Metabolism of the (+)-, (+/-)-, and (-)-enantiomers of alpha-methylfluorene-2-acetic acid (cicloprofen) in rats

Xenobiotica; the Fate of Foreign Compounds in Biological Systems
A V DeanE C Schreiber


1. After oral or intraperitoneal administration of (+/-)-[14C]cicloprofen to rats, the peak plasma concentrations of radioactivity and the areas under the plasma concentration/time curves did not increase proportionally with dose; total urinary and faecal excretions of radioactivity did increase with dose, suggesting saturation of plasma protein binding of drug and faster elimination of unbound drug at higher doses. 2. [14C]Cicloprofen and its metabolites were eliminated mainly via biliary excretion. Ratios of faecal to urinary excretion ranged from 2 to 3 and depended on dose administered. 3. Rats with cannulated bile ducts excreted the drug almost exclusively in bile, whereas intact rats excreted up to 32% of the dose in urine in 6 days, suggesting that [14C]cicloprofen or its metabolites or both undergo extensive enterohepatic recirculation in the rats. 4. The major metabolites of [14C]cicloprofen excreted in urine or bile were the 7-hydroxy, 9-hydroxy-, 7,9-dihydroxy-, and 9-hydroxy-9-methoxy-derivatives and their glucuronide or sulphate conjugates. 5. The (+)-enantiomer of [14C]cicloprofen was hydroxylated and excreted by rats at a faster rate than its (-)-antipode; no qualitative stereoselective metabolism of the individu...Continue Reading


Feb 1, 1978·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·S J LanA I Cohen
Jul 1, 1979·Journal of Pharmaceutical Sciences·T IshidaT Aratani
Nov 1, 1981·Journal of Pharmaceutical Sciences·J K StoltenborgF M Vane
Nov 1, 1992·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·T Ishida, T Matsumoto


Mar 1, 1976·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·K J KripalaniE C Schreiber
Jan 1, 1973·Drug Metabolism Reviews·P Jenner, B Testa
Oct 1, 1972·Journal of Medicinal Chemistry·E T StillerS D Levine

Related Concepts

Metabolic Process, Cellular
Structure-Activity Relationship
Anti-Inflammatory Agents
Body Excretions
Metabolic Pathway
Excretory Function
Bile Duct Structure

Trending Feeds


Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Synapse Loss as Therapeutic Target in MS

As we age, the number of synapses present in the human brain starts to decline, but in neurodegenerative diseases this occurs at an accelerated rate. In MS, it has been shown that there is a reduction in synaptic density, which presents a potential target for treatment. Here is the latest research on synapse loss as a therapeutic target in MS.

Artificial Intelligence in Cardiac Imaging

Artificial intelligence (ai) techniques are increasingly applied to cardiovascular (cv) medicine in cardiac imaging analysis. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

Social Learning

Social learning involves learning new behaviors through observation, imitation and modeling. Follow this feed to stay up to date on the latest research.

Cell Atlas of the Human Eye

Constructing a cell atlas of the human eye will require transcriptomic and histologic analysis over the lifespan. This understanding will aid in the study of development and disease. Find the latest research pertaining to the Cell Atlas of the Human Eye here.

Single Cell Chromatin Profiling

Techniques like ATAC-seq and CUT&Tag have the potential to allow single cell profiling of chromatin accessibility, histones, and TFs. This will provide novel insight into cellular heterogeneity and cell states. Discover the latest research on single cell chromatin profiling here.

Genetic Screens in iPSC-derived Brain Cells

Genetic screening is a critical tool that can be employed to define and understand gene function and interaction. This feed focuses on genetic screens conducted using induced pluripotent stem cell (iPSC)-derived brain cells.