ArticleDrug metabolism and disposition: the biological fate of chemicals2011
Effect of dose escalation on the in vivo oral absorption and disposition of glycylsarcosine in wild-type and Pept1 knockout mice.
Article in Drug metabolism and disposition: the biological fate of chemicals, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 22 citations in OpenAlex.
- Corrigendum: Inflammatory and Microbiota-Related Regulation of the Intestinal Epithelial Barrier.Frontiers in nutrition · 2021Article
- Inflammatory and Microbiota-Related Regulation of the Intestinal Epithelial Barrier.Frontiers in nutrition · 2021Review
- Current Evidence on the Bioavailability of Food Bioactive Peptides.Molecules (Basel, Switzerland) · 2020Review
- Evaluating the intestinal and oral absorption of the prodrug valacyclovir in wildtype and huPepT1 transgenic mice.Biochemical pharmacology · 2018Article
- In Silico Absorption Analysis of Valacyclovir in Wildtype and Pept1 Knockout Mice Following Oral Dose Escalation.Pharmaceutical research · 2017Article
- Carnosine Attenuates the Development of both Type 2 Diabetes and Diabetic Nephropathy in BTBR ob/ob Mice.Scientific reports · 2017Article
- The proton-coupled oligopeptide transporter 1 plays a major role in the intestinal permeability and absorption of 5-aminolevulinic acid.British journal of pharmacology · 2016Article
- Strategic approaches to optimizing peptide ADME properties.The AAPS journal · 2015Review
- Modern prodrug design for targeted oral drug delivery.Molecules (Basel, Switzerland) · 2014Article
- Development and characterization of a novel mouse line humanized for the intestinal peptide transporter PEPT1.Molecular pharmaceutics · 2014Article
- In vivo absorption and disposition of cefadroxil after escalating oral doses in wild-type and PepT1 knockout mice.Pharmaceutical research · 2013Article
- Relevance of PepT1 in the intestinal permeability and oral absorption of cefadroxil.Pharmaceutical research · 2013Article
- Significance of peptide transporter 1 in the intestinal permeability of valacyclovir in wild-type and PepT1 knockout mice.Drug metabolism and disposition: the biological fate of chemicals · 2013Article
- Proton-coupled oligopeptide transporter family SLC15: physiological, pharmacological and pathological implications.Molecular aspects of medicineReview
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
This study evaluated the in vivo absorption and disposition of glycylsarcosine (GlySar), after escalating oral doses, in wild-type and peptide transporter 1 (Pept1) knockout mice. [(3)H]GlySar was administered to mice at doses of 1, 10, 100, 1000, and 5000 nmol/g b.wt. Serial blood samples were obtained over 480 min, the plasma was harvested, and the area under the plasma concentration-time curve (AUC) was determined. It was observed that the GlySar AUC was 60, 45, and 30% lower in knockout than wild-type mice when evaluated over 2, 4, and 8 h, respectively (p < 0.01). Plasma levels of GlySar reached a plateau at 90 min in knockout mice and then rose to a second plateau at 240 min. In wild-type mice, the plasma levels rose continuously to reach a single plateau at 90 min. When partial AUC (0-120 min) was used as an indicator for rate of absorption, there was a 60% reduction in GlySar absorption rate in knockout mice compared with wild-type animals. Tissue distribution studies were also performed after 10 nmol/g oral doses of [(3)H]GlySar. When sampled 1 h after dosing, GlySar tissue concentrations were significantly lower in knockout versus wild-type mice and, with the exception of intestines, reflected differences in the systemic exposure of dipeptide between these two genotypes. Overall, PEPT1 ablation in mice resulted in significant reductions, in vivo, in the rate and extent of GlySar absorption. The AUC of GlySar was proportional to dose in both genotypes over 1 to 100 nmol/g, with minor decrements at the two highest doses.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.