ArticleDrug metabolism and disposition: the biological fate of chemicals2010
Monocarboxylate transporter-mediated transport of gamma-hydroxybutyric acid in human intestinal Caco-2 cells.
Article in Drug metabolism and disposition: the biological fate of chemicals, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 34 citations in OpenAlex.
- Gut Microbiota Alter Colonic Expression of Genes Encoding Drug Transporters and Drug-Metabolizing Enzymes in Mice.International journal of molecular sciences · 2026Article
- Toxicokinetic/Toxicodynamic Interaction Studies in Rats between the Drugs of Abuse γ-Hydroxybutyric Acid and Ketamine and Treatment Strategies for Overdose.Pharmaceutics · 2021Article
- γ-Hydroxybutyric Acid: Pharmacokinetics, Pharmacodynamics, and Toxicology.The AAPS journal · 2021Review
- Establishing quasi-steady state operations of microphysiological systems (MPS) using tissue-specific metabolic dependencies.Scientific reports · 2018Article
- Toxicologic/transport properties of NCS-382, a γ-hydroxybutyrate (GHB) receptor ligand, in neuronal and epithelial cells: Therapeutic implications for SSADH deficiency, a GABA metabolic disorder.Toxicology in vitro : an international journal published in association with BIBRA · 2018Article
- The Drug of Abuse Gamma-Hydroxybutyric Acid Exhibits Tissue-Specific Nonlinear Distribution.The AAPS journal · 2017Article
- Effect of chronic γ-hydroxybutyrate (GHB) administration on GHB toxicokinetics and GHB-induced respiratory depression.The American journal of drug and alcohol abuse · 2017Article
- Butyric acid increases transepithelial transport of ferulic acid through upregulation of the monocarboxylate transporters SLC16A1 (MCT1) and SLC16A3 (MCT4).Archives of biochemistry and biophysics · 2016Article
- A Novel Monocarboxylate Transporter Inhibitor as a Potential Treatment Strategy for γ-Hydroxybutyric Acid Overdose.Pharmaceutical research · 2015Article
- Effect of 3,4-methylenedioxymethamphetamine on the toxicokinetics and sedative effects of the drug of abuse, γ-hydroxybutyric acid.Journal of pharmaceutical sciences · 2014Article
- Mechanistic modeling of monocarboxylate transporter-mediated toxicokinetic/toxicodynamic interactions between γ-hydroxybutyrate and L-lactate.The AAPS journal · 2014Article
- Role of monocarboxylate transporters in drug delivery to the brain.Current pharmaceutical design · 2014Review
- Toxicokinetics/Toxicodynamics of γ-hydroxybutyrate-ethanol intoxication: evaluation of potential treatment strategies.The Journal of pharmacology and experimental therapeutics · 2013Article
- Effects of monocarboxylate transporter inhibition on the oral toxicokinetics/toxicodynamics of γ-hydroxybutyrate and γ-butyrolactone.The Journal of pharmacology and experimental therapeutics · 2013Article
- Native disorder mediates binding of dynein to NudE and dynactin.Biochemical Society transactions · 2012Review
- γ-Hydroxybutyrate blood/plasma partitioning: effect of physiologic pH on transport by monocarboxylate transporters.Drug metabolism and disposition: the biological fate of chemicals · 2012Article
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
The objectives of this study were to determine mRNA expression of monocarboxylate transporters (MCT) and to evaluate intestinal transport of the MCT substrates gamma-hydroxybutyrate (GHB) and d-lactate in human intestinal Caco-2 cells. The presence of mRNA for MCT1, 2, 3, and 4 was observed in Caco-2 cells. The uptake of both GHB and d-lactate in Caco-2 cells was demonstrated to be pH- and concentration-dependent and sodium-independent. The uptake of GHB and d-lactate was best described by a Michaelis-Menten equation with passive diffusion (GHB: K(m) = 17.6 +/- 10.5 mM, V(max) = 17.3 +/- 11.7 nmol/min/mg, and P = 0.38 +/- 0.15 microl/min/mg; and d-lactate: K(m) = 6.0 +/- 2.9 mM, V(max) = 35.0 +/- 18.4 nmol/min/mg, and P = 1.3 +/- 0.6 microl/min/mg). The uptake of GHB and d-lactate was significantly decreased by the known MCT inhibitor alpha-cyano-4-hydroxycinnamate and the MCT substrates GHB and d-lactate but not by the organic cation tetraethylammonium chloride. Directional flux studies with both GHB and d-lactate suggested the involvement of carrier-mediated transport with the permeability in the apical to basolateral direction higher than that in the basolateral to apical direction. These findings confirm the presence of MCT1-4 in Caco-2 cells and demonstrate GHB and d-lactate transport characteristics consistent with proton-dependent MCT-mediated transport.
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Registered trials
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.