[The pharmacologic activity of p-substituted DL-2-phenylglycine octyl esters].
DL-2-phenylglycine octyl ester has antiphlogistic, analgesic and spasmolytic activities as shown in different animal models. The antiphlogistic effectiveness is changed only a little by the p-substitution at the phenyl ring, whereas the analgesic action is markedly influenced. Most of the substituted compounds are significantly more active than the unsubstituted ester. DL-2-(benzyloxyphenyl)glycine octyl ester is the most active compound, it has furthermore the highest therapeutic quotient. Using the i.p. application its efficacy exceeds that of acetylsalicylic acid, phenylbutazone and indometacin, respectively. The spasmolytic activity is differently changed by the substituents. The most active ester, DL-2-(p-methoxyphenyl)glycine octyl ester, is about two times more active than papaverine. In histamine induced spasm the effectiveness is low compared with the specific antagonist mepyramine. The results obtained show that the activities of the p-substituted DL-2-phenylglycine octyl esters are different with regard to the three investigated pharmacological properties.
Schulz
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Institut für Pharmakologie und Toxikologie der Universität Rostock.
Sprung
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WD
Kobow
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D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology* / Q000633:toxicity; D001169:Arthritis, Experimental / Q000517:prevention & control; D002210:Caprylates / Q000494:pharmacology* / Q000633:toxicity; D002351:Carrageenan; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy; D005260:Female; D005998:Glycine / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000633:toxicity; D006168:Guinea Pigs; D066298:In Vitro Techniques; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D010276:Parasympatholytics; D051381:Rats; D011919:Rats, Inbred Strains
D000894:Anti-Inflammatory Agents, Non-Steroidal; D002210:Caprylates; D010276:Parasympatholytics; C008852:2-phenylglycine; D002351:Carrageenan; D005998:Glycine
Zur pharmakologischen Wirksamkeit p-substituierter DL-2-Phenylglycinoctylester.