VU University Medical Center, Departments of Pathology1, Physiology2, Cardiac Surgery3, Cardiology4, Amsterdam, the Netherlands. ICaR-VU5, Amsterdam, the Netherlands. Netherlands Forensic Institute6 (NFI), The Hague, the Netherlands. Sanquin Research, Department of Immunopathology7, Amsterdam, The Netherlands. Academic Medical Center, Department of Hematology8 Amsterdam, The Netherlands Maastri...

Two morphine prodrugs ('PDA' and 'PDB') were synthesized and the kinetics of esterase-mediated morphine release from these prodrugs were determined when incubated with plasma from different animal species. Morphine was rapidly released from PDA by all species plasma with the maximum reached within 5-10min; the released morphine was biologically active as determined by an in vitro cAMP assay. Th...

Recently, multiple C1 inhibitor (C1-INH) replacement products have been approved for the treatment of hereditary angioedema (HAE). This review summarizes HAE and its current treatment modalities and focuses on findings from bench to bedside trials of a new C1-INH replacement, conestat alfa. Conestat alfa is unique among the other C1-INH replacement products because it is produced from transgeni...

OBJECTIVES To evaluate the use of Cinryze (nanofiltered C1-esterase inhibitor [C1 INH-nf]) for the acute management and prevention of hereditary angioedema attacks in the subgroup of children and adolescents who participated in 2 placebo-controlled and 2 open-label extension studies. STUDY DESIGN In the acute-attack treatment studies, the efficacy of 1000 U of C1 INH-nf (with an additional 10...

Petrosamine (1)—a colored pyridoacridine alkaloid from the Belizean sponge, Petrosia sp., that is also a potent inhibitor of acetylcholine esterase (AChE)—was investigated by spectroscopic and computational methods. Analysis petrosamine-free energy landscapes, pKa tautomerism, revealed an accurate electronic depiction molecular structure 1 as di-keto form, with net charge q = +1, rather than di...

In septic shock, hypotension, disseminated intravascular coagulation, and neutrophil activation are related to the activation of the blood coagulation contact system. This study evaluates in dogs the effect of the C1-esterase inhibitor (C1-INH), a main inhibitor of the blood coagulation contact system, on the cardiovascular and respiratory dysfunction associated with endotoxic shock. Two groups...

Sir: We have demonstrated that aminopeptidases, phosphatases and esterases are located not only in cells but also on the cellular membrane of various kinds of animal cells1-3) and that inhibitors of these enzymes modified immune responses4,5). Among these inhibitors, bestatin, amastatin and forphenicine enhanced immune responses, but esterastin which inhibited esterase suppressed immune respons...

The importance of laboratory testing in the diagnosis of hereditary angioedema (HAE) has increased with the advent of new treatment options in recent years. It has been 50 years since HAE was linked to a decrease of C1INH (the inhibitor of complement enzyme, C1 esterase), a link that provided for the first laboratory test available for this disorder. HAE is subdivided into types that can be di...

somal dominant disorder that results in episodes of acute edema in various organs, including the gastrointestinal tract, skin and larynx. It is estimated to affect about 1 in 50 000–100 000 people. The symptoms, including abdominal pain, laryngeal edema and subcutaneous edema, usually begin in childhood and persist throughout life with unpredictable severity. Hereditary angioedema is classified...

Two novel mechanisms of organophosphate resistance were isolated and characterized from a population of Culex pipiens L. from Cyprus. Two strains, one expressing the novel, highly active esterases A5 and B5 (strain A5B5-R), and one expressing insensitive acetylcholinesterase (strain Ace-R), were developed by single pair crosses and selection with temephos and propoxur, respectively. The A5B5-R ...