Genomes and Genes
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.
Publications151 found, 100 shown here
- Downregulation of tonic GABA currents following epileptogenic stimulation of rat hippocampal culturesJin 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...
- Cyclothiazide induces robust epileptiform activity in rat hippocampal neurons both in vitro and in vivoJinshun 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...
- Comparative toxicity of bentazon and molinate on growth, photosynthetic pigments, photosynthesis, and respiration of the Portuguese ricefield cyanobacterium Nostoc muscorumVictor 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...
- BDNF-TrkB signaling pathway mediates the induction of epileptiform activity induced by a convulsant drug cyclothiazideYun 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...
- Photocatalytic degradation of bentazone in soil washing wastes containing alkylpolyoxyethylene surfactantsM 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...
- Epileptiform response of CA1 neurones to convulsant stimulation by cyclothiazide, kainic acid and pentylenetetrazol in anaesthetized ratsBinbin 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...
- Cyclothiazide induces seizure behavior in freely moving ratsShuzhen 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...
- Des-A-ring benzothiadiazines: inhibitors of HCV genotype 1 NS5B RNA-dependent RNA polymerasePamela 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...
- Determination of two phototransformation products of bentazone using quadrupole time-of-flight mass spectrometryManuela 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)...
- Induction and inactivation of a cytochrome P450 confering herbicide resistance in wheat seedlingsN 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...
- Map-based cloning of a novel rice cytochrome P450 gene CYP81A6 that confers resistance to two different classes of herbicidesGang 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...
- Second generation of hydroxyethylamine BACE-1 inhibitors: optimizing potency and oral bioavailabilityNicolas 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...
- BPDZ 154 activates adenosine 5'-triphosphate-sensitive potassium channels: in vitro studies using rodent insulin-secreting cells and islets isolated from patients with hyperinsulinismKaren 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...
- Cyclothiazide: a subunit-specific inhibitor of GABAC receptorsAn 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...
- Substituted benzothiadizine inhibitors of Hepatitis C virus polymeraseAntony 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...
- Characterization of the inhibition of hepatitis C virus RNA replication by nonnucleosidesLicia 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 ..
- 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....
- Influences of educational interventions and adverse news about calcium-channel blockers on first-line prescribing of antihypertensive drugs to elderly people in British ColumbiaM Maclure
PharmaCare, British Columbia Ministry of Health, Victoria, Canada
Lancet 352:943-8. 1998....
- The potential savings of using thiazides as the first choice antihypertensive drug: cost-minimisation analysisAtle 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...
- Choosing a first-line drug in the management of elevated blood pressure: what is the evidence? 1: Thiazide diureticsJ 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...
- 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 diureticsD 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...
- Treating high blood pressure in Africans with type 2 diabetesE O Okoro
Ethn Dis 14:160-1. 2004
- Risk of congestive heart failure in an elderly population treated with peripheral alpha-1 antagonistsChris L Bryson
VA Puget Sound Health Services Research and Development, VAMC, Seattle, Washington 98108, USA
J Am Geriatr Soc 52:1648-54. 2004....
- [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...
- [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...
- The return on INVESTMichael H Alderman
JAMA 290:2859-61. 2003
- [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
- Comparison of candesartan with lisinopril on ambulatory blood pressure and morning surge in patients with systemic hypertensionKazuo Eguchi
Department of Cardiology, Jichi Medical School, Tochigi, Japan
Am J Cardiol 92:621-4. 2003....
- [ALLHAT=other leading physicians have alternative interpretations]Alan Charles
Lakartidningen 100:2073-4. 2003
- Distinguishing between presynaptic and postsynaptic mechanisms of short-term depression during action potential trainsAdrian Y C Wong
Department of Cell Physiology and Pharmacology, University of Leicester, Leicester, LE1 9HN, United Kingdom
J Neurosci 23:4868-77. 2003....
- 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
- [Tax payers have payed billions for the "blood pressure maffia's" actions]Bengt Järhult
Lakartidningen 100:1917-8. 2003
- 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 drugsA Q Adigun
Department of Medicine, Division of Clinical Pharmacology, Indiana University School of Medicine, Indianapolis, USA
J Hum Hypertens 17:277-85. 2003....
- Properties of quantal transmission at CA1 synapsesSridhar 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....
- [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...
- [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
- Cyclothiazide prolongs low [Mg2+]-induced seizure-like eventsBálint 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...
- [Comrades! There must be some blood order in the field of hypertension!]Arne Melander
NEPI, Malmö och Stockholm
Lakartidningen 102:1068-70. 2005
- Quality of life and antihypertensive drug therapyJoel 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...
- C-terminal truncation affects kinetic properties of GluR1 receptorsErika 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...
- 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
- Diuretics for cardiovascular prevention in the elderlyO Hanon
Department of Geriatrics, Hopital Broca, rue Pascal, Paris, France
J Hum Hypertens 18:S15-22. 2004....
- Angiotensin-converting enzyme inhibitors and diuretics: optimal combination therapyMori J Krantz
Ann Intern Med 141:893; author reply 893. 2004
- [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....
- Antihypertensive therapy and incidence of type 2 diabetes in an elderly cohortRaj 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...
- Use of beta-blockers and risk of fracturesRaymond G Schlienger
Basel Pharmacoepidemiology Unit, Division of Clinical Pharmacology and Toxicology, University Hospital, Basel, Switzerland
JAMA 292:1326-32. 2004....
- Improving prescribing of antihypertensive and cholesterol-lowering drugs: a method for identifying and addressing barriers to changeAtle 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...
- Following evidence-based prescribing guidelines for antihypertensives could save big bucksGina Rollins
Rep Med Guidel Outcomes Res 15:1, 6-7. 2004
- [Thiazides or ACE inhibitors? A drug-economic analysis]Ivar Aursnes
Tidsskr Nor Laegeforen 124:1668. 2004
- [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...
- ALLHAT: a critical assessmentAke 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...
- Relative roles of different mechanisms of depression at the mouse endbulb of HeldHua 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...
- Long-term potentiation alters the modulator pharmacology of AMPA-type glutamate receptorsBin 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...
- [Consequences of ALLHAT: Thiazides rehabilitated--time to change prescription patterns]Anders Hernborg
Avdelningen för medicin, Universitetssjukhuset MAS, Malmo
Lakartidningen 100:408-10. 2003
- Fixed dose combination therapy in the treatment of hypertensionT Stanton
Department of Medicine and Therapeutics, University of Glasgow, Glasgow, Scotland, UK
J Hum Hypertens 16:75-8. 2002
- The thiazide-sensitive na-cl cotransporter and human disease: reemergence of an old playerDavid H Ellison
J Am Soc Nephrol 14:538-40. 2003
- [Policy of antihypertensive therapy in arterial hypertension in the elderly. II]M A Gurevich
Klin Med (Mosk) 80:9-13. 2002
- [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...
- Blocking AMPA receptor desensitization prolongs spontaneous EPSC decay times and depolarizes H1 horizontal cells in carp retinal slicesH 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...
- Hypertension: treatment--now & tomorrowChike M Nzerue
Ethn Dis 12:S2-43-5. 2002
- Activity-dependent change in AMPA receptor properties in cerebellar stellate cellsSiqiong 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...
- Effect of 14 years of antihypertensive treatment on renal function and urinary albumin excretion in primary hypertensionA 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...
- Prescribing patterns and therapeutic implications for diabetic hypertension in BahrainK 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...
- [Established blood pressure drug wins out in a comparative study. In hypertension, a diuretic first!]Ulrike Wepner
MMW Fortschr Med 145:10-2. 2003
- Correlation of AMPA receptor subunit composition with synaptic input in the mammalian cochlear nucleiS M Gardner
Department of Physiology, University of Wisconsin Medical School-Madison, Madison, Wisconsin 53706, USA
J Neurosci 21:7428-37. 2001....
- AMPA receptors on developing medial septum/diagonal band neurons are sensitive to early postnatal binge-like ethanol exposureShu 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...
- Hypertension, anti-hypertensive drug therapy and erectile dysfunction in diabetesP 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...
- Treatment of hypertension in type 2 diabetes mellitus: blood pressure goals, choice of agents, and setting priorities in diabetes careSandeep 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...
- The evidence base for tight blood pressure control in the management of type 2 diabetes mellitusVincenza Snow
American College of Physicians, 190 N Independence Mall West, Philadelphia, Pennsylvannia 19106, USA
Ann Intern Med 138:587-92. 2003
- Diuretics: from classical carbonic anhydrase inhibitors to novel applications of the sulfonamidesClaudiu 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. 2008The 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 ..
- ATP-sensitive potassium channel openers and 2,3-dimethyl-2-butylamine derivativesHai 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...
- Studies of benzothiadiazine derivatives as hepatitis C virus NS5B polymerase inhibitors using 3D-QSAR, molecular docking and molecular dynamicsX 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)...
- Novel 2,2-dioxide-4,4-disubstituted-1,3-H-2,1,3-benzothiadiazines as non-nucleoside reverse transcriptase inhibitorsJ 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...
- A continuous high frequency stimulation of the subthalamic nucleus determines a suppression of excitatory synaptic transmission in nigral dopaminergic neurons recorded in vitroAda Ledonne
Universita degli Studi di Roma Tor Vergata, Rome, Italy
Exp Neurol 233:292-302. 2012..The deficit of transmission between the STN and the SNpc could have a role in the therapeutic effects of the DBS procedure...
- [Synthesis, physicochemical and pharmacological properties of pentacyclic alkaloid-analogues]Máté Bubenyák
Semmelweis Egyetem Gyógyszerészi Kémiai Intézet 1092 Bp Hogyes Endre u 9
Acta Pharm Hung 81:139-49. 2011..attributes of the synthesized intermediaries were defined, such as the pKa constants of 2,3-poly-methylene-benzothiadiazines. Proton/deuteron exchange kinetic constants of active methylene-groups of five tricyclic compounds were ..
- Sodium disorders in the elderlyNaureen 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...
- Mechanisms underlying presynaptic facilitatory effect of cyclothiazide at the calyx of Held of juvenile ratsT 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...
- AMPA receptor desensitization as a determinant of vulnerability to focally evoked status epilepticusFrancesco Fornai
Department of Pharmacology, W215 Research Bldg, 3970 Reservoir Road NW, Georgetown University, Washington, DC 20057, USA
Eur J Neurosci 21:455-63. 2005....
- Paired-pulse depression at photoreceptor synapsesKatalin 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...
- Physicochemical evaluation of PVP-thiazide diuretic interactions in co-spray-dried composites--analysis of glass transition composition relationshipsLidia 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...
- 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 polymeraseRosanna 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...
- Laboratory degradation studies of bentazone, dichlorprop, MCPA, and propiconazole in Norwegian soilsC 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...
- Determination of bentazone, dichlorprop, and MCPA in different soils by sodium hydroxide extraction in combination with solid-phase preconcentrationC 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...
- Combination therapy in the management of hypertension: focus on angiotensin receptor blockers combined with diureticsPaolo 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...
- LY392098, a novel AMPA receptor potentiator: electrophysiological studies in prefrontal cortical neuronsP Baumbarger
Lilly Research Laboratories, Neuroscience Discovery, Eli Lilly and Company, Indianapolis, IN 46285-0510, USA
Neuropharmacology 40:992-1002. 2001..Spontaneous activity of PFC neurons was also increased. Collectively, these results demonstrate that LY392098 is a highly potent, selective and centrally active positive modulator of native AMPA receptors...
- Positive allosteric modulators of AMPA receptors reduce proton-induced receptor desensitization in rat hippocampal neuronsS 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...
- Simultaneous determination of enantiomerization and hydrolysis kinetic parameters of chiral N-alkylbenzothiadiazine derivativesMarina 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...
- Association of a mutation in thiazide-sensitive Na-Cl cotransporter with familial Gitelman's syndromeK Takeuchi
Second Department of Internal Medicine, Tohoku University School of Medicine, Sendai, Japan
J Clin Endocrinol Metab 81:4496-9. 1996....
- Role of non-NMDA receptors in osmotic and glutamate stimulation of vasopressin release: effect of rapid receptor desensitizationC 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...
- Satellite NG2 progenitor cells share common glutamatergic inputs with associated interneurons in the mouse dentate gyrusJean 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...
- In silico studies of urease inhibitors to explore ligand-enzyme interactionsFarzana 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...
- Effects of S 18986-1, a novel cognitive enhancer, on memory performances in an object recognition task in ratsC 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...
- 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....
- Chronic magnesium administration enhances oxidative glucose metabolism in thiazide treated hypertensive patientsG 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)..
- Efficacy and safety of cilazapril, a new angiotensin-converting enzyme inhibitorR 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...
- Regulation of SULT2B1a (pregnenolone sulfotransferase) expression in rat C6 glioma cells: relevance of AMPA receptor-mediated NO signalingAtsushi 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...
- Activity of a potent hepatitis C virus polymerase inhibitor in the chimpanzee modelChih 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...
- Targeting AMPA receptor gating processes with allosteric modulators and mutationsNicholas A Mitchell
Center for Neuropharmacology and Neuroscience, Albany Medical College, Albany, New York 12208, USA
Biophys J 92:2392-402. 2007....
- Cyclothiazide selectively inhibits mGluR1 receptors interacting with a common allosteric site for non-competitive antagonistsAlexander Surin
Department of Pharmacology, Georgetown University Medical Center, 3900 Reservoir Road NW, Washington, DC 20057, USA
Neuropharmacology 52:744-54. 2007....
- Studies of enantiomerization of chiral 3,4-dihydro-1,2,4-benzothiadiazine 1,1-dioxide type compoundsG Cannazza
Dipartimento di Scienze Farmaceutiche, Universita degli Studi di Modena e Reggio Emilia, Modena, Italy
Chirality 13:94-101. 2001....
- Angiotensin-converting enzyme inhibitors in the treatment of mild to moderate essential hypertensionA 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...
- Differential effects of TARPs on AMPA receptor subunitsAMY ARAI; Fiscal Year: 2007....
- DIFFERENCES IN SYNAPTIC VS NONSYNAPTIC AMPA RECEPTORSAMY ARAI; Fiscal Year: 2004..Determining which cellular factor stabilizes the low-affinity receptors will constitute the Fifth Aim of this application. ..
- Seizures & Amydala-Based Socioemotional DysfunctionLudise 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. ..
- Control of Synaptic Glutamate ReleaseSteven Mennerick; Fiscal Year: 2007....
- Synaptic Pathways in the Mammalian RetinaEDMUND TREXLER; Fiscal Year: 2007..abstract_text> ..
- Neural Substrates of Socioemotional DevelopmentLudise 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. ..
- Home Automatic external Defibrillator TrainingThomas 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. ..
- 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. ..
- Synaptic Transmission in the Mammalian Inner RetinaJOSHUA SINGER; Fiscal Year: 2007..abstract_text> ..
- Glutamate Receptor Desensitization and its ModulationKATHRYN PARTIN; Fiscal Year: 2005....
- Pseudopteroxazole and Related Antitubercular AgentsMichael 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. ..
- EFFECTS OF ACID ON BONEDavid 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. ..
- Axonal Signaling in the HippocampusSteven 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. ..
- Synaptic transmission in the rod pathway of the mammalian retinaJoshua 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. ..
- Contribution of increased VDR and CaR to Hypercalciuria in the GHS RatDavid A Bushinsky; Fiscal Year: 2010..These studies will advance research on hypercalciuria and may ultimately lead to improved care of patients with kidney stones. ..
- Glutamate Receptor Desensitization and its ModulationKATHRYN 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. ..
- Use-dependent intrinsic plasticity in the cerebellumDavid 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. ..
- EFFECTS OF ACID ON BONEDavid 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. ..
- CRCNS: Biophysical properties of parallel neural circuits serving night visionJoshua 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. ..
- Hypoglycemia in the Developing Diabetic BrainKelvin 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. ..
- EFFECTS OF ACID ON BONEDavid 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. ..
- CLINICAL PHARMACOLOGY OF LOOP DIURETICSD 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. ..
- CLINICAL PHARMACOLOGY OF LOOP DIURETICSD 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. ..
- Regulation of thiazide-sensitive NaCl transportDavid 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. ..
- BENZANNULATION APPROACH TO BIARYL ETHERSMichael Harmata; Fiscal Year: 2001..abstract_text> ..
- Glial-cytokine-neuronal interactions in neuropathic painHan Rong Weng; Fiscal Year: 2010..1 ..
- Human genetic variation and ventricular fibrillation resuscitation outcomesThomas 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. ..
- Synaptic transmission in the rod pathway of the mammalian retinaJOSHUA 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. ..
- Cost-effectiveness of genetic screening for colon cancerSandeep 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. ..
- REGULATION OF THIAZIDE SENSITIVE NACL TRANSPORTDavid 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. ..
- NEURONAL INFORMATION STORAGE IN CEREBELLAR DEEP NUCLEIDavid Linden; Fiscal Year: 2004..In addition, they have potential clinical relevance for both cerebellar motor disorders and disorders of learning and memory generally. ..
- LONG TERM POTENTIATION AND DEPRESSION IN THE CEREBELLUMDavid 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. ..
- EFFECTS OF ACID ON BONEDavid 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. ..
- CELLULAR SUBSTRATES OF CEREBELLAR INFORMATION STORAGEDavid Linden; Fiscal Year: 2007..In addition, they have potential clinical relevance for both cerebellar motor disorders and disorders of learning and memory generally...
- Regulation of thiazide-sensitive NaCl transportDavid 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. ..
- Reducing Adverse Self-Medication Behaviors in Older Adults with HypertensionPatricia Neafsey; Fiscal Year: 2007..Healthcare utilization will be compared between the 2 groups after 52 weeks and a cost-benefit analysis conducted. ..