PMID: 8595061Oct 1, 1995Paper

Metabolic fate of the new antithrombotic agent aspalatone in rats. In vivo and in vitro study

Arzneimittel-Forschung
D Y SuhB H Han

Abstract

In order to determine whether aspalatone ([3-(2-methyl-4-pyronyl)]-2- acetyloxybenzoate, CAS 147249-33-0), a new antiplatelet agent, behaves as a prodrug of acetylsalicylic acid (ASA), metabolism studies in rats were carried out in vivo and in vitro using the whole animal and tissue homogenates. The ASA molecule was not detected in the plasma samples taken after oral administration of aspalatone at 80 mg/kg. Instead, salicylic acid maltol ester (SM), the deacetylated metabolite of aspalatone, was detected in the plasma and it was rapidly hydrolyzed to salicylic acid. In in vitro experiments with rat serum, intestinal fluid, liver and gastric mucosal homogenates, SM was the only compound formed after 4 min incubation at 37 degrees C. From these results it was concluded that aspalatone does not behave as a prodrug of ASA in rats. In addition, the results of experiments using certain esterase inhibitors, suggested the major contribution of B-esterase(s) in the metabolism of aspalatone to SM particularly in serum and intestinal fluid.

Related Concepts

Trending Feeds

COVID-19

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.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

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.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. 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.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.