Effect of op 1206, a prostaglandin E1 derivative, on guinea-pig platelet functions
1980; Elsevier BV; Volume: 20; Issue: 5-6 Linguagem: Inglês
10.1016/0049-3848(80)90145-0
ISSN1879-2472
AutoresToshimichi Tsuboi, Buichi Fujitani, J. Maeda, Kōji Yoshida, M Shimizu, A Kawasaki, T Okegawa, M Tsuboshima,
Tópico(s)Analytical Methods in Pharmaceuticals
ResumoOP 1206, 17(S)-methyl-ω-homo-trans-Δ2-prostaglandin E1, inhibited guinea-pig platelet aggregation induced by ADP, collagen, A 23187, arachidonic acid, labile aggregation stimulating substances (LASS) and thromboxane A2 (TXA2)-like substance, and platelet adhesiveness to a glass bead column. The potency of inhibition was 10–16 times stronger than that of prostaglandin E1 (PGE1). ADP-induced platelet aggregation was notably disaggregated by the addition of OP 1206 after induction of aggregation. The release of ATP and ADP from guinea-pig platelets induced by collagen was suppressed by OP 1206, of which potency was 9–10 times stronger than that of PGE1. OP 1206 and PGE1 increased guinea-pig platelet cyclic AMP levels, and the increased levels were augmented by the pretreatment with theophylline. OP 1206 and PGE1 inhibited synthesis of guinea-pig platelet malondialdehyde (MDA) induced by thrombin but not by arachidonic acid. This inhibition was released by exogenous calcium. OP 1206 and PGE1 showed no influence on synthesis of radioactive TXA2 (measured as a stable form, TXB2) from [14C] arachidonic acid. From these results, increased levels of platelet cyclic AMP by OP 1206 as well as PGE1 may exert their action on platelet functions.
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