding the process by which the bone detects and neutralizes the acid can lead to an improvement in bone health. ..
  19. CRCNS: Biophysical properties of parallel neural circuits serving night vision
    Joshua H Singer; Fiscal Year: 2010
    ..g., at the annual Society for Neuroscience meeting) to bring together researchers working on combined experimental and computational studies of neural circuits. ..
  20. Hypoglycemia in the Developing Diabetic Brain
    Kelvin Yamada; Fiscal Year: 2005
    ..g., spatial motor, memory, leaning tasks), and finally addressing whether hypoglycemia and diabetes have synergistic injurious effects upon the developing brain. ..
  21. EFFECTS OF ACID ON BONE
    David Bushinsky; Fiscal Year: 2004
    ..Our long term goal is to develop a model to describe how acidosis affects bone in order to devise therapy to preserve mineral while maintaining the H+ buffering properties of bone. ..
  22. CLINICAL PHARMACOLOGY OF LOOP DIURETICS
    D Brater; Fiscal Year: 1999
    ..This proposal begins a long-term attempt to unravel these factors with an ultimate goal of designing therapeutic strategies in patients with CHF which decrease the frequency of decompensation. ..
  23. CLINICAL PHARMACOLOGY OF LOOP DIURETICS
    D Brater; Fiscal Year: 2004
    ..These data will provide insights into the causes and pathophysiology of decompensation in patients with CHF, thus enhancing our understanding of this increasingly prevalent disease and leading to better therapeutic strategies. ..
  24. Regulation of thiazide-sensitive NaCl transport
    David H Ellison; Fiscal Year: 2010
    ..A large portion of hypertension is related to genetics. This proposal will help unravel genetic contributions to human blood pressure variation, with the goal of finding better treatments, or better preventive maneuvers. ..
  25. BENZANNULATION APPROACH TO BIARYL ETHERS
    Michael Harmata; Fiscal Year: 2001
    ..abstract_text> ..
  26. Glial-cytokine-neuronal interactions in neuropathic pain
    Han Rong Weng; Fiscal Year: 2010
    ..1 ..
  27. Human genetic variation and ventricular fibrillation resuscitation outcomes
    Thomas D Rea; Fiscal Year: 2010
    ..Analyses will incorporate standard and novel approaches of genetic association to assess if and how genetic variation influences resuscitation outcome. ..
  28. Synaptic transmission in the rod pathway of the mammalian retina
    JOSHUA SINGER; Fiscal Year: 2007
    ..4 are responsible for X-linked incomplete congenital stationary night blindness, understanding the role that these channels play normally in synaptic transmission may provide insight into this disease. ..
  29. Cost-effectiveness of genetic screening for colon cancer
    Sandeep Vijan; Fiscal Year: 2006
    ..Outcome measures: The risks of developing or dying from CRC, the costs of screening, and the incremental cost-effectiveness of various screening regimens. ..
  30. REGULATION OF THIAZIDE SENSITIVE NACL TRANSPORT
    David Ellison; Fiscal Year: 2003
    ..The underlying hypothesis of these experiments is that some Gitelman's mutations impair protein-protein interactions that are crucial for maintenance of transport activity. ..
  31. NEURONAL INFORMATION STORAGE IN CEREBELLAR DEEP NUCLEI
    David Linden; Fiscal Year: 2004
    ..In addition, they have potential clinical relevance for both cerebellar motor disorders and disorders of learning and memory generally. ..
  32. LONG TERM POTENTIATION AND DEPRESSION IN THE CEREBELLUM
    David Linden; Fiscal Year: 2002
    ..In addition, these investigations have potential clinical relevance not only for cerebellar motor disorders, but also for disorders of learning and memory generally. ..
  33. EFFECTS OF ACID ON BONE
    David Bushinsky; Fiscal Year: 2007
    ..The current proposal is aimed at understanding the first steps by which acid is detected by bone cells. Understanding the process by which the bone detects and neutralizes the acid can lead to an improvement in bone health. ..
  34. CELLULAR SUBSTRATES OF CEREBELLAR INFORMATION STORAGE
    David Linden; Fiscal Year: 2007
    ..In addition, they have potential clinical relevance for both cerebellar motor disorders and disorders of learning and memory generally...
  35. Regulation of thiazide-sensitive NaCl transport
    David Ellison; Fiscal Year: 2007
    ..Although Mendelian forms of hypertension are rare, they help to elucidate mechanisms of blood pressure regulation that almost certainly contribute to the more common essential variety. ..
  36. Reducing Adverse Self-Medication Behaviors in Older Adults with Hypertension
    Patricia Neafsey; Fiscal Year: 2007
    ..Healthcare utilization will be compared between the 2 groups after 52 weeks and a cost-benefit analysis conducted. ..