Inhibition of PAF-induced histamine secretion and bronchoconstriction by WEB 2086.
Platelet activating factor (PAF) stimulates histamine secretion from rabbit mixed leukocytes in a concentration-dependent fashion (EC50 10 ng/ml). The PAF (10 ng/ml)-induced histamine secretion was inhibited by WEB 2086 (IC50 = 20 nM). Furthermore, PAF (10 ng/kg, i.v.)-induced bronchoconstriction in guinea pig was also inhibited by WEB 2086 (ID50 = 5.3 micrograms/kg, i.v., 5 minutes). These data showed the existence of PAF-receptors on rabbit basophils and in guinea pig airways which are highly sensitive to blockade by WEB 2086.
Chand
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Department of Pharmacology, Wallace Laboratories, Division of Carter-Wallace, Inc., Cranbury, New Jersey 08512.
Pillar
J
J
Nolan
K
K
Diamantis
W
W
Sofia
R D
RD
D000818:Animals; D001381:Azepines / Q000494:pharmacology*; D001980:Bronchi / Q000187:drug effects; D004205:Cromolyn Sodium / Q000494:pharmacology; D006168:Guinea Pigs; D006636:Histamine Release / Q000187:drug effects*; D066298:In Vitro Techniques; D007962:Leukocytes / Q000187:drug effects; D008297:Male; D009130:Muscle, Smooth / Q000187:drug effects*; D010972:Platelet Activating Factor / Q000037:antagonists & inhibitors*; D011817:Rabbits; D014227:Triazines / Q000494:pharmacology*; D014230:Triazoles
D001381:Azepines; D010972:Platelet Activating Factor; D014227:Triazines; D014230:Triazoles; C052518:WEB 2086; D004205:Cromolyn Sodium