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Phase-solubility techniques were used to assess the effect of pH on itraconazole complexation with 2-hydroxypropyl-beta-cyclodextrin (HPbetaCD). In addition, molecular modeling using beta-cyclodextrin as a surrogate for HPbetaCD was completed. Data suggested A(p)-type solubility relationships, indicating higher order complexation at higher HPbetaCD(More)
The effects of a series of analogues of the antiallergic drug astemizole on the exocytosis of the enzyme beta-hexosaminidase were studied in a mast cell model, the rat basophilic leukemia (RBL-2H3) cell. Besides differences in the effects on Fc epsilonRI receptor-stimulated exocytosis, changes were also observed in Ca2+ influx and in the perturbation of the(More)
Drug Utilization Research and Pharmacoepidemiology Meeting U t r e c h t ( T h e N e t h e r l a n d s ) , 19 M a y 1995 Organized by the Section of Drug Utilization and Pharmacoepidemiology of the Dutch Society of Pharmaceutical Sciences (Sectie Geneesmiddelengebruiksonderzoek en Farmacoepidemiologie van de Nederlandse Vereniging voor Farmaceutische(More)
For 6 large series of compounds derived from the piperidine moieties of spiperone, pimozide, haloperidol, pethidine, fentanyl and 4-methocarboxy-fentanyl, IC50 values were determined in the opiate and neuroleptic binding assay using [3H]-fentanyl and [3H]-haloperidol as ligands, respectively. The specificity and difference between both receptors were(More)
The use of the Electronegativity Equalization Method (EEM) is presented for high performance calculation of molecular electrostatic descriptors, giving quite similar results to those obtained through Density Functional Theory (B3LYP/6-31G*) calculations. Molecular descriptors include atomic charges and different related descriptors as well as Fukui(More)
Today, more than 40 protein amino acid (AA) sequences of membrane receptors coupled to guanine nucleotide binding proteins (G-proteins) are available. For those working in the field of medicinal chemistry, these sequences present a new type of information that should be taken into consideration. To make maximal use of sequence data it is essential to be(More)
Rabbit polyclonal antisera were raised against the pYV-encoded outer membrane protein P1 of five Yersinia enterocolitica strains belonging to serogroups O:3, O:5,27, O:8, and O:9. Analysis of these strains with the sera showed that P1 presented at least six different antigenic factors. Two of the serum specimens were chosen to test the P1 agglutinability of(More)