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Pinane-thromboxane A2 (PTA2, [1alpha,2 beta(Z),-3 alpha (1E,3R*),5 alpha]-7-(3-(3-hydroxy-1-octenyl)-6,6-dimethylbicyclo[3.1.1]hept-2-yl)-5-heptenoic acid) has been synthesized and tested for biological activity in systems responsive to thromboxane A2, stable prostaglandin endoperoxide (PGH2) analogs, and prostatacyclin (PGI2). At low concentrations, PTA2 inhibited cat coronary artery constriction induced by stable prostaglandin endoperoxide analogs, and it stabilized liver lysosomes. At slightly higher concentrations, it inhibited platelet aggregation. At still higher concentrations, PTA2 inhibited thromboxane synthetase, but it had no effect on prostacyclin synthetase. The analog also had no effect on the inhibition of platelet aggregation by PGI2 or prostaglandin D2. It is suggested that PTA2 has a suitable biochemical profile for use as an antithrombotic agent.
K C Nicolaou, and
R L Magolda, and
J B Smith, and
D Aharony, and
E F Smith, and
A M Lefer
November 1982,
Prostaglandins, leukotrienes, and medicine,
K C Nicolaou, and
R L Magolda, and
J B Smith, and
D Aharony, and
E F Smith, and
A M Lefer
January 2001,
Zeitschrift fur Naturforschung. C, Journal of biosciences,
K C Nicolaou, and
R L Magolda, and
J B Smith, and
D Aharony, and
E F Smith, and
A M Lefer
January 1978,
Pharmacological research communications,
K C Nicolaou, and
R L Magolda, and
J B Smith, and
D Aharony, and
E F Smith, and
A M Lefer
January 1985,
Nature,
K C Nicolaou, and
R L Magolda, and
J B Smith, and
D Aharony, and
E F Smith, and
A M Lefer
August 1998,
Journal of cardiovascular pharmacology,
K C Nicolaou, and
R L Magolda, and
J B Smith, and
D Aharony, and
E F Smith, and
A M Lefer
March 1989,
FEBS letters,
K C Nicolaou, and
R L Magolda, and
J B Smith, and
D Aharony, and
E F Smith, and
A M Lefer
July 1991,
Zhongguo yao li xue bao = Acta pharmacologica Sinica,
K C Nicolaou, and
R L Magolda, and
J B Smith, and
D Aharony, and
E F Smith, and
A M Lefer
June 1997,
The Journal of pharmacology and experimental therapeutics,
K C Nicolaou, and
R L Magolda, and
J B Smith, and
D Aharony, and
E F Smith, and
A M Lefer
January 1980,
Advances in prostaglandin and thromboxane research,
K C Nicolaou, and
R L Magolda, and
J B Smith, and
D Aharony, and
E F Smith, and
A M Lefer
January 1987,
Haemostasis,
