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PAF-receptor. 1. 'Cache-oreilles' effect of selected high-potency platelet-activating factor (PAF) antagonists.
J Lipid Mediat. 1989 Jul-Aug; 1(4):201-15.JL

Abstract

Three-dimensional electrostatic maps were calculated for six potent antagonists of platelet-activating factor (PAF), the antagonists being selected for their apparent structural heterogeneity. The molecules examined were the compact Ginkgolides BN 52020, BN 52021 and BN 52022 (1, 2 and 3), the semi-rigid kadsurenone (4), a flexible synthetic dinor type C furanoid lignan L-652,731 (5a) and the triazolothienobenzodiazepine WEB 2086 (7). Calculation of the electrostatic potential generated around all the above molecules showed the existence of two wells of negative potential or 'cache-oreilles' (ear-muffs), i.e., the isocontours drawn at -10 kcal/mol, located at 180 degrees from each other and separated by a maximum distance of 22-27 A. Except for the synthetic dinor type C furanoid lignan (5a), the molecules also presented a moderate hydrophobic fragment, which constitutes a third point of interaction with the high-affinity binding site in rabbit and human platelets. The findings of the present study allow speculation that this high-affinity acceptor site may be a 'polarized cylinder' with a diameter of 10-12 A.

Authors+Show Affiliations

Laboratoire de Microbiologie, Institut de Chimie, Liège, Belgium.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

2562434

Citation

Dive, G, et al. "PAF-receptor. 1. 'Cache-oreilles' Effect of Selected High-potency Platelet-activating Factor (PAF) Antagonists." Journal of Lipid Mediators, vol. 1, no. 4, 1989, pp. 201-15.
Dive G, Godfroid JJ, Lamotte-Brasseur J, et al. PAF-receptor. 1. 'Cache-oreilles' effect of selected high-potency platelet-activating factor (PAF) antagonists. J Lipid Mediat. 1989;1(4):201-15.
Dive, G., Godfroid, J. J., Lamotte-Brasseur, J., Batt, J. P., Heymans, F., Dupont, L., & Braquet, P. (1989). PAF-receptor. 1. 'Cache-oreilles' effect of selected high-potency platelet-activating factor (PAF) antagonists. Journal of Lipid Mediators, 1(4), 201-15.
Dive G, et al. PAF-receptor. 1. 'Cache-oreilles' Effect of Selected High-potency Platelet-activating Factor (PAF) Antagonists. J Lipid Mediat. 1989 Jul-Aug;1(4):201-15. PubMed PMID: 2562434.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - PAF-receptor. 1. 'Cache-oreilles' effect of selected high-potency platelet-activating factor (PAF) antagonists. AU - Dive,G, AU - Godfroid,J J, AU - Lamotte-Brasseur,J, AU - Batt,J P, AU - Heymans,F, AU - Dupont,L, AU - Braquet,P, PY - 1989/7/1/pubmed PY - 1989/7/1/medline PY - 1989/7/1/entrez SP - 201 EP - 15 JF - Journal of lipid mediators JO - J Lipid Mediat VL - 1 IS - 4 N2 - Three-dimensional electrostatic maps were calculated for six potent antagonists of platelet-activating factor (PAF), the antagonists being selected for their apparent structural heterogeneity. The molecules examined were the compact Ginkgolides BN 52020, BN 52021 and BN 52022 (1, 2 and 3), the semi-rigid kadsurenone (4), a flexible synthetic dinor type C furanoid lignan L-652,731 (5a) and the triazolothienobenzodiazepine WEB 2086 (7). Calculation of the electrostatic potential generated around all the above molecules showed the existence of two wells of negative potential or 'cache-oreilles' (ear-muffs), i.e., the isocontours drawn at -10 kcal/mol, located at 180 degrees from each other and separated by a maximum distance of 22-27 A. Except for the synthetic dinor type C furanoid lignan (5a), the molecules also presented a moderate hydrophobic fragment, which constitutes a third point of interaction with the high-affinity binding site in rabbit and human platelets. The findings of the present study allow speculation that this high-affinity acceptor site may be a 'polarized cylinder' with a diameter of 10-12 A. SN - 0921-8319 UR - https://www.unboundmedicine.com/medline/citation/2562434/PAF_receptor__1__'Cache_oreilles'_effect_of_selected_high_potency_platelet_activating_factor__PAF__antagonists_ DB - PRIME DP - Unbound Medicine ER -