Reference : Ly 186655, a Phosphodiesterase Inhibitor, Inhibits Histamine Release from Human Basop...
Scientific journals : Article
Human health sciences : Cardiovascular & respiratory systems
Ly 186655, a Phosphodiesterase Inhibitor, Inhibits Histamine Release from Human Basophils, Lung and Skin Fragments
Louis, Renaud mailto [Université de Liège - ULiège > Département des sciences cliniques > Pneumologie - Allergologie]
Bury, Thierry [Université de Liège - ULiège > Département des sciences de la motricité > Physiologie humaine et physiologie de l'effort physique]
Corhay, Jean-Louis mailto [Université de Liège - ULiège > > Pneumologie-Allergologie >]
Radermecker, Maurice [Université de Liège - ULiège > Services généraux (Faculté de médecine) > Relations académiques et scientifiques (Médecine) >]
International Journal of Immunopharmacology
Yes (verified by ORBi)
[en] LY 186655 (Tibenelast, Lilly) is a new phosphodiesterase inhibitor, not derived from the xanthine, possessing bronchodilating activity in animals. The aim of this work was to study the effect of LY 186655 and theophylline on histamine release from human leukocytes, skin and lung fragments. Histamine was measured using a spectrofluorometric method. Both drugs (3 x 10(-5)-3 x 10(-3) M) exhibited a dose-dependent inhibition on anti-IgE (1/2000)-induced histamine release from human leukocytes. At 3 x 10(-3) M, theophylline was significantly more effective than LY 186655 (mean inhibition 94 and 42%, respectively). On lung fragments, theophylline and LY 186655 (3 x 10(-5)-3 x 10(-3) M) caused strong and comparable inhibitory effects on anti-IgE (1/500)-induced histamine release with a mean inhibition reaching maximally 65%. Histamine release induced by compound 48/80 (1 mg/ml) on sliced human foreskin was reduced with both drugs (3 x 10(-3) M) by about 37%. We conclude that LY 186655 inhibits in vitro immunological histamine release from human lung and cutaneous mast cells as well as basophils with a similar pattern of activity to theophylline.

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