Effects of TRK-100, a stable prostacyclin analogue, on regulation of cyclic AMP metabolism in platelets.

作者: K. Nogimori , N. Kajikawa , S. Nishio , M. Yajima

DOI: 10.1016/0090-6980(89)90057-9

关键词: EndocrinologyRadioimmunoassayTrk receptorAdenylate kinaseInternal medicineIntracellularBiologyProstacyclinMetabolismCyclase activityPlatelet

摘要: Abstract TRK-100 is a chemically stable analogue of prostacyclin and effective in inhibiting platelet aggregation when orally administered experimental animals. In the present study we compared potency with those PGI 2 PGE 1 to cause an activation adenylate cyclase activity rat human membranes. was half as , 10 times more than both also induced phosphodiesterase directly added intact platelets probably feedback mechanism intracellular cAMP level like did. would mimic regulation metabolism.

参考文章(21)
C H Macphee, D H Reifsnyder, T A Moore, K M Lerea, J A Beavo, Phosphorylation results in activation of a cAMP phosphodiesterase in human platelets. Journal of Biological Chemistry. ,vol. 263, pp. 10353- 10358 ,(1988) , 10.1016/S0021-9258(19)81523-5
Jasmine J. Fazzari, John R. Jacobs, Robert Alvarez, Adair Taylor, Regulation of cyclic AMP metabolism in human platelets. Sequential activation of adenylate cyclase and cyclic AMP phosphodiesterase by prostaglandins. Molecular Pharmacology. ,vol. 20, pp. 302- 309 ,(1981)
M.J. Cho, M.A. Allen, Chemical stability of prostacyclin (PGI2) in aqueous solutions. Prostaglandins. ,vol. 15, pp. 943- 954 ,(1978) , 10.1016/0090-6980(78)90037-0
K. Schr�r, H. Darius, R. Matzky, R. Ohlendorf, The antiplatelet and cardiovascular actions of a new carbacyclin derivative (ZK 36 374)--equipotent to PGI2 in vitro. Naunyn-schmiedebergs Archives of Pharmacology. ,vol. 316, pp. 252- 255 ,(1981) , 10.1007/BF00505658
Alfred G. Gilman, G proteins and dual control of adenylate cyclase Cell. ,vol. 36, pp. 577- 579 ,(1984) , 10.1016/0092-8674(84)90336-2
M. Lombroso, S. Nicosia, R. Paoletti, B.J.R. Whittle, S. Moncada, J.R. Vane, The use of stable prostaglandins to investigate prostacyclin (PGI2)-binding sites and PGI2-sensitive adenylate cyclase in human platelet membranes Prostaglandins. ,vol. 27, pp. 321- 333 ,(1984) , 10.1016/0090-6980(84)90083-2
S. Stürzebecher, M. Haberey, B. Müller, E. Schillinger, G. Schröder, W. Skuballa, G. Stock, H. Vorbrüggen, W. Witt, Pharmacological profile of a novel carbacyclin derivative with high metabolic stability and oral activity in the rat Prostaglandins. ,vol. 31, pp. 95- 109 ,(1986) , 10.1016/0090-6980(86)90228-5