New isosorbide 5-mononitrate derivative with hypotensive activity.
Synthesis and pharmacological properties of the 5-fluoro-nicotinic ester with isosorbide-5-mononitrate 3 are reported. The new compound shows an in vitro activity on rabbit aortic helical strips five times higher than isosorbide-5-mononitrate. The hypotensive activity in guinea-pigs of 3 is markedly superior to that of 5-ISMN. In the rat 3 shows a bioavailability and an acute toxicity inferior to those of 5-ISMN after oral administration.
Coppi
G
G
Borella
F
F
Gatti
M T
MT
Comini
A
A
Dall' Asta
L
L
D000818:Animals; D000959:Antihypertensive Agents / Q000138:chemical synthesis* / Q000633:toxicity; D001794:Blood Pressure / Q000187:drug effects; D055598:Chemical Phenomena; D002621:Chemistry; D005260:Female; D006168:Guinea Pigs; D066298:In Vitro Techniques; D007548:Isosorbide Dinitrate / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology / Q000633:toxicity; D008297:Male; D051379:Mice; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains
D000959:Antihypertensive Agents; D007548:Isosorbide Dinitrate; C030397:isosorbide-5-mononitrate