[The modification of the biosynthesis and effect of thromboxane A2 and prostacyclin by trapidil (Rocornal)]. 1983

H U Block, and I Heinroth, and C Giessler, and K Pönicke, and P Mentz, and U Zehl, and W Rettkowski, and A Dunemann, and W Förster

The influence of the antianginal drug trapidil on the biosynthesis of thromboxane A2 (TXA2) and/or prostacyclin (PGI2), metabolites of arachidonic acid (AA), was investigated in rabbit and human platelet rich plasma (PRP), in homogenates of rabbit spleen and of rat lung and in aortic preparations of rats and rabbits, respectively. Trapidil showed a marked inhibition of the AA-induced aggregation and TXA2 biosynthesis in rabbit and human PRP. The TXA2 inhibition by trapidil was not demonstrable in damaged platelets and seems to require intact cells. In homogenates of rat lungs, trapidil remained without effect on the TXA2 and PGI2 synthesis. In rabbit spleen homogenates the drug induced an inhibition of the formation of both AA metabolites. In contrast to Japanese authors we could not observe any increase in PGI2 release in rat aortic preparation. The PGI2 release from isolated perfused guinea pigs hearts was enhanced; on the other hand, the PGI2 efflux from rabbit hearts remained unchanged. The antiaggregatory effect of PGI2 on the ADP-induced aggregation was strengthened by trapidil, showing an overadditive effect in rabbit PRP. The aggregation inducing effect of the prostaglandin endoperoxide analog U-46619 was inhibited by trapidil. A possible clinical significance of the inhibitions of the synthesis and effect of TXA2 for therapy of ischemic heart disease is discussed.

UI MeSH Term Description Entries
D008168 Lung Either of the pair of organs occupying the cavity of the thorax that effect the aeration of the blood. Lungs
D008297 Male Males
D009206 Myocardium The muscle tissue of the HEART. It is composed of striated, involuntary muscle cells (MYOCYTES, CARDIAC) connected to form the contractile pump to generate blood flow. Muscle, Cardiac,Muscle, Heart,Cardiac Muscle,Myocardia,Cardiac Muscles,Heart Muscle,Heart Muscles,Muscles, Cardiac,Muscles, Heart
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
D011450 Prostaglandin Endoperoxides, Synthetic Synthetic compounds that are analogs of the naturally occurring prostaglandin endoperoxides and that mimic their pharmacologic and physiologic activities. They are usually more stable than the naturally occurring compounds. Prostaglandin Endoperoxide Analogs,Prostaglandin Endoperoxide Analogues,Synthetic Prostaglandin Endoperoxides,Analogues, Prostaglandin Endoperoxide,Endoperoxide Analogues, Prostaglandin,Endoperoxides, Synthetic Prostaglandin
D011453 Prostaglandins A group of compounds derived from unsaturated 20-carbon fatty acids, primarily arachidonic acid, via the cyclooxygenase pathway. They are extremely potent mediators of a diverse group of physiological processes. Prostaglandin,Prostanoid,Prostanoids
D011464 Epoprostenol A prostaglandin that is a powerful vasodilator and inhibits platelet aggregation. It is biosynthesized enzymatically from PROSTAGLANDIN ENDOPEROXIDES in human vascular tissue. The sodium salt has been also used to treat primary pulmonary hypertension (HYPERTENSION, PULMONARY). Prostacyclin,Prostaglandin I2,Epoprostanol,Epoprostenol Sodium,Epoprostenol Sodium Salt, (5Z,9alpha,11alpha,13E,15S)-Isomer,Flolan,Prostaglandin I(2),Veletri
D011743 Pyrimidines A family of 6-membered heterocyclic compounds occurring in nature in a wide variety of forms. They include several nucleic acid constituents (CYTOSINE; THYMINE; and URACIL) and form the basic structure of the barbiturates.
D011817 Rabbits A burrowing plant-eating mammal with hind limbs that are longer than its fore limbs. It belongs to the family Leporidae of the order Lagomorpha, and in contrast to hares, possesses 22 instead of 24 pairs of chromosomes. Belgian Hare,New Zealand Rabbit,New Zealand Rabbits,New Zealand White Rabbit,Rabbit,Rabbit, Domestic,Chinchilla Rabbits,NZW Rabbits,New Zealand White Rabbits,Oryctolagus cuniculus,Chinchilla Rabbit,Domestic Rabbit,Domestic Rabbits,Hare, Belgian,NZW Rabbit,Rabbit, Chinchilla,Rabbit, NZW,Rabbit, New Zealand,Rabbits, Chinchilla,Rabbits, Domestic,Rabbits, NZW,Rabbits, New Zealand,Zealand Rabbit, New,Zealand Rabbits, New,cuniculus, Oryctolagus
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

Related Publications

H U Block, and I Heinroth, and C Giessler, and K Pönicke, and P Mentz, and U Zehl, and W Rettkowski, and A Dunemann, and W Förster
January 1989, The Journal of biological chemistry,
H U Block, and I Heinroth, and C Giessler, and K Pönicke, and P Mentz, and U Zehl, and W Rettkowski, and A Dunemann, and W Förster
June 1988, Proceedings of the National Academy of Sciences of the United States of America,
H U Block, and I Heinroth, and C Giessler, and K Pönicke, and P Mentz, and U Zehl, and W Rettkowski, and A Dunemann, and W Förster
January 1974, Die Pharmazie,
H U Block, and I Heinroth, and C Giessler, and K Pönicke, and P Mentz, and U Zehl, and W Rettkowski, and A Dunemann, and W Förster
January 1976, Die Pharmazie,
H U Block, and I Heinroth, and C Giessler, and K Pönicke, and P Mentz, and U Zehl, and W Rettkowski, and A Dunemann, and W Förster
January 1976, Die Pharmazie,
H U Block, and I Heinroth, and C Giessler, and K Pönicke, and P Mentz, and U Zehl, and W Rettkowski, and A Dunemann, and W Förster
January 1978, Die Pharmazie,
H U Block, and I Heinroth, and C Giessler, and K Pönicke, and P Mentz, and U Zehl, and W Rettkowski, and A Dunemann, and W Förster
March 1981, Prostaglandins and medicine,
H U Block, and I Heinroth, and C Giessler, and K Pönicke, and P Mentz, and U Zehl, and W Rettkowski, and A Dunemann, and W Förster
August 1976, Die Pharmazie,
H U Block, and I Heinroth, and C Giessler, and K Pönicke, and P Mentz, and U Zehl, and W Rettkowski, and A Dunemann, and W Förster
December 1975, Die Pharmazie,
H U Block, and I Heinroth, and C Giessler, and K Pönicke, and P Mentz, and U Zehl, and W Rettkowski, and A Dunemann, and W Förster
January 1990, Advances in prostaglandin, thromboxane, and leukotriene research,
Copied contents to your clipboard!