These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: PAF-agonistic and -antagonistic behaviour of new synthetic ether phospholipids. II. Relationships between chemical structure and inhibition of PAF-induced human platelet activation.
    Author: Ostermann G, Hofmann B, Kertscher HP, Till U.
    Journal: J Lipid Mediat; 1991; 3(2):225-37. PubMed ID: 1797154.
    Abstract:
    A series of 30 newly synthesised racemic ether phospholipids was evaluated for PAF-antagonistic action on human blood platelets in vitro. The chemical structure of these compounds was derived from the 1-O-hexadecyl-2-O-ethyl-glycero-3-phosphoric acid 4-(N,N-dimethylamino)pyridinium ethylester which was recently characterised as a PAF-specific antagonist. Anti-PAF effects were demonstrated by means of an aggregation and a binding assay. The inhibition was concentration-dependent and of competitive type. KB-values for inhibiting platelet aggregation in plasma were greater than or equal to 0.3 mumol/l. The most effective antagonists were 3-10 times more effective in comparison with the ginkgolide BN 52021. Structure-activity relationship studies showed the 4-dimethylaminopyridine moiety in the 3 position to be the ultimate structural requirement for expressing PAF-antagonistic activity. Moreover, a short-chain substituent in the 2 position and a distinct distance between the phosphate group and the onium center were found to be essential for high PAF-antagonistic activity.
    [Abstract] [Full Text] [Related] [New Search]