Effect of etofylline clofibrate on experimental thrombosis and platelet function. 1980

A K Sim, and M E Davies, and A P McCraw, and G Metz

1-(Theophyllin-7yl)-ethyl-2-[2-(p-chlorophenoxy)-2-methylpropionate] (etofylline clofibrate, ML 1024, Duolip) was shown to be a potent inhibitor of experimental thrombus formation in the microvasculature of the hamster cheek pouch and of platelet aggregation and adhesiveness in the cynomolgus monkey. Inhibitory effect on thrombus formation was superior to that obtained with either of the molecule components (clofibric acid and etofylline) or their 1 : 1 mixture and a synergistic effect was apparent. Etofylline clofibrate was more active than a commercial antithrombotic drug combination of acetylsalicylic acid (ASA) and dipyridamole as an inhibitor of thrombus formation in this test system (p less than 0.05) at the proposed therapeutic dose level for each drug. In the cynomolgus monkey, etofylline clofibrate was shown again to be a potent inhibitor of platelet aggregation induced by ADP and collagen and of platelet adesiveness after administration of 12 mg/kg/day for 21 days. A mixture of clofibrate and etofylline (21.25 mg/kg/day and 3.75 mg/kg/day, respectively) had relatively less effect on platelet aggregation and no consistent effect on platelet adhesiveness. The activity found in both test systems indicates a promising antithrombotic potential for etofylline clofibrate and warrants further investigation in humans.

UI MeSH Term Description Entries
D008252 Macaca fascicularis A species of the genus MACACA which typically lives near the coast in tidal creeks and mangrove swamps primarily on the islands of the Malay peninsula. Burmese Long-Tailed Macaque,Crab-Eating Monkey,Cynomolgus Monkey,M. f. aurea,M. fascicularis,Macaca fascicularis aurea,Monkey, Crab-Eating,Monkey, Cynomolgus,Crab-Eating Macaque,Burmese Long Tailed Macaque,Crab Eating Macaque,Crab Eating Monkey,Crab-Eating Macaques,Crab-Eating Monkeys,Cynomolgus Monkeys,Long-Tailed Macaque, Burmese,Macaque, Burmese Long-Tailed,Macaque, Crab-Eating,Monkey, Crab Eating
D008297 Male Males
D010973 Platelet Adhesiveness The process whereby PLATELETS adhere to something other than platelets, e.g., COLLAGEN; BASEMENT MEMBRANE; MICROFIBRILS; or other "foreign" surfaces. Adhesiveness, Platelet,Adhesivenesses, Platelet,Platelet Adhesivenesses
D010974 Platelet Aggregation The attachment of PLATELETS to one another. This clumping together can be induced by a number of agents (e.g., THROMBIN; COLLAGEN) and is part of the mechanism leading to the formation of a THROMBUS. Aggregation, Platelet
D001792 Blood Platelets Non-nucleated disk-shaped cells formed in the megakaryocyte and found in the blood of all mammals. They are mainly involved in blood coagulation. Platelets,Thrombocytes,Blood Platelet,Platelet,Platelet, Blood,Platelets, Blood,Thrombocyte
D002994 Clofibrate A fibric acid derivative used in the treatment of HYPERLIPOPROTEINEMIA TYPE III and severe HYPERTRIGLYCERIDEMIA. (From Martindale, The Extra Pharmacopoeia, 30th ed, p986) Athromidin,Atromid,Atromid S,Clofibric Acid, Ethyl Ester,Ethyl Chlorophenoxyisobutyrate,Miscleron,Miskleron,Chlorophenoxyisobutyrate, Ethyl
D005260 Female Females
D006224 Cricetinae A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS. Cricetus,Hamsters,Hamster
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D000960 Hypolipidemic Agents Substances that lower the levels of certain LIPIDS in the BLOOD. They are used to treat HYPERLIPIDEMIAS. Antihyperlipidemic,Antilipemic,Antilipemic Agents,Antilipemic Drug,Hypolipidemic Agent,Hypolipidemic Drug,Antihyperlipemics,Antihyperlipidemics,Antilipemic Drugs,Antilipemics,Hypolipidemic Drugs,Agent, Hypolipidemic,Agents, Antilipemic,Agents, Hypolipidemic,Drug, Antilipemic,Drug, Hypolipidemic,Drugs, Antilipemic,Drugs, Hypolipidemic

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