Proaggregatory and inhibitory effects of 2-O-ethyl analogues of platelet-activating factor (PAF) on human and rabbit platelets.

Abstract:

:A series of 8 analogues of platelet-activating factor (PAF) in which both the acetyl group and the polar head are changed, were tested for biological activities on human and rabbit platelets in plasma. Two of these compounds, 1-O-hexadecyl-2-O-ethyl-rac-glycero-3-phosphoric acid-5'-trimethylammoniumpentyl ester and 1-O-hexadecyl-2-O-ethyl-rac-glycero-3-phosphoric acid-6'-trimethylammoniumhexyl ester inhibit selectively the PAF-induced aggregation response without showing any agonistic activity. Schild analysis revealed a competitive antagonism and KB values of 4.4 and 10.5 mumol/l, respectively. These results point to a crucial role of the distance between the phosphoryl group and the polar head for expression of PAF-antagonistic properties. Moreover, the substituent at the 2-position was found to influence predominantly the agonistic behaviour.

journal_name

Thromb Res

journal_title

Thrombosis research

authors

Hofmann B,Ostermann G,Kertscher HP,Till U

doi

10.1016/0049-3848(88)90244-7

subject

Has Abstract

pub_date

1988-02-15 00:00:00

pages

415-23

issue

4

eissn

0049-3848

issn

1879-2472

journal_volume

49

pub_type

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