H O Heuer's research while affiliated with Boehringer Ingelheim and other places
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Publications (4)
The selective hetrazepinoic platelet-activating factor (PAF) antagonist WEB 2170 (Bepafant) was used to study the pathophysiological role of PAF in several models of anaphylaxis in mice and guinea pigs. In actively sensitized mice, the PAF antagonist WEB 2170 (1.0-10 mg/kg p.o.) protected mice from anaphylactic death in a dose-dependent manner when...
The development of selective PAF receptor antagonists may provide a novel approach to the treatment of human bronchial asthma. In preclinical animal models of human asthma, PAF receptor antagonists have been found to be efficacious in blocking antigen-induced changes in lung function. However, the majority of these models involve acute inflammatory...
We have examined the effects of a PAF receptor antagonist, WEB 2170, on several indices of acute and chronic airway inflammation and associated changes in lung function in a primate model of allergic asthma. A single oral administration WEB 2170 provided dose related inhibition of the release of leukotriene C(4) (LTC(4)) and prostaglandin D(2) (PGD...
Citations
... Consequently, preliminary structureactivity relationships have been established that are summarized in a review article, a patent, and a book chapter contribution [28][29][30]. Notably, the antiplatelet activity of certain metal-based PAF-induced inhibitors was comparable or even higher than that of known organic small molecules (WEB 2170, BN 52021, CV-3988, etc.) with potencies in the submicromolar range [29][30][31][32]. In the meantime, this topic has collected interest from other research groups [33][34][35]. ...
... However, day-2 through day-5 plasma samples contained significant amounts of PMN priming activity compared with buffer-treated controls or day-1 samples (P Ͻ .05). Moreover, 64% Ϯ 8% of this priming activity could be inhibited by pretreatment of the PMNs with WEB 2170, a lipid receptor antagonist, [35][36][37] and 67% Ϯ 14% of the plasma priming activity was chloroform extractable, defining it as a lipid, a result identical to previous reports. 15,16 Since previous data documented that PMN priming activity accumulates in the plasma during routine storage of platelets, we quantified the amount of PMN priming activity in the implicated WB-PLT units and compared this activity with activity in the control group of platelets that were not implicated in transfusion reactions, as described above (Figure 1). ...
