Purpose: To compare the mucosal membrane transport of gabapentin and pregabalin in animal small intestine.
Methods: Uptake of the two drugs by brush-border membrane vesicles (BBMV) from rat and rabbit small intestine was studied as a function of temperature, uptake-medium sodium content, and intestinal region. Amino acid inhibition studies were conducted with pregabalin.
Results: Gabapentin uptake by rat and rabbit jejunal BBMV was sodium independent, whereas pregabalin uptake was sodium dependent. Uptake of both drugs in rabbit small intestinal vesicles was greater at 25 degrees C than at 4 degrees C in the absence of sodium and an additional increase in uptake was observed for pregabalin at 25 degrees C in the presence of sodium. Pregabalin uptake in rabbit duodenal, jejunal, and ileal BBMV was equivalent, whereas gabapentin uptake was greater in duodenal and ileal BBMV, compared with jejunal BBMV. Although inhibition is weak, a decrease in BBMV uptake of pregabalin is observed with coincubation of high concentrations of both neutral and basic amino acids.
Conclusions: Amino acid carriers mediate the apical uptake of both drugs in the small intestine. Although gabapentin and pregabalin are structurally similar, their small intestinal mucosal uptake differs in sodium dependence and region dependence. Gabapentin uptake is likely mediated by system b0,+, whereas pregabalin uptake is also mediated by B0 and/or B0,+.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1023/a:1010970809090 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
C1orf115 interacts with clathrin adaptors to undergo endocytosis and induces ABCA1 to promote enteric cholesterol efflux.
Cell Mol Life Sci
January 2025
School of Biomedical Sciences, The University of Hong Kong, Pokfulam, Hong Kong.
C1orf115 has been identified in high-throughput screens as a regulator of multidrug resistance possibly mediated through an interaction with ATP-dependent membrane transporter ABCB1. Here we show that C1orf115 not only shares structural similarities with FACI/C11orf86 to interact with clathrin adaptors to undergo endocytosis, but also induces ABCA1 transcription to promote cholesterol efflux. C1orf115 consists of an N-terminal intrinsically disordered region and a C-terminal α-helix.
View Article and Find Full Text PDFIntestinal rearrangement of biliopancreatic limbs, alimentary limbs, and common limbs in obese type 2 diabetic mice after duodenal jejunal bypass surgery.
Front Endocrinol (Lausanne)
January 2025
Department of Metabolic Surgery, Jinshazhou Hospital of Guangzhou University of Chinese Medicine, Guangzhou, China.
Bariatric surgery is an effective treatment for type 2 Diabetes Mellitus (T2DM), yet the precise mechanisms underlying its effectiveness remain incompletely understood. While previous research has emphasized the role of rearrangement of the gastrointestinal anatomy, gaps persist regarding the specific impact on the gut microbiota and barriers within the biliopancreatic, alimentary, and common limbs. This study aimed to investigate the effects of duodenal-jejunal bypass (DJB) surgery on obese T2DM mice.
View Article and Find Full Text PDFNatural life cycle and molecular characterization of Dollfus, 1960 (Cestoda: Taeniidae) from northwestern Patagonia, Argentina.
Int J Parasitol Parasites Wildl
April 2025
División Zoología Invertebrados, Facultad de Ciencias Naturales y Museo, Universidad Nacional de La Plata, CONICET-Centro Científico Tecnológico La Plata, Buenos Aires. Paseo del Bosque s/n La Plata, (1900), Buenos Aires, Argentina.
Through morphological and molecular studies, the natural life cycle of Dollfus, 1960 (Cestoda: Taeniidae) from Argentine Patagonia is elucidated, involving subterranean rodents (Ctenomyidae) as intermediate hosts, and the Andean fox (Canidae) as definitive host. Metacestodes (mono- and polycephalic fimbriocerci) were found mainly in the peritoneal cavity of , and the strobilate adult in the intestine of . Correspondence between metacestodes and strobilate adults was based primarily on number, size and shape of rostellar hooks: 45-53 hooks alternated in two rows, small hooks 88-180 μm long and large hooks 230-280 μm long, with the characteristic shape described in the two main description of the species, both that of the metacestode (original description) and that of the strobilate adult (obtained experimentally).
View Article and Find Full Text PDFStudy on the effects of Massa Medicata Fermentata with different formulations on the intestinal microbiota and enzyme activities in mice with spleen deficiency constipation.
Front Cell Infect Microbiol
January 2025
Scientific Research Department, Hunan Academy of Chinese Medicine, Changsha, China.
Objective: This study aims to explore the therapeutic mechanism of Massa Medicata Fermentata (MMF) with different formulations on spleen deficiency constipation in mice by analyzing gastrointestinal hormones, D-xylose, intestinal microbiota, and intestinal enzyme activities.
Methods: A spleen deficiency constipation model was established using an oral administration of Sennae Folium decoction combined with controlled diet and water intake. After successful model establishment, the mice with spleen deficiency constipation were treated with MMF S1, S2, S3.
Interaction of B0AT1 deficiency and diet on metabolic function and diabetes incidence in male NOD mice.
Endocrinology
January 2025
Australian National University School of Medicine and Psychology, Australian National University, Acton, ACT, 0200, Australia.
Context: The obesity epidemic parallels an increasing type 1 diabetes incidence, such that westernized diets, containing high fat, sugar and/or protein, through inducing nutrient-induced islet beta-cell stress, have been proposed as contributing factors. The broad-spectrum neutral amino acid transporter (B0AT1), encoded by Slc6a19, is the major neutral amino acids transporter in intestine and kidney. B0AT1 deficiency in C567Bl/6J mice, causes aminoaciduria, lowers insulinemia and improves glucose tolerance.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!