| Autor: |
Ponpipom MM; Merck Sharp & Dohme Research Laboratories, Rahway, NJ 07065., Hwang SB, Doebber TW, Acton JJ, Alberts AW, Biftu T, Brooker DR, Bugianesi RL, Chabala JC, Gamble NL, et. al. |
| Jazyk: |
angličtina |
| Zdroj: |
Biochemical and biophysical research communications [Biochem Biophys Res Commun] 1988 Feb 15; Vol. 150 (3), pp. 1213-20. |
| DOI: |
10.1016/0006-291x(88)90758-9 |
| Abstrakt: |
The title compound, L-659,989, is a highly potent, competitive, and selective antagonist of the binding of [3H]PAF to its receptors in platelet membranes from rabbits and humans. It exhibits equilibrium inhibition constants for PAF binding of 1.1 nM (rabbit) to 9.0 nM (human), values that are at least 1-2 orders of magnitude lower than those of other PAF antagonists tested. L-659,989 potently inhibits PAF-induced aggregation of rabbit platelets and degranulation of rat (ED50 4.5 nM) and human (ED50 10 nM) neutrophils. L-659,989 inhibits PAF-induced extravasation and lysosomal enzyme release in rats, and is active orally in female rats (ED50 0.2 mg/kg) with an extraordinary oral duration of action of 12 to 16 hours at 1.0 mg/kg p.o. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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