Search results for "drug discovery"

Residual vein thrombosis and D-dimer for optimizing duration of anticoagulation in idiopathic deep vein thrombosis.

2010

Long-term anticoagulant treatment is highly effective in preventing recurrent Venous Thrombo-Embolism (VTE) in patients with idiopathic Deep Vein Thrombosis (DVT) of the lower limbs, though associated with an increased risk for major bleeding that may offset the benefits of anticoagulation. Accordingly to recent guidelines, patients with idiopathic DVT should be treated for at least 3 months and then should be evaluated for the risk-benefit ratio of long-term therapy. However, such ‘time for decision’ is often unclear and the optimal duration of VKA remains debatable. In recent studies, markers for the assessment of the individual risk for recurrent thrombosis have been proposed, which can …

Managing Bleeding Complications in Patients Treated with the Old and the New Anticoagulants

2010

An increasing number of patients receive anticoagulant therapy to prevent and treat arterial or venous thromboembolism. The major complication of anticoagulant therapy is the increase of the individual bleeding risk. All anticoagulant drugs can cause haemorrhages, that can sometimes be life-threatening. Although heparins and the vitamin K antagonists have been the most widely used anticoagulants for decades, the correct management of bleeding complications associated with these agents has been poorly studied. More recently, new anticoagulant drugs, both parenteral and oral, have been approved for clinical use. Currently, none of these new agents has a specific antidote, and little advise ca…

Characterisation of [11C]PR04.MZ in Papio anubis baboon: A selective high-affinity radioligand for quantitative imaging of the dopamine transporter

2012

N-(4-fluorobut-2-yn-1-yl)-2β-carbomethoxy-3β-(4′-tolyl)nortropane (PR04.MZ, 1) is a PET radioligand for the non-invasive exploration of the function of the cerebral dopamine transporter (DAT). A reliable automated process for routine production of the carbon-11 labelled analogue [11C]PR04.MZ ([11C]-1) has been developed using GMP compliant equipment. An adult female Papio anubis baboon was studied using a test–retest protocol with [11C]-1 in order to assess test–retest reliability, metabolism and CNS distribution profile of the tracer in non-human primates. Blood sampling was performed throughout the studies for determination of the free fraction in plasma (fP), plasma input functions and m…

Darstellung und Reaktionen von 2-Methylen-canrenon

1995

Ausgehend vom Mannich-Salz 1 des Aldosteronantagonisten Canrenon oder von 2-Methylen-canrenon (2) wurden die am A-Ring anellierten Hetero- und Carbocyclen 5, 6, 8–13 dargestellt. Mit den Verbindungen 2, 3, 4b, 5, 6b, 8 und 12 wurden Bindungsstudien am Estradiol-, Progesteron-, Androgen-, Glucocorticoid- und Mineralocorticoid-Rezeptor sowie an den Serumproteinen Sexualhormonbindendes Globulin (SHBG) und Corticosteroidbindendes Globulin (CBG) durchgefuhrt. Die relativen Bindungsaffinitaten lagen bei CBG unter 1%, in allen anderen Fallen niedriger als 0.01%. Synthesis and Reactions of 2-Methylene-canrenone Starting from the Mannich salt 1 of the aldosterone antagonist canrenone or from 2-methy…

Effects of repeated treatments with an extract ofGinkgo biloba (EGb 761) and bilobalide on liver and muscle glycogen contents in the non-insulin-depe…

1997

The effects of repeated (15-day) oral treatments with an extract of Ginkgo biloba (EGb 761; 50 mg/kg/day) or with its terpenoid constituent, bilobalide (2 mg/kg/day), were assessed in normal rats and in rats that had been previously injected with streptozotocin (50 mg/kg, i.p. in saline solution), a dose which provided a model of non-insulin-dependent diabetes mellitus (NIDDM). In this model of diabetes, blood glucose is significantly increased while the circulating insulin level remains unchanged. Glucose penetrates cells because of decreased glycogen turnover, a metabolic abnormality that can be revealed by using an oral glucose tolerance test (OGTT). In control rats, hyperglycemia was ac…

Effects of repeated treatments with an extract ofGinkgo biloba (EGb 761) and bilobalide on glucose uptake and glycogen synthesis in rat erythrocytes:…

1994

The metabolic action of an extract of Ginkgo biloba (EGb 761) has been examined in an ex vivo study of rat erythrocytes. Oral administration of EGb 761 (100 mg/kg/day) for 5 days to Wistar rats caused an increase in the in vitro uptake of glucose by erythrocytes, especially in high-glucose (13.32 mM) medium, an effect that was associated with an increase in intracellular energy metabolism and reflected as a significant reduction in free glucose concentration. In contrast, the lactate concentration of the erythrocytes and lactate release to the bathing medium were not modified. Conversion of glucose into glycogen was significantly increased in the erythrocytes of EGb 761-treated animals. Tak…

Porphyria cutanea tarda und Farbenblindheit

1966

Die Untersuchung von 15 Kranken mit Porphyria cutanea tarda auf das Vorliegen von Farbsinnstorungen ergab eine uberzufallige Korrelation von Porphyria cutanea tarda und angeborener Deuteranomalie.

The follow-up of dietary treatment of obesity

2008

Antiketogene Wirkung von Xylit bei alloxandiabetischen Ratten

1963

Bei alloxandiabetischen Ratten mit Ketonurie zeigt Xylit je nach Versuchsbedingungen in 50–80% der Falle eine statistisch gesicherte antiketogene Wirkung.

Die rechnergestützte Diabeteseinstellung

1985

Blood glucose self-monitoring is essential to stabilize diabetes on a normoglycemic level. But often patients do not find the correct insulin adaptation. Therefore, we developed a computerized system which adapts insulin doses using a control matrix. During a first in-patient period we had a remarkable blood glucose normalization and stabilization.