EM 405: a new compound with analgesic and anti-inflammatory properties and no gastrointestinal side-effects.
EM 405 has analgesic and antitussive effects, probably exerted by noradrenaline uptake inhibition and local anaesthetic actions. It showed anti-inflammatory, which may be due to anti-histaminic and indirect sympathomimetic properties. As oral application of EM 405 did not induce gastrointestinal side effects a possible ulcer preventing action was investigated. EM 405 reduced gastric ulcers induced by ethnology or indomethacin with ED50 values of 45 and 26 mg/kg p.o. Stress-induced ulcer was inhibited with an ED50 of 34 mg/kg. EM 405 reduced basal and stimulated gastric secretion by reducing volume as well as H(+)- and Cl(-)-production. Therefore ulcer prevention by EM 405 may be explained by its inhibitory effects on gastric secretion. The results characterise EM 405 as a novel anti-inflammatory compound with ulcer-protective action.
Selve
N
N
Department of Pharmacology, Grünenthal GmbH, Aachen, FRG.
Friderichs
E
E
Graudums
I
I
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology* / Q000633:toxicity; D003510:Cyclohexanes / Q000008:administration & dosage / Q000494:pharmacology* / Q000633:toxicity; D053138:Cyclohexenes; D005744:Gastric Acid / Q000378:metabolism; D008297:Male; D010418:Pentagastrin / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D013276:Stomach Ulcer / Q000139:chemically induced / Q000188:drug therapy* / Q000517:prevention & control; D013312:Stress, Physiological
D000894:Anti-Inflammatory Agents, Non-Steroidal; D003510:Cyclohexanes; D053138:Cyclohexenes; C069436:EM 405; D010418:Pentagastrin