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PAF-agonistic and -antagonistic behaviour of new synthetic ether phospholipids. I. Studies on blood platelets in vitro.
J Lipid Mediat. 1990 Jan-Feb; 2(1):21-31.JL

Abstract

Structural analogues of platelet-activating factor (PAF, 1-O-alkyl-2-O-acetyl-sn-glycero-3-phosphocholine) in which the acetyl group and the polar head have been replaced by ethyl and a pyridine ring, respectively, were tested for biological activities on blood platelets in vitro. In comparison with PAF most of the analogues exerted weak pro-aggregatory effects and both structural modifications were found to contribute to the lowering of platelet-stimulating activity. 1-O-Hexadecyl-2-O-ethyl-rac-glycero-3-phosphoric acid 4-(N,N-dimethylamino)-pyridinium ethylester (DMAP-ethyl-PAF) did not activate platelets but inhibited PAF-induced platelet responses. The inhibition was concentration-dependent and of competitive type. KB values for inhibiting the PAF-induced aggregation of human and rabbit platelets in plasma were 3.2 and 0.55 mumol/l, respectively. There is also evidence that the PAF-antagonistic behaviour of DMAP-ethyl-PAF is attributable to an inhibition of the binding of PAF to its putative receptor.

Authors+Show Affiliations

Institute of Pathological Biochemistry, Medical Academy of Erfurt, G.D.R.No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article

Language

eng

PubMed ID

1966804

Citation

Ostermann, G, et al. "PAF-agonistic and -antagonistic Behaviour of New Synthetic Ether Phospholipids. I. Studies On Blood Platelets in Vitro." Journal of Lipid Mediators, vol. 2, no. 1, 1990, pp. 21-31.
Ostermann G, Hofmann B, Kertscher HP, et al. PAF-agonistic and -antagonistic behaviour of new synthetic ether phospholipids. I. Studies on blood platelets in vitro. J Lipid Mediat. 1990;2(1):21-31.
Ostermann, G., Hofmann, B., Kertscher, H. P., & Till, U. (1990). PAF-agonistic and -antagonistic behaviour of new synthetic ether phospholipids. I. Studies on blood platelets in vitro. Journal of Lipid Mediators, 2(1), 21-31.
Ostermann G, et al. PAF-agonistic and -antagonistic Behaviour of New Synthetic Ether Phospholipids. I. Studies On Blood Platelets in Vitro. J Lipid Mediat. 1990 Jan-Feb;2(1):21-31. PubMed PMID: 1966804.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - PAF-agonistic and -antagonistic behaviour of new synthetic ether phospholipids. I. Studies on blood platelets in vitro. AU - Ostermann,G, AU - Hofmann,B, AU - Kertscher,H P, AU - Till,U, PY - 1990/1/1/pubmed PY - 1990/1/1/medline PY - 1990/1/1/entrez SP - 21 EP - 31 JF - Journal of lipid mediators JO - J Lipid Mediat VL - 2 IS - 1 N2 - Structural analogues of platelet-activating factor (PAF, 1-O-alkyl-2-O-acetyl-sn-glycero-3-phosphocholine) in which the acetyl group and the polar head have been replaced by ethyl and a pyridine ring, respectively, were tested for biological activities on blood platelets in vitro. In comparison with PAF most of the analogues exerted weak pro-aggregatory effects and both structural modifications were found to contribute to the lowering of platelet-stimulating activity. 1-O-Hexadecyl-2-O-ethyl-rac-glycero-3-phosphoric acid 4-(N,N-dimethylamino)-pyridinium ethylester (DMAP-ethyl-PAF) did not activate platelets but inhibited PAF-induced platelet responses. The inhibition was concentration-dependent and of competitive type. KB values for inhibiting the PAF-induced aggregation of human and rabbit platelets in plasma were 3.2 and 0.55 mumol/l, respectively. There is also evidence that the PAF-antagonistic behaviour of DMAP-ethyl-PAF is attributable to an inhibition of the binding of PAF to its putative receptor. SN - 0921-8319 UR - https://www.unboundmedicine.com/medline/citation/1966804/PAF_agonistic_and__antagonistic_behaviour_of_new_synthetic_ether_phospholipids__I__Studies_on_blood_platelets_in_vitro_ L2 - https://antibodies.cancer.gov/detail/CPTC-AKT1-3 DB - PRIME DP - Unbound Medicine ER -