Pathophysiological actions of thromboxane A2 and their pharmacological antagonism by thromboxane receptor blockade with GR32191.
With a growing general conviction that thromboxane A2 does have a pathological role in occlusive vascular disease, there is a current debate on the ideal type of drug treatment needed. The more widely accepted view now seems to be that drugs that antagonize the actions of thromboxane A2 by blocking its receptors have greater clinical potential than those that block its synthesis. However, this premise has yet to be proven clinically. The historical development of thromboxane receptor blockers as a new class of medicines and, in particular, that of GR32191, are described here. The clinical evaluation of GR32191 should determine the importance of thromboxane A2 in cardiovascular disease.
Humphrey
P P
PP
Glaxo Group Research Limited, Ware, Hertfordshire, UK.
Hallet
P
P
Hornby
E J
EJ
Wallis
C J
CJ
Collington
E W
EW
Lumley
P
P
D000818:Animals; D001713:Biphenyl Compounds / Q000494:pharmacology*; D002318:Cardiovascular Diseases / Q000188:drug therapy; D016861:Cyclooxygenase Inhibitors; D006168:Guinea Pigs; D006538:Heptanoic Acids / Q000494:pharmacology*; D006801:Humans; D066298:In Vitro Techniques; D008297:Male; D009131:Muscle, Smooth, Vascular / Q000187:drug effects; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000494:pharmacology; D011982:Receptors, Prostaglandin / Q000187:drug effects*; D017482:Receptors, Thromboxane; D013928:Thromboxane A2 / Q000037:antagonists & inhibitors* / Q000494:pharmacology*; D013930:Thromboxane-A Synthase / Q000037:antagonists & inhibitors
D001713:Biphenyl Compounds; D016861:Cyclooxygenase Inhibitors; D006538:Heptanoic Acids; D010975:Platelet Aggregation Inhibitors; D011982:Receptors, Prostaglandin; D017482:Receptors, Thromboxane; D013928:Thromboxane A2; D013930:Thromboxane-A Synthase; C060013:vapiprost