ABSTRACT
The synthesis of N-phenyl-1,3,3-trimethyl-2-oxabicyclo[2.2.2]octan-6-cis-amine (III) starting from 6-nitrimino-1,3,3-trimethyl-2-oxabicyclo[2.2.2]octane, as well as of a series of amides (IV) and ureas (VI) derived from (III), is described. A number of compounds (IV) showed strong hypotensive and bradycardic activity in rats, whereas the urea (IVb) showed infiltration anesthesia in mice similar to that of lidocaine. Antiarrhythmic activity in mice and antiacetylcholine activity in vitro are also reported.
Subject(s)
Antihypertensive Agents/chemical synthesis , Bridged Bicyclo Compounds/chemical synthesis , Bridged-Ring Compounds/chemical synthesis , Acetylcholine/antagonists & inhibitors , Anesthetics, Local/chemical synthesis , Animals , Bridged Bicyclo Compounds/pharmacology , Chemical Phenomena , Chemistry , Heart Rate/drug effects , Mice , Rats , Time FactorsSubject(s)
Intestines/drug effects , Muscle, Smooth/drug effects , Phosphocreatine/pharmacology , Uterus/drug effects , Animals , Female , Mice , Rabbits , RatsABSTRACT
An experimental assessment was made of the analgesic, anti-inflammatory and platelet anticlumping activity of ketoprophene lysine, and its effect on body temperature and prostaglandin synthesis. The drug's pharmacodynamics was very similar to that of ketoprophene and its gastric tolerance was better. It was also well tolerated by the dog joint surfaces and cardiovascular apparatus when given i.m. or i.v., even at doses higher than those advised for man, or when infiltrated in ketoreceptor areas.
