GLC determination of dl-2-(3-phenoxyphenyl)propionic acid (fenoprofen) in human plasma

✍ Scribed by J. F. Nash; R. J. Bopp; A. Rubin

• Publisher: John Wiley and Sons
• Year: 1971
• Tongue: English
• Weight: 358 KB
• Volume: 60
• Category: Article
• ISSN: 0022-3549
• DOI: 10.1002/jps.2600600713

✦ Synopsis

H /N=C(-0)-. \ +

In general, of the compounds studied, the lactams possess predominantly CNS-stimulant activities. This effect is especially pronounced with 2-azacyclooctanone and 2-azacyclononanone. While many compounds were studied in order to make a generalization with regard to the effects of lipophilic-hydrophilic character and alkyl substitutions on the general biological behavior of these drugs, the majority of the report converges on the most active stimulants, namely 2-azacyclooctanone and 2-azacyclononanone. By various methodologies, sufficient data and information were obtained to conclude that they are CNS stimulants with the predominant site of action located in the midbrain and the medulla. that is, supraspinal and subcortical.

Nikethamide and pentylenetetrazole are two clinically useful stimulant drugs thought to exert their effects also in the midbrain and medulla. Moreover, all penicillins are irritating to the CNS. EEG abnormalities and convulsions have followed the application of penicillin directly to the human cerebral cortex (10). The administration of high doses of penicillin intravenously has produced convulsions in some patients, and convulsions and death have occurred following intraarterial administration of large doses of penicillin to patients with impaired renal function (1 I). The penicillins, like nikethamide and pentylenetetrazole, also contain moieties that have similar resonating structures to the compounds discussed in this report. These observations, together with the results presented in this report, particularly those obtained with 2-azacyclooctanone and 2-azacyclononanone, demonstrate that the resonating moiety referred to confers upon many substances CNS-stimulant activities.