Pyridazines 79. Novel oxazolo[3',2':1,2]pyrrolo[3,4-d]pyridazines and imidazolo[1'2':1,2]pyrrolo[3,4-d]pyridazines: synthesis and biological evaluation.
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Antiviral Agents↗
Biomedical subjects
H Stoiber
Publications and source records attributed to H Stoiber.
Inhibition of HIV-1 infection in vitro by monoclonal antibodies to the complement receptor type 3 (CR3): an accessory role for CR3 during virus entry?
Adhesion molecules are known to contribute to infectivity of HIV-1. Here we tested whether the complement receptor type 3 (CR3, CD11b), an alpha(m)beta2 integrin, plays an accessory role in the infection process of HIV-1, because ICAM-1, a ligand of CR3, is present on the envelope of HIV-1. In addition, the viral transmembrane protein gp41 shares four regions of homology with the complement component C3, a further CR3 ligand. Infection of PBMCs with HIV-IIIB and primary isolates was partially inhibited by anti-CR3 antibodies. A peptide derived from the complement component C3, covering the CR3-binding site of C3 and sharing strong similarity to the immunosuppressive region of gp41, significantly reduced the HIV-1 titer in infection assays. Recombinant soluble gp41 (rsgp41) and the peptide covering the immunosuppressive domain of gp41 inhibited the rosetting of iC3b-coated sheep erythrocytes with U937 via complement receptors (CRs) with an efficiency comparable to monoclonal anti-CR antibodies. In addition, sub-populations of CD4 + and CD8 + T-cells isolated from HIV-infected individuals were found to upregulate CR3 as determined by FACS analysis and on the mRNA level. Since gp41 has been implicated in viral fusion, an interaction of its C3-homology region in gp41 or an interaction of ICAM on the surface of free virus with CRs might contribute to facilitate viral entry.
Anti-HIV Agents↗
Drug monitoring and viral response to lopinavir/ritonavir or saquinavir/ritonavir containing regimens in individuals infected with the human immunodeficiency virus type 1.
The aim of this study was to correlate results of therapeutic drug monitoring, genotypic resistance and viral response to lopinavir/ritonavir (LPV/r) or saquinavir/ritonavir (SQV/r) containing antiretroviral regimens. The retrospective short-term study included 20 patients with LPV/r and 20 patients with SQV/r containing highly active antiretroviral therapy (HAART). At baseline 7 LPV/r patients and 10 SQV/r patients had CD4+T cell counts above 410 cells/microl. After 6 months CD4+T cells had doubled in 5 LPV/r and 2 SQV/r patients. In LPV/r patients the mean serum concentration of lopinavir (LPV) was 2.6 ppm and 67% of all LPV/r samples had 50 or fewer viral copies/ml. In SQV/r patients the mean serum concentration of saquinavir (SQV) was 2.1 ppm. 79% of all SQV/r samples had 50 or fewer viruses/ml. Pharmacoenhanced regimens efficiently suppress human immunodeficiency virus type 1 (HIV-1) and the risk of developing resistance mutations is therefore reduced. The implementation of drug monitoring is an additional tool to determine optimal treatment conditions.
Adult↗
[Hemodynamic and gasometric modifications during the anesthesia recovery period in patients undergoing ventilation after surgery of the abdominal aorta].
This study was carried out on 12 patients (mean age 61) in order to assess the oxygen consumption (VO2) in the post-operative stage of an elective surgical procedure (replacement of the abdominal aorta). Anesthesia was a combination of thiopentone, pancuronium bromide and high doses of droperidol and fentanyl. Patients were kept intubated and ventilated in the post-operative period. VO2 and other related metabolic parameters as well as hemodynamic parameters were measured every 45 minutes over a period of 5 hours. A VO2 increase (127%) related to the increase in body temperature was noted. Mean VO2 for all patients during the whole period was 170 +/- 13 ml.min-1.m-2 (range: 51-411 ml.min-1.m-2). Mean value of maximal VO2 was 240 +/- 21 ml.min-1.m-2 (range: 1471-411 ml.min-1.m-2). Large dose of droperidol are shown to limit VO2 increase. In patients with shivering, the maximal value of VO2 was found during shivering. The amount of droperidol administered during anesthesia was greater in patients without shivering. VO2 increase was due to a rise in tissular O2 extraction. Cardiac index was insufficiently increased (+ 9.4%) and a certain extent of myocardial inadaptability was suspected in relation with: high blood pressure, hypovolaemia and/or myocardial effect of anesthesia agents.
Anesthesia Recovery Period↗