N-Phenyl-1,3,3-trimethyl-2-oxabicyclo[2.2.2]octan-6-cis-amine derivatives with hypotensive and other activities.

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.

[Experimental assessment of some pharmacodynamic features of ketoprofen lysine. Pain relief activity, antipyretic effects, anti-inflammatory activity, anti-platelet aggregation activity and interference with the biosynthesis of prostaglandins]. / Analisi sperimentale di alcuni aspetti farmacodinamici del ketoprofene lisina. Attività antidolorifica, effetti antipiretici, attività anti-infiammatoria, attività antiaggregante piastrinica ed interferenze con la biosintesi delle prostaglandine.

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.