Synthesis and pharmacology of a novel class of long-lasting PAF receptor antagonists.
Several new charged PAF receptor antagonists were prepared, where the phosphate moiety has been replaced by a methylsulfonylcarbamoylpyridinium moiety, and evaluated for duration of inhibitory activity against PAF-induced bronchoconstriction and hemoconcentration in the guinea pig. One of these compounds (1d; SDZ 64-619) has shown potency and duration of inhibition in the range of CV-6209 (1c).
Houlihan
W J
WJ
Sandoz Research Institute, East Hanover, NJ 07936.
Cheon
S H
SH
Handley
D A
DA
Larson
D A
DA
D000328:Adult; D000818:Animals; D016085:Bronchoconstrictor Agents / Q000494:pharmacology; D006168:Guinea Pigs; D006400:Hematocrit; D006801:Humans; D015394:Molecular Structure; D010972:Platelet Activating Factor; D010975:Platelet Aggregation Inhibitors / Q000494:pharmacology; D010980:Platelet Membrane Glycoproteins; D011956:Receptors, Cell Surface / Q000037:antagonists & inhibitors* / Q000378:metabolism; D043562:Receptors, G-Protein-Coupled
D016085:Bronchoconstrictor Agents; D010972:Platelet Activating Factor; D010975:Platelet Aggregation Inhibitors; D010980:Platelet Membrane Glycoproteins; D011956:Receptors, Cell Surface; D043562:Receptors, G-Protein-Coupled; C039351:platelet activating factor receptor