Pharmacologic profile of BN 50739, a new PAF antagonist and
1990; Elsevier BV; Volume: 39; Issue: 5 Linguagem: Inglês
10.1016/0090-6980(90)90031-p
ISSN1878-416X
AutoresT-L. Yue, Reuven Rabinovici, Michel Y. Farhat, G Feuerstein,
Tópico(s)Nitric Oxide and Endothelin Effects
ResumoThe effect of a new PAF antagonist BN 50739 was studied on PAF-induced [3H]-serotonin ralease from washed rabbit platelets in vitro and on PAF-induced hypotension in vivo. BN 50739 competitively inhibited PAF-induced [3H]-serotonin release from the platelets in a dose-dependent manner. In the presence of 4, 10 and 50 nM of BN 50739, the concentration of PAF inducing 50% maximal [3H]-serotonin release from the platelets (EC50) increased from 2.15 nM to 5.10, 45.10 and 900 nM, respectively. The IC50 of BN 50739 for PAF (10 nM) induced [3H]-serotonin release was 3.67 nM. Under the same experimental condition, the IC50S of BN 50726, BN 50730, BN 50741, WEB 2086, SRI 63–441 and BN 52021 were 5.40, 4.61, 6.88, 5.98, 40.90 nM and 14.90 μM, respectively. PAF-induced hypotension in conscious rats was also inhibited dose-dependently by i.p. pretreatment of BN 50739 (3 and 10 mg/kg). PAF-induced hypotension was diminished both in magnitude and duration in rats pretreated with BN 50739. These data taken together indicate that BN 50739 is a most potent PAF antagonist in vitro and in vivo.
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