Pharmacology of mesoionic oxatriazole derivatives in blood, cardiovascular and respiratory systems.
Mesoionic oxatriazole derivatives were synthetized by GEA LTD1. The GEA compounds (GEAC) constitute a new class of NO-donors, some of which stimulate selectively guanylate cyclase abiding either platelets or leukocytes or lung tissues. In consequence, some of GEAC are potent anti-platelet, fibrinolytic, thrombolytic or broncholytic agents, both in vitro and in vivo. GEAC synergize with prostacyclin in their thrombolytic actions. They also suppress the release of histamine and leukotriene B4, and prevent degranulation of granulocytes. Methylene blue reduces, and zaprinast augments their pharmacological effects. It is suggested that within a series of the newly synthetized GEA compounds there are likely to be found potential candidates for treating either thrombotic or asthmatic disorders.
Corell
T
T
A/S GEA Farmaceutisk Fabrik, Pharmacological and Toxicological Department Hvidovre, Denmark.
Pedersen
S B
SB
Lissau
B
B
Moilanen
E
E
Metsä-Ketelä
T
T
Kankaanranta
H
H
Vuorinen
P
P
Vapaatalo
H
H
Rydell
E
E
Andersson
R
R
D000818:Animals; D001792:Blood Platelets / Q000187:drug effects* / Q000378:metabolism; D001794:Blood Pressure / Q000187:drug effects; D016084:Bronchoconstriction / Q000187:drug effects; D002415:Cats; D006152:Cyclic GMP / Q000378:metabolism; D005260:Female; D005342:Fibrinolysis / Q000187:drug effects; D006162:Guanylate Cyclase / Q000378:metabolism; D006168:Guinea Pigs; D006636:Histamine Release / Q000187:drug effects; D006801:Humans; D066298:In Vitro Techniques; D007962:Leukocytes / Q000187:drug effects* / Q000378:metabolism; D008297:Male; D009130:Muscle, Smooth / Q000187:drug effects; D009569:Nitric Oxide / Q000378:metabolism*; D010069:Oxadiazoles / Q000097:blood / Q000494:pharmacology*; D010974:Platelet Aggregation / Q000187:drug effects; D011817:Rabbits; D051381:Rats; D017208:Rats, Wistar; D014132:Trachea / Q000187:drug effects* / Q000502:physiology; D014230:Triazoles / Q000097:blood / Q000494:pharmacology*; D014664:Vasodilation / Q000187:drug effects
D010069:Oxadiazoles; D014230:Triazoles; D009569:Nitric Oxide; D006162:Guanylate Cyclase; D006152:Cyclic GMP