NONSPECIFIC ANTAGONISM AGAINST THROMBOXANE A2 OF 7-ETHOXYCARBONYL-6,8-DIMETHYL-4-HYDROXYMETHYL-1(2H)-PHTHALAZINONE (EG-626) IN CONTRACTION OF ISOLATED SMOOTH MUSCLES

被引:5
作者
HARADA, Y
TANAKA, K
KATORI, M
机构
[1] Department of Pharmacology, School of Medicine Kitasato University, Sagamihara, Kanagawa
来源
PROSTAGLANDINS | 1979年 / 17卷 / 06期
关键词
D O I
10.1016/0090-6980(79)90066-2
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
7-Ethoxycarbonyl-6,8-dimethyl-4-hydroxymethyl-1(2H)-phthalazinone (EG-626) was reported as an antagonist of thromboxane (Tx) A2 in the contraction of rabbit aorta. It was, however, observed that EG-626 did inhibit the contraction of superfused rabbit aorta, but also did inhibit that of rabbit coeliac artery, rat stomach strip and rat colon induced by TxA2, PG endoperoxides, angiotensin II and PGF2α in non-specific manner. EG-626 had no effect on the biosynthesis of PG endoperoxides as well as TxA2. These results indicate that EG-626 is not a TxA2 antagonist, but has a general inhibitory effect on the smooth muscles. This inhibitory effect of EG-626 may be explained by the inhibition of phosphodiesterase. © 1979.
引用
收藏
页码:957 / 966
页数:10
相关论文
共 12 条
[1]   PHOSPHODIESTERASE INHIBITORS - THEIR COMPARATIVE EFFECTIVENESS INVITRO IN VARIOUS ORGANS [J].
ADACHI, K ;
NUMANO, F .
JAPANESE JOURNAL OF PHARMACOLOGY, 1977, 27 (01) :97-103
[2]   PROSTAGLANDINS, OXYGEN-TENSION AND SMOOTH MUSCLE TONE [J].
ECKENFEL.A ;
VANE, JR .
BRITISH JOURNAL OF PHARMACOLOGY, 1972, 45 (03) :451-&
[3]   PROSTAGLANDINS RELEASED BY SPLEEN [J].
GILMORE, N ;
VANE, JR ;
WYLLIE, JH .
NATURE, 1968, 218 (5147) :1135-&
[4]   THROMBOXANES - NEW GROUP OF BIOLOGICALLY-ACTIVE COMPOUNDS DERIVED FROM PROSTAGLANDIN ENDOPEROXIDES [J].
HAMBERG, M ;
SVENSSON, J ;
SAMUELSSON, B .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1975, 72 (08) :2994-2998
[5]  
MIYAMOTO T, 1976, J BIOL CHEM, V251, P2629
[6]   IMIDAZOLE - SELECTIVE INHIBITOR OF THROMBOXANE SYNTHETASE [J].
MONCADA, S ;
BUNTING, S ;
MULLANE, K ;
THOROGOOD, P ;
VANE, JR ;
RAZ, A ;
NEEDLEMAN, P .
PROSTAGLANDINS, 1977, 13 (04) :611-618
[7]   PROSTAGLANDIN ENDOPEROXIDE AND THROMBOXANE GENERATING SYSTEMS AND THEIR SELECTIVE-INHIBITION [J].
MONCADA, S ;
NEEDLEMAN, P ;
BUNTING, S ;
VANE, JR .
PROSTAGLANDINS, 1976, 12 (03) :323-335
[8]   IDENTIFICATION OF AN ENZYME IN PLATELET MICROSOMES WHICH GENERATES THROMBOXANE-A-2 FROM PROSTAGLANDIN ENDOPEROXIDES [J].
NEEDLEMAN, P ;
MONCADA, S ;
BUNTING, S ;
VANE, JR ;
HAMBERG, M ;
SAMUELSSON, B .
NATURE, 1976, 261 (5561) :558-560
[9]   THROMBOXANE A2-ANTAGONISTIC EFFECT OF PYRIDINOLCARBAMATE AND PHTHALAZINOL [J].
SHIMAMOTO, T ;
TAKASHIMA, Y ;
KOBAYASHI, M ;
MORIYA, K ;
TAKAHASHI, T .
PROCEEDINGS OF THE JAPAN ACADEMY, 1976, 52 (10) :591-594
[10]  
TAKEGUCHI C, 1971, BIOCHEMISTRY-US, V10, P2372