BIIL 284 is a new LTB(4) receptor antagonist. It is a prodrug and has negligible binding to the LTB(4) receptor. However, ubiquitous esterases metabolize BIIL 284 to the active metabolites BIIL 260… (More)
1. The novel cation channel blocker, LOE 908, was tested for its effects on Ca2+ entry and membrane currents activated by depletion of intracellular Ca2+ stores in human endothelial cells. 2. LOE 908… (More)
(1) PAF-acetylhydrolases form a major pathway for the degradation of platelet-activating factor (PAF). Here we investigate the role of the kidney and the liver in the control of PAF-acetylhydrolase… (More)
Two new antagonists of platelet-activating factor (PAF), the pyrrolothiazole derivative 52770 RP and the triazolodiazepine WEB 2086, have been studied as radioligands in intact human platelets.… (More)
In 5 cases of invasive ductal and lobular carcinoma of the breast multiple epithelioid and giant cell containing granulomas were detected, localized mainly in circumferential regions, but also in the… (More)
We recently reported the development of a receptor-modeling concept based on 5D-QSAR (quantitative structure-activity relationships) and which explicitly allows for the simulation of induced fit. In… (More)
Chemotactic factors bound to receptors of the seven-transmembrane domain family signal leukocytes through associated guanine nucleotide-binding (G) proteins. Human leukocytes of the HL-60 line, which… (More)
Platelet-activating factor (PAF) is a unique phospholipid mediator with multifunctional properties. Evidence generated in experimental studies suggests that PAF plays a pathogenetic role in… (More)
Hetrazepines such as WEB-2086 or WEB-2170 are potent, specific, competitive PAF antagonists binding at the same site as the PAF molecule. Despite their structural similarity to known hypnotic drugs… (More)
A novel class of CCR3 modulators is described. Starting with lead compound 4a (K(i): 110 nM), which turned out to be an antagonist of eotaxin at the CCR3 receptor, further optimization led to… (More)