Search results for " vivo"
showing 10 items of 1661 documents
Synthesis and Characterization of a Novel Series of Agonist Compounds as Potential Radiopharmaceuticals for Imaging Dopamine D-2/3 Receptors in Their…
2014
Imaging of dopamine D2/3 receptors (D2/3R) can shed light on the nature of several neuropsychiatric disorders in which dysregulation of D2/3R signaling is involved. Agonist D2/3 tracers for PET/SPECT imaging are considered to be superior to antagonists because they are more sensitive to dopamine concentrations and may selectively label the high-affinity receptor state. Carbon-11-labeled D2/3R agonists have been developed, but these short-lived tracers can be used only in centers with a cyclotron. Here, we report the development of a series of novel D2R agonist compounds based on the 2-aminomethylchromane (AMC) scaffold that provides ample opportunities for the introduction of longer-lived […
Pretreatment with gonadotropin-releasing hormone (GnRH) antagonists to prevent the flare-up effect of long-acting GnRH agonists: results of a pilot s…
2007
This study evaluated in vivo whether the flare-up effect of GnRH agonists can be suppressed through pretreatment with a GnRH antagonist. The classic flare-up effect caused by 3.8 mg goserelin acetate could not be suppressed through pretreatment using a single dosage of 3.24 mg cetrorelix acetate.
Die nächste Generation „atypischer” Antipsychotika: Der Beitrag der Positronenemissionstomographie
2003
Almost fifteen years of research with Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT) have led to a profound understanding of the relationships between antipsychotic doses and plasma levels on the one hand and occupancy of (striatal) D 2 -like dopamine receptors on the other hand as well as with the associated clinical effects and side effects. Furthermore, with the development of clinically atypical" antipsychotics PET studies helped to generate hypotheses regarding the essential pharmacological properties of this heterogeneous class of drugs. Possible mechanisms of action include combined D 2 -/5-HT 2 antagonism, preferential mesolimbic binding, a…
Synthesis, characterization of diorganotin(IV) complexes of N-(2-hydroxyarylidene)aminoacetic acid and antitumour screening in vivo in ehrlich ascite…
2001
Some new diorganotin(IV) complexes have been prepared by reacting potassium N-(2-hydroxyarylidene)aminoacetate with R2SnCl2(R = Me,nBu,Ph). The complexes have been characterized by 1H,13C,119Sn NMR, IR and 119mSn Mössbauer spectroscopic techniques in combination with elemental analysis. In the solid state, the complexes possess penta- and hexa-coordinated tin centres. The hexa-coordinated tin complexes were found to dissociate in solution, giving rise to penta-coordinated species as revealed by 119Sn NMR spectroscopy. Antitumour screening in vivo of the complexes L4snPh2,L4SnPh2· Ph3SnCl and L4SntBU2·t Bu2SnCl2 (L4 = N-(2-hydroxyacetophenone)aminoacetate) is also reported. Copyright © 2001 …
Immunogenicity of Semisynthetic Penicillins
1969
Allergic reactions following drug therapy with penicillin are a well known, unpleasant, rather frequent and occasionally dangerous phenomenon. The immunological processes leading to sensitization against Penicillin G (PG) and the factors operative in the elicitation of hypersensitivity reactions against the drug have mainly been elucidated by the extensive work of Eisen, Parker [25–27], DeWeck [41–45] and B. Levine [16–23]. Antibodies with penicilloyl specificity have been demonstrated in the serum of animals experimentally immunized with PG and more important in the majority of human beings suffering from allergy against penicillin. In vivo allergic reactions could be elicited with penicil…
Erythrocytes labeled with [18F]SFB as an alternative to radioactive CO for quantification of blood volume with PET
2013
Inhaled radioactive CO is currently the tracer of choice for blood volume quantification by positron emission tomography (PET). This measurement is of great interest for several clinical and research applications. However, owing to the short half-life of the radiolabeled CO, it can only be used in centers equipped with a cyclotron. In the present work, we propose an alternative method to label the red blood cells with [(18) F] in order to obtain blood volume measurements by PET. The use of the radioactive synthon [(18) F] N-succinimidyl 4-[(18) F]fluorobenzoate ([(18) F]SFB) was evaluated for erythrocyte labeling and PET blood volume imaging. The images provided by [(18) F]SFB labeled eryth…
Aminobisphosphonate-activated γδ T cells in immunotherapy of cancer: doubts no more
2008
BACKGROUND: Activated V gamma 9 V delta 2 T cells are able to kill most tumour cells because of recognition by T cell receptor and natural killer receptors. OBJECTIVE: We discuss the possibility that the intentional activation of gammadelta T cells in vivo by aminobisphosphonates may represent a promising target for the design of novel and highly innovative immunotherapy in cancer patients. METHODS: The antitumoral effects of gammadelta T cells both in vitro and in vivo have been demonstrated suggesting a new therapeutic approach for translation into the clinical setting. RESULTS/CONCLUSION: V gamma 9 V delta 2 T lymphocytes represent a particularly interesting target for immunotherapeutic …
Semi-physiologic model validation and bioequivalence trials simulation to select the best analyte for acetylsalicylic acid
2015
Abstract The objective of this paper is to apply a previously developed semi-physiologic pharmacokinetic model implemented in NONMEM to simulate bioequivalence trials (BE) of acetyl salicylic acid (ASA) in order to validate the model performance against ASA human experimental data. ASA is a drug with first-pass hepatic and intestinal metabolism following Michaelis–Menten kinetics that leads to the formation of two main metabolites in two generations (first and second generation metabolites). The first aim was to adapt the semi-physiological model for ASA in NOMMEN using ASA pharmacokinetic parameters from literature, showing its sequential metabolism. The second aim was to validate this mod…
Noninvasive sampling of phenylalanine by reverse iontophoresis.
1999
While iontophoresis is typically associated with drug delivery across the skin, the symmetry of the technique permits its application to the essentially noninvasive withdrawal of biologically important analytes from the subcutaneous space to the body's surface. The identification of other substances which can be monitored by this procedure, and to its optimization and development as a more general clinical chemistry tool, is a long-term objective. In this paper, we describe a preliminary in vitro investigation into the feasibility of extracting and analyzing the amino acid, phenylalanine, with the ultimate aim to develop a diagnostic test for phenylketonuria, a potentially fatal metabolic d…
Rapid vascularization of starchâ poly(caprolactone) in vivo by outgrowth endothelial cells in co-culture with primary osteoblasts
2011
The successful integration of in vitro-generated tissues is dependent on adequate vascularization in vivo. Human outgrowth endothelial cells (OECs) isolated from the mononuclear cell fraction of peripheral blood represent a potent population of circulating endothelial progenitors that could provide a cell source for rapid anastomosis and scaffold vascularization. Our previous work with these cells in co-culture with primary human osteoblasts has demonstrated their potential to form perfused vascular structures within a starch–poly(caprolactone) biomaterial in vivo. In the present study, we demonstrate the ability of OECs to form perfused vascular structures as early as 48 h following subcut…