Prostaglandin H2 (PGH2) was first isolated from incubations of arachidonic acid with ovine seminal vesicle microsomes, and was described as a potent vasoconstrictor.1 PGH2 is the precursor for all 2-series PGs and thromboxanes (TXs),2 and is a TP receptor agonist which irreversibly aggregates human platelets at 50-100 ng/ml. PGH2 is a suicide substrate for platelet TX synthase possessing a Ki of 18 µM as compared to 28 µM for PGH1.3
1
Hamberg, M., Svensson, J., Wakabayashi, T., et al. Isolation and structure of two prostaglandin endoperoxides that cause platelet aggregation. Proc Natl Acad Sci USA71345-349(1974).
2
Samuelsson, B., Goldyne, M., Granström, E., et al. Prostaglandins and thromboxanes. Annu Rev Biochem47997-1029(1978).
3
Jones, D.A., and Fitzpatrick, F.A. “Suicide” inactivation of thromboxane A2 synthase. Characteristics of mechanism-based inactivation with isolated enzyme and intact platelets.. J Biol Chem26520166-20171(1990).
Jones, D.A., and Fitzpatrick, F.A. “Suicide” inactivation of thromboxane A2 synthase. Characteristics of mechanism-based inactivation with isolated enzyme and intact platelets.. J Biol Chem26520166-20171(1990).
Samuelsson, B., Goldyne, M., Granström, E., et al. Prostaglandins and thromboxanes. Annu Rev Biochem47997-1029(1978).
Hamberg, M., Svensson, J., Wakabayashi, T., et al. Isolation and structure of two prostaglandin endoperoxides that cause platelet aggregation. Proc Natl Acad Sci USA71345-349(1974).
Prostaglandin H2 is available in the following screening
library: