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. pmc Cyclothiazide induces robust epileptiform activity in rat hippocampal neurons both in vitro and in vivo
    Jinshun Qi
    Department of Biology, 201 Life Sciences Building, The Pennsylvania State University, University Park, PA 16802, USA
    J Physiol 571:605-18. 2006
  2. pmc Cyclothiazide induces seizure behavior in freely moving rats
    Shuzhen Kong
    Research Centre of Medicinal Chemistry and Chemical Biology, Chongqing Technology and Business University, Chongqing, China
    Brain Res 1355:207-13. 2010
  3. pmc Downregulation of tonic GABA currents following epileptogenic stimulation of rat hippocampal cultures
    Jin Shun Qi
    Department of Biology, 201 Life Sciences Building, Huck Institutes of Life Sciences, The Pennsylvania State University, University Park, PA 16802, USA
    J Physiol 577:579-90. 2006
  4. ncbi Epileptiform response of CA1 neurones to convulsant stimulation by cyclothiazide, kainic acid and pentylenetetrazol in anaesthetized rats
    Binbin Qian
    Institutes of Brain Science, State Key Laboratory for Medical Neurobiology, Fudan University, Shanghai 200032, China
    Seizure 20:312-9. 2011
  5. pmc BDNF-TrkB signaling pathway mediates the induction of epileptiform activity induced by a convulsant drug cyclothiazide
    Yun Wang
    Institutes of Brain Science and State Key Laboratory for Medical Neurobiology, Fudan University, Shanghai 200032, China
    Neuropharmacology 57:49-59. 2009
  6. ncbi Comparative toxicity of bentazon and molinate on growth, photosynthetic pigments, photosynthesis, and respiration of the Portuguese ricefield cyanobacterium Nostoc muscorum
    Victor Galhano
    Department of Biology and Environmental Engineering Centre for Research and Technology of Agro Environment and Biological Sciences, University of Tras os Montes and Alto Douro, Apartado 1013 5001 801 Vila Real, Portugal
    Environ Toxicol 25:147-56. 2010
  7. ncbi Map-based cloning of a novel rice cytochrome P450 gene CYP81A6 that confers resistance to two different classes of herbicides
    Gang Pan
    College of Agriculture and Biotechnology, Zhejiang University, Hangzhou, 310029, Zhejiang, China
    Plant Mol Biol 61:933-43. 2006
  8. ncbi BPDZ 154 activates adenosine 5'-triphosphate-sensitive potassium channels: in vitro studies using rodent insulin-secreting cells and islets isolated from patients with hyperinsulinism
    Karen E Cosgrove
    Department of Biomedical Science, Institute of Molecular Physiology, University of Sheffield, Western Bank, Sheffield S10 2TN, UK
    J Clin Endocrinol Metab 87:4860-8. 2002
  9. ncbi Second generation of hydroxyethylamine BACE-1 inhibitors: optimizing potency and oral bioavailability
    Nicolas Charrier
    Neurology and Gastrointestinal Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Park, Harlow, Essex, UK
    J Med Chem 51:3313-7. 2008
  10. pmc Cyclothiazide: a subunit-specific inhibitor of GABAC receptors
    An Xie
    Department of Ophthalmology and Visual Sciences, University of Illinois at Chicago, 1855 W Taylor Street, Chicago, IL 60612, USA
    J Physiol 586:2743-52. 2008

Research Grants

Detail Information

Publications187 found, 100 shown here

  1. pmc Cyclothiazide induces robust epileptiform activity in rat hippocampal neurons both in vitro and in vivo
    Jinshun Qi
    Department of Biology, 201 Life Sciences Building, The Pennsylvania State University, University Park, PA 16802, USA
    J Physiol 571:605-18. 2006
    ..The long-lasting epileptiform activity after CTZ washout may also make it a very useful model in screening antiepileptic drugs...
  2. pmc Cyclothiazide induces seizure behavior in freely moving rats
    Shuzhen Kong
    Research Centre of Medicinal Chemistry and Chemical Biology, Chongqing Technology and Business University, Chongqing, China
    Brain Res 1355:207-13. 2010
    ..Since CTZ acts on both GABAergic and glutamatergic systems, this new animal epilepsy model will be useful for anticonvulsant drug testing and general epilepsy research...
  3. pmc Downregulation of tonic GABA currents following epileptogenic stimulation of rat hippocampal cultures
    Jin Shun Qi
    Department of Biology, 201 Life Sciences Building, Huck Institutes of Life Sciences, The Pennsylvania State University, University Park, PA 16802, USA
    J Physiol 577:579-90. 2006
    ..Thus, in addition to synaptic alteration of GABAergic transmission, regulation of tonic inhibition may also play an important role during epileptogenesis...
  4. ncbi Epileptiform response of CA1 neurones to convulsant stimulation by cyclothiazide, kainic acid and pentylenetetrazol in anaesthetized rats
    Binbin Qian
    Institutes of Brain Science, State Key Laboratory for Medical Neurobiology, Fudan University, Shanghai 200032, China
    Seizure 20:312-9. 2011
    ..The results from this study indicate that hippocampal neurons respond to various convulsant stimulation differently which may reflect the complicated causes of the seizure in clinics...
  5. pmc BDNF-TrkB signaling pathway mediates the induction of epileptiform activity induced by a convulsant drug cyclothiazide
    Yun Wang
    Institutes of Brain Science and State Key Laboratory for Medical Neurobiology, Fudan University, Shanghai 200032, China
    Neuropharmacology 57:49-59. 2009
    ..We conclude that activation of BDNF-TrkB signaling pathway is fundamentally important during the CTZ-induction of epileptiform activity both in vitro and in vivo...
  6. ncbi Comparative toxicity of bentazon and molinate on growth, photosynthetic pigments, photosynthesis, and respiration of the Portuguese ricefield cyanobacterium Nostoc muscorum
    Victor Galhano
    Department of Biology and Environmental Engineering Centre for Research and Technology of Agro Environment and Biological Sciences, University of Tras os Montes and Alto Douro, Apartado 1013 5001 801 Vila Real, Portugal
    Environ Toxicol 25:147-56. 2010
    ..5-2 mM). The herbicides had contrasting effects on carbohydrates content: molinate increased this organic fraction whereas bentazon decreased it. Photosynthesis and respiration were inhibited by both herbicides...
  7. ncbi Map-based cloning of a novel rice cytochrome P450 gene CYP81A6 that confers resistance to two different classes of herbicides
    Gang Pan
    College of Agriculture and Biotechnology, Zhejiang University, Hangzhou, 310029, Zhejiang, China
    Plant Mol Biol 61:933-43. 2006
    ..Based on these results we conclude that the novel cytochrome P450 monooxygenase CYP81A6 encoded by Bel confers resistance to two different classes of herbicides...
  8. ncbi BPDZ 154 activates adenosine 5'-triphosphate-sensitive potassium channels: in vitro studies using rodent insulin-secreting cells and islets isolated from patients with hyperinsulinism
    Karen E Cosgrove
    Department of Biomedical Science, Institute of Molecular Physiology, University of Sheffield, Western Bank, Sheffield S10 2TN, UK
    J Clin Endocrinol Metab 87:4860-8. 2002
    ..These data suggest that BPDZ 154 or BPDZ 154-like compounds may have therapeutic potential in the treatment of certain forms of hyperinsulinism...
  9. ncbi Second generation of hydroxyethylamine BACE-1 inhibitors: optimizing potency and oral bioavailability
    Nicolas Charrier
    Neurology and Gastrointestinal Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Park, Harlow, Essex, UK
    J Med Chem 51:3313-7. 2008
    ..Optimization of a first generation of BACE-1 inhibitors led to the discovery of novel hydroxyethylamines (HEAs) bearing a tricyclic nonprime side. These derivatives have nanomolar cell potency and are orally bioavailable...
  10. pmc Cyclothiazide: a subunit-specific inhibitor of GABAC receptors
    An Xie
    Department of Ophthalmology and Visual Sciences, University of Illinois at Chicago, 1855 W Taylor Street, Chicago, IL 60612, USA
    J Physiol 586:2743-52. 2008
    ..4 s, but the kinetics were approximately 10-fold slower when GABA is absent. The ability of CTZ to interact with various types of neurotransmitter receptors indicates that the drug has multiple actions in the CNS...
  11. 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...
  12. pmc 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 ..
  13. ncbi Des-A-ring benzothiadiazines: inhibitors of HCV genotype 1 NS5B RNA-dependent RNA polymerase
    Pamela L Donner
    Antiviral Research, Global Pharmaceutical Research, and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
    Bioorg Med Chem Lett 18:2735-8. 2008
    ..We observed that small aromatic rings and alkenyl groups appended to the 5-position of the B-ring were optimal, resulting in inhibitors with low nanomolar potencies...
  14. ncbi Photocatalytic degradation of bentazone in soil washing wastes containing alkylpolyoxyethylene surfactants
    M Davezza
    Dipartimento di Chimica Analitica, Universita di Torino, 10125 Torino, Italy
    Chemosphere 86:335-40. 2012
    ..Useful information about the photocatalytic degradation route was obtained from the HPLC-MS analysis of transient intermediates formed in water...
  15. ncbi Induction and inactivation of a cytochrome P450 confering herbicide resistance in wheat seedlings
    N Forthoffer
    , CNRS-UPR 406, , Strasbourg, France
    Eur J Drug Metab Pharmacokinet 26:9-16. 2001
    ..This increased capacity of wheat to detoxify the herbicide through the induction of P450 enzymes seems to be for a large extend the mechanism which confers a tolerance on various herbicides...
  16. ncbi Determination of two phototransformation products of bentazone using quadrupole time-of-flight mass spectrometry
    Manuela Peschka
    Europa University of Applied Sciences, Limburger Strasse 2, Idstein, Germany
    Anal Bioanal Chem 388:1227-34. 2007
    ..The required irradiation time was matrix dependent. 2-(Isopropylcarbamoyl)phenylsulfamic acid was detected in a drainage channel in the Ebro river delta (Catalonia, Spain)...
  17. pmc 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
    ....
  18. pmc 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...
  19. 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
    ....
  20. 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...
  21. pmc 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...
  22. 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
    ....
  23. 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...
  24. 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
  25. ncbi [ALLHAT trial--antithesis to the overuse of vasodilating antihypertensive drugs]
    Iwao Kuwajima
    Division of Internal Medicine, Tokyo Metropolitan Geriatric Hospital
    Nihon Rinsho 62:648-53. 2004
  26. ncbi [Policy of antihypertensive therapy in arterial hypertension in the elderly. II]
    M A Gurevich
    Klin Med (Mosk) 80:9-13. 2002
  27. 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
    ....
  28. ncbi [Comrades! There must be some blood order in the field of hypertension!]
    Arne Melander
    NEPI, Malmö och Stockholm
    Lakartidningen 102:1068-70. 2005
  29. ncbi The return on INVEST
    Michael H Alderman
    JAMA 290:2859-61. 2003
  30. 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...
  31. 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
  32. 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...
  33. 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
    ....
  34. ncbi [Consequences of ALLHAT: Thiazides rehabilitated--time to change prescription patterns]
    Anders Hernborg
    Avdelningen för medicin, Universitetssjukhuset MAS, Malmo
    Lakartidningen 100:408-10. 2003
  35. 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...
  36. 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...
  37. 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...
  38. ncbi [Tax payers have payed billions for the "blood pressure maffia's" actions]
    Bengt Järhult
    Lakartidningen 100:1917-8. 2003
  39. 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...
  40. 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
  41. 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
  42. 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
    ....
  43. 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
  44. ncbi [ALLHAT=other leading physicians have alternative interpretations]
    Alan Charles
    Lakartidningen 100:2073-4. 2003
  45. 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...
  46. 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...
  47. 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
    ....
  48. ncbi [Thiazides or ACE inhibitors? A drug-economic analysis]
    Ivar Aursnes
    Tidsskr Nor Laegeforen 124:1668. 2004
  49. 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...
  50. 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...
  51. ncbi Treating high blood pressure in Africans with type 2 diabetes
    E O Okoro
    Ethn Dis 14:160-1. 2004
  52. 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
    ....
  53. ncbi Following evidence-based prescribing guidelines for antihypertensives could save big bucks
    Gina Rollins
    Rep Med Guidel Outcomes Res 15:1, 6-7. 2004
  54. 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...
  55. 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
    ....
  56. 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...
  57. 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
    ....
  58. 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
    ....
  59. ncbi Angiotensin-converting enzyme inhibitors and diuretics: optimal combination therapy
    Mori J Krantz
    Ann Intern Med 141:893; author reply 893. 2004
  60. 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...
  61. 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...
  62. 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...
  63. 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
  64. ncbi Hypertension: treatment--now & tomorrow
    Chike M Nzerue
    Ethn Dis 12:S2-43-5. 2002
  65. 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
  66. 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...
  67. pmc 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...
  68. 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 ..
  69. 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...
  70. 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)...
  71. 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...
  72. ncbi Coupling of AMPA receptors with the Na(+)/Ca(2+) exchanger in cultured rat astrocytes
    J P Smith
    Department of Neurosciences, University of New Mexico, School of Medicine, Albuquerque, NM 87131, USA
    Brain Res 887:98-109. 2000
    ..This proposed mechanism requires neither Ca(2+)-permeant AMPARs nor the activation of VGCCs to be effective...
  73. ncbi Effects of the AMPA receptor modulator S 18986 on measures of cognition and oxidative stress in aged rats
    S J Kelly
    Department of Psychology, University of South Carolina, Columbia, SC 29208, USA
    Psychopharmacology (Berl) 202:225-35. 2009
    ..Development of cognitive-enhancing drugs that delay or halt mild cognitive impairment progression to Alzheimer's disease would be of great benefit...
  74. pmc 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...
  75. ncbi AMPA-preferring receptors mediate excitatory non-NMDA responses of primate retinal ganglion cells
    R A Jacoby
    Department of Opthalmology, Cullen Eye Institute, Baylor College of Medicine, Houston, TX 77030, USA
    Vis Neurosci 18:703-10. 2001
    ..We conclude that the non-NMDA component of the excitatory, glutamatergic input to primate ganglion cells is mediated largely by AMPA-preferring receptors, with little, if any, kainate-preferring receptor-mediated response...
  76. ncbi Functional Gitelman syndrome?
    Peter Gross
    Am J Kidney Dis 43:586; author reply 586-7. 2004
  77. ncbi Determination of kinetic parameters of enantiomerization of benzothiadiazines by DCXplorer
    Giuseppe Cannazza
    Dipartimento di Scienze Farmaceutiche, Universita degli Studi di Modena e Reggio Emilia, 4100 Modena, Italy
    Chirality 22:789-97. 2010
    b>Benzothiadiazines differently substituted at the sulfonamidic nitrogen atom, at the stereogenic carbon atom and at the anilinic nitrogen atom have been synthesized and fully characterized...
  78. pmc The effects of thiazide diuretics on bone mineral metabolism
    R O Pierce
    Department of Orthopaedic Surgery, Indiana University School of Medicine, Indianapolis 46208, USA
    J Natl Med Assoc 90:46-50. 1998
    ..At the end of 35 days postinjury, all animals were sacrificed. Biochemical and biomechanical results were analyzed, and revealed that animals that received thiazide diuretics and a fracture had the highest bone mineral content...
  79. ncbi Effects of the herbicide bentazon on growth and photosystem II maximum quantum yield of the marine diatom Skeletonema costatum
    R S Macedo
    Programa de Pós Graduação em Ecologia e Conservação, Universidade Federal do Parana, Centro Politecnico, Curitiba, Parana, Brazil
    Toxicol In Vitro 22:716-22. 2008
    ....
  80. ncbi Inverse modelling for estimating sorption and degradation parameters for pesticides
    Igor G Dubus
    Cranfield Centre for EcoChemistry, Cranfield University, Silsoe, Bedfordshire, MK45 4DT, UK
    Pest Manag Sci 60:859-74. 2004
    ..Research is needed to identify data requirements for robust estimation of sorption and degradation parameters through calibration of pesticide fate models against leaching data...
  81. ncbi Oxaluria--the neglected stepchild of nephrolithiasis?
    Glenn M Preminger
    J Urol 170:402-3. 2003
  82. ncbi Hypertension therapy: mixing, matching, and meeting targets
    Massimo Volpe
    Faculty of Medicine, University of Rome La Sapienza, Osp Sant Andrea IRCCS Neuromed Pozzilli IS, Rome, Italy
    Adv Ther 21:107-22. 2004
    ..In addition, angiotensin-receptor blocker/diuretic combinations may have cardiovascular benefits beyond those from blood pressure lowering itself...
  83. ncbi Angiotensin-receptor blockers and diuretics--advantages of combination
    A Mimran
    Department of Medicine, University of Montpellier, Montpellier, France
    Blood Press 14:6-11. 2005
    ..The combination of an ARB and a thiazide diuretic may be of particular value in patient populations who tend to have poor BP control on monotherapy, or have additional cardiovascular or renal risk factors...
  84. ncbi Piperidine carboxylic acid derivatives of 10H-pyrazino[2,3-b][1,4]benzothiazine as orally-active adhesion molecule inhibitors
    Toshihiko Kaneko
    Tsukuba Research Laboratories, Eisai Co Ltd, 5 1 3 Tokudai, Tsukuba, Ibaraki 300 2635, Japan
    Chem Pharm Bull (Tokyo) 52:675-87. 2004
    ....
  85. ncbi [Thiazides one more time]
    Terje Forslund
    Tidsskr Nor Laegeforen 125:919. 2005
  86. ncbi [Why not always diuretics?]
    Per Omvik
    Hjerteavdelingen, Haukeland Universitetssykehus, 5021 Bergen
    Tidsskr Nor Laegeforen 124:1419-20. 2004
    ..The resolution was supported by results from the ALLHAT study (antihypertensive and lipid-lowering treatment to prevent heart attack trial)...
  87. ncbi Triphenylphosphonium salts of 1,2,4-benzothiadiazine 1,1-dioxides related to diazoxide targeting mitochondrial ATP-sensitive potassium channels
    Céline Constant-Urban
    Department of Medicinal Chemistry, Center for Interdisciplinary Research on Medicines CIRM, University of Liege, 1, Avenue de l Hopital, B 4000 Liege, Belgium
    Bioorg Med Chem Lett 23:5878-81. 2013
    ..However, the most active (inhibition of insulin release) compound 17 was found to penetrate the cardiac cells and to reach mitochondria. ..
  88. ncbi Enhanced relative expression of glutamate receptor 1 flip AMPA receptor subunits in hippocampal astrocytes of epilepsy patients with Ammon's horn sclerosis
    Gerald Seifert
    Experimental Neurobiology, Department of Neurosurgery, University of Bonn, 53105 Bonn, Germany
    J Neurosci 24:1996-2003. 2004
    ..These findings imply that in AHS, glutamate may lead to prolonged depolarization of astrocytes, thereby facilitating the generation or spread of seizure activity...
  89. 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...
  90. ncbi Modulation of AMPA receptor kinetics differentially influences synaptic plasticity in the hippocampus
    A C Arai
    Department of Pharmacology, Southern Illinois University School of Medicine, MC 9629, 801 North Rutledge Street, Springfield, IL 62702, USA
    Neuroscience 123:1011-24. 2004
    ....
  91. ncbi DRUG FOCUS: S 18986: A positive allosteric modulator of AMPA-type glutamate receptors pharmacological profile of a novel cognitive enhancer
    Katy Bernard
    Institut de Recherches Internationales Servier, Courbevoie, France
    CNS Neurosci Ther 16:e193-212. 2010
    ..From these results, S 18986 is expected to treat memory deficits associated with early cerebral aging and neurological diseases in elderly people...
  92. ncbi Inhibitors of hepatitis C virus polymerase: synthesis and biological characterization of unsymmetrical dialkyl-hydroxynaphthalenoyl-benzothiadiazines
    Rolf Wagner
    Global Pharmaceutical Research and Development, Abbott, Abbott Park, Illinois 60064, USA
    J Med Chem 52:1659-69. 2009
    ..of HCV polymerase inhibitors resulted in the identification of unsymmetrical dialkyl-hydroxynaphthalenoyl-benzothiadiazines 2 and 3...
  93. ncbi Long-term diuretic therapy: effects of dose reduction on antihypertensive efficacy and counterregulatory systems
    B Weisser
    Medizinische Poliklinik, University of Bonn, Germany
    J Cardiovasc Pharmacol 19:361-6. 1992
    ..Furthermore, our results indicate that long-term studies might be necessary to assess the full antihypertensive potential of low doses of antihypertensive agents...
  94. ncbi Role of GluR2 expression in AMPA-induced toxicity in cultured murine cerebral cortical neurons
    J B Jensen
    The Royal Danish School of Pharmacy, NeuroScience PharmaBiotech Research Center, Department of Pharmacology, 2 Universitetsparken, DK-2100 Copenhagen, Denmark
    J Neurosci Res 65:267-77. 2001
    ..The components of direct AMPA-R-mediated toxicity are proposed to be 1) toxicity mediated by GluR2(R)-lacking AMPA-R and 2) toxicity mediated by low-Ca(2+)-permeability AMPA-R containing GluR2(R)...
  95. ncbi (S)-2,3-dihydro-[3,4]cyclopentano-1,2,4-benzothiadiazine-1,1-dioxide: (S18986-1) a positive modulator of AMPA receptors enhances (S)-AMPA-mediated [3H]noradrenaline release from rat hippocampal and frontal cortex slices
    B Lockhart
    Institut de Recherches Servier, Division of Cerebral Pathology, 125, Chemin de Ronde, 78290 Croissy sur Seine, France
    Eur J Pharmacol 401:145-53. 2000
    ..These results suggest that the capacity of S18986-1 to enhance AMPA receptor-mediated release of noradrenaline in rat hippocampus and frontal cortex, could contribute to the cognition enhancing mechanisms of S18986-1...
  96. ncbi [Hyponatremic crisis--a serious side effect of diuretics in the elderly]
    J O Aaseth
    Medisinsk avdeling Kongsvinger sjukehus 2226 Kongsvinger
    Tidsskr Nor Laegeforen 121:921-3. 2001
    ..Previous reports indicate that elderly women develop more severe manifestations than men. The risk of developing hyponatremia increases when thiazide diuretics are given simultaneously with NSAIDs...
  97. pmc Pharmacological analysis of the activation and receptor properties of the tonic GABA(C)R current in retinal bipolar cell terminals
    Stefanie M Jones
    Neuroscience Group, Institute for Science and Technology in Medicine, Keele University, Keele, United Kingdom
    PLoS ONE 6:e24892. 2011
    ..These results extend our understanding of the multiple forms of GABAergic inhibition that exist in the CNS and contribute to visual signal processing in the retina...
  98. pmc Effect of diuretics on fetal growth: A drug effect or confounding by indication? Pooled Danish and Scottish cohort data
    C Olesen
    The Danish Epidemiology Science Centre at the Department of Epidemiology and Social Medicine, University of Aarhus, DK 8000 Aarhus C, Denmark
    Br J Clin Pharmacol 51:153-7. 2001
    ..We analysed whether the purchase of prescription drugs for diuretics during pregnancy was associated with measures of fetal growth...
  99. ncbi Role of non-NMDA receptors in vasopressin and oxytocin release from rat hypothalamo-neurohypophysial explants
    D J Morsette
    Department of Physiology and Biophysics, Finch University of Health Sciences, The Chicago Medical School, North Chicago, Illinois 60064, USA
    Am J Physiol Regul Integr Comp Physiol 280:R313-22. 2001
    ..NMDA-stimulated VP but not OT release was prevented by blockade of non-NMDA-Rs, but AMPA-stimulated VP/OT release was not prevented by NMDA-R blockade...
  100. ncbi Hepatitis C NS5B polymerase inhibitors: functional equivalents for the benzothiadiazine moiety
    Douglas K Hutchinson
    Department of Antiviral Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
    Bioorg Med Chem Lett 21:1876-9. 2011
    ..Several of these compounds exhibited potent activity in enzymatic and replicon assays...
  101. ncbi Molecular cloning, primary structure, and characterization of two members of the mammalian electroneutral sodium-(potassium)-chloride cotransporter family expressed in kidney
    G Gamba
    Harvard Center for Study of Kidney Disease, Harvard Medical School, Boston, Massachusetts
    J Biol Chem 269:17713-22. 1994
    ..These proteins establish a new family of Na(+)-(K+)-Cl- cotransporters...

Research Grants25

  1. 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. ..
  2. Differential effects of TARPs on AMPA receptor subunits
    AMY ARAI; Fiscal Year: 2008
    ..unreadable] [unreadable]..
  3. Use-dependent intrinsic plasticity in the cerebellum
    David J Linden; Fiscal Year: 2010
    ..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. ..
  4. Neural Substrates /Socioemotional Disturbances /Develop.
    Ludise Malkova; Fiscal Year: 2003
    ..This information will provide a rationale basis for the design of therapeutic interventions directed at correcting the underlying biological dysfunctions that give rise to autism and related socioemotional disorders. ..
  5. Control of Synaptic Glutamate Release
    Steven Mennerick; Fiscal Year: 2004
    ..In addition, we expect our results to elucidate details of the mechanisms of action potential coupling to chemical neurotransmission and a possible mechanism of synaptic plasticity. ..
  6. SYNAPTIC ALTERATIONS AFTER HYPOGLYCEMIC SEIZURES
    Kelvin Yamada; Fiscal Year: 2008
    ..Understanding mechanisms of diabetes/diabetes complication-induced brain dysfunction may lead to new targets for treatment interventions to prevent or retard cognitive impairment in diabetes. ..
  7. 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. [unreadable] [unreadable] [unreadable]..
  8. Synaptic Pathways in the Mammalian Retina
    EDMUND TREXLER; Fiscal Year: 2008
    ..abstract_text> ..
  9. Advances in Renal Research: Human Diseases of Protein Processing
    David Ellison; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  10. 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. ..
  11. 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. ..
  12. Neural Substrates of Socioemotional Development
    Ludise Malkova; Fiscal Year: 2007
    ..unreadable] [unreadable]..
  13. 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. [unreadable] [unreadable]..
  14. Synaptic Transmission in the Mammalian Inner Retina
    JOSHUA SINGER; Fiscal Year: 2007
    ..abstract_text> ..
  15. 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. ..
  16. 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. ..
  17. 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. ..
  18. 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. ..
  19. 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. ..
  20. 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. ..
  21. 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. ..
  22. BENZANNULATION APPROACH TO BIARYL ETHERS
    Michael Harmata; Fiscal Year: 2001
    ..abstract_text> ..
  23. 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. [unreadable] [unreadable] [unreadable]..