PAF receptor and "Cache-oreilles" effect. Simple PAF antagonists.

J Lamotte-Brasseur; F Heymans; G Dive; A Lamouri; J P Batt; C Redeuilh; D Hosford; P Braquet; J J Godfroid

doi:10.1007/bf02536524

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PAF receptor and "Cache-oreilles" effect. Simple PAF antagonists.

J Lamotte-Brasseur·F Heymans·G Dive·A Lamouri·J P Batt·C Redeuilh·D Hosford·P Braquet·J J Godfroid

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Abstract

Nine simple and structurally flexible PAF antagonists were synthesized and their inhibitory effects on PAF induced platelet aggregation were measured. Compounds with PAF antagonistic activity exhibited a negative electrostatic potential generated by two trimethoxyphenyl groups (isocontour at -10 Kcal/mole) at various distances between the negative clouds. The optimal distance between the atoms generating the "cache-oreilles" system for exhibiting potent PAF antagonistic activity is estimated to be 11-13 A. In the flexible molecules studied, the dispersion of the electronic distribution is not necessarily favorable for anti-PAF activity. The data support the simple bipolarized model for the PAF receptor that has been proposed by the authors.

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Animals Calorimetry Drug Design Electrochemistry Indicators and Reagents Magnetic Resonance Spectroscopy Molecular Conformation Molecular Structure Platelet Activating Factor Platelet Aggregation Platelet Membrane Glycoproteins Rabbits Receptors, Cell Surface Receptors, G-Protein-Coupled Comparative Study Journal Article

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J Lamotte-Brasseur, F Heymans, G Dive, A Lamouri, J P Batt, C Redeuilh, D Hosford, P Braquet, J J Godfroid. 1991. PAF receptor and "Cache-oreilles" effect. Simple PAF antagonists.. https://doi.org/10.1007/bf02536524

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