+ Site Statistics
+ Search Articles
+ Subscribe to Site Feeds
EurekaMag Most Shared ContentMost Shared
EurekaMag PDF Full Text ContentPDF Full Text
+ PDF Full Text
Request PDF Full TextRequest PDF Full Text
+ Follow Us
Follow on FacebookFollow on Facebook
Follow on TwitterFollow on Twitter
Follow on LinkedInFollow on LinkedIn

+ Translate

Disposition of aprophen in rats

Disposition of aprophen in rats

Journal of Pharmacy and Pharmacology 38(12): 928-930

The pharmacokinetics of [14C]aprophen and its distribution were determined after intravenous administration to rats. The drug was distributed rapidly with a t1/2 (.alpha.) of 4 min to highly perfused organs like the brain, kidney and adrenals. An elimination phase was apparent 10 min after injection with a t1/2 (.beta.) of 23.5 min. The high plasma clearance of the drug was due both to a large volume of distribution and to a high metabolic rate. Aprophen could be hydrolysed to diphenylpropionic acid and diethylaminoethanol in-vivo and in-vitro. Diethylaminoethanol competed with [3H]QNB binding to muscarinic receptors of N4TG1 cells, whereas diphenylpropionic acid did not. The lower plasma concentrations and lower binding activity of diethylaminoethanol compared with aprophen indicate that unchanged aprophen is largely responsible for the in-vitro actions.

(PDF emailed within 1 workday: $29.90)

Accession: 005170752

Download citation: RISBibTeXText

PMID: 2880971

Related references

Isolation and identification of beta-hydroxyethylaprophen: a urinary metabolite of aprophen in rats. Journal of Chromatography 563(2): 466-471, 1991

Antagonism by atropine scopolamine and aprophen of physostigmine effects on rats performance of a radial maze learning task. Society for Neuroscience Abstracts 15(1): 734, 1989

Comparative effect of central cholinolytics amisyl, aprophen and corresponding quinuclidine esters on conditioned reflex activity and behavior of rats. Farmakologiia i Toksikologiia 32(1): 16-20, 1969

Comparative effects of the central anti cholinergics benactyzine and aprophen and of the quinuclidine ethers corresponding to them on the conditioned reflex activity and behavior of rats. Farmakologiya i Toksikologiya (Moscow) 32(1): 16-20, 1969

Disposition of a glucose load in fed rats and rats adapted to a high-carbohydrate diet. American Journal of Physiology 256(6 Pt 1): E811-E817, 1989

The influence of Aprophen. Tr Orenburg Otd Vses Fiziol Obshchest 3: 262-265, 1964

A new qualitative reaction for aprophen. Aptechnoe Delo 10: 54-56, 1961

The use of aprophen in internal diseases. Sovetskaia Meditsina 21(8): 122-124, 1957

The new spasmolytics, Aprophen and Diprophen. Med Promyshlennost Sssr 6: 43-45, 1957

Antimuscarinic activity of aprophen. Biochemical Pharmacology 32(19): 2979-2981, 1983

Pharmacology of a new spasmolytic drug aprophen. Farmakologiia i Toksikologiia 20(4): 42-48, 1957

The determination of aprophen in medicinal forms. Farmatsiia 22(2): 58-60, 1973

Treatment of coronary insufficiency with aprophen. Klinicheskaia Meditsina 36(5): 138-139, 1958

Use of aprophen in the preparation for and induction of labor. Akusherstvo i Ginekologiia 27(4): 39-43, 1988