Inhibition of cytosolic Ca++ mobilization in human platelets by the antianginal drug trapidil and its derivative AR 12463.
The antianginal drug trapidil (5-methyl-7-diethylamino-s-triazolo-(1.5-a)pyrimidine) and its derivative AR 12463 (5-piperidino-7-(N-(n-amyl)-N-(beta-hydroxyethyl)-amino)-s-triazolo(1.5- a) pyrimidine) inhibit the thromboxane A2 agonist (U-46619)-induced mobilization of intracellular platelet-free Ca++ as measured with the fluorescent Ca++ indicator Indo-1. This inhibitory effect is independent of extracellular Ca++ concentration, and AR 12463 is about 70-fold more active than trapidil itself.
Block
H U
HU
Institute of Pharmacology and Toxicology, Martin Luther University, Halle, GDR.
Gabbasov
Z A
ZA
Pozin
E Y
EY
Popov
E G
EG
Mest
H J
HJ
D019796:15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid; D000959:Antihypertensive Agents / Q000494:pharmacology*; D001792:Blood Platelets / Q000187:drug effects / Q000378:metabolism*; D002118:Calcium / Q000097:blood*; D003600:Cytosol / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D066298:In Vitro Techniques; D007700:Kinetics; D010727:Phosphoric Diester Hydrolases / Q000097:blood; D010974:Platelet Aggregation / Q000187:drug effects; D011450:Prostaglandin Endoperoxides, Synthetic / Q000494:pharmacology; D011743:Pyrimidines / Q000494:pharmacology*; D013931:Thromboxanes / Q000097:blood; D014192:Trapidil / Q000031:analogs & derivatives / Q000494:pharmacology*
D000959:Antihypertensive Agents; D011450:Prostaglandin Endoperoxides, Synthetic; D011743:Pyrimidines; D013931:Thromboxanes; D019796:15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid; D010727:Phosphoric Diester Hydrolases; D014192:Trapidil; D002118:Calcium; C053729:AR 12463