(R,R)-MK 287 (L-680574) is a tetrahydrofuran derivative that potently inhibits the binding of [3H]C18- PAF to human platelets, polymorphonuclear leukocytes (PMNs), and lung membranes with Ki values of 6.1, 3.2, and 5.49 nM, respectively. (R,R)-MK 287 potently and selectively inhibits PAF-induced platelet aggregation (ED 50 =56 nM) and elastase release from PMNs (ED 50 =4.4 nM). (R,R)-MK 287 inhibits PAF-induced lethality in mice (ED 50 =0.8 mg/kg, po) and PAF-induced bronchospasm in guinea pigs (ED 50 =0.18 mg/kg).
Products | Products > Disease Areas > Blood or Cardio-cerebrovascular Disease | Products > Signaling Pathways > GPCR/G Protein | Products > Research Areas > Cardiovascular Disease | Products > Signaling Pathways > Platelet-activating Factor Receptor (PAFR)
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