Pub. Date : 2022 May
PMID : 35090865
7 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | The aim of this study was to investigate the contributions of multiple transport mechanisms to the intestinal absorption of metformin, focusing on OCT3, PMAT, THTR2, SERT and OCTN2. | Metformin | solute carrier family 19 member 3 | Homo sapiens |
| 2 | Uptake studies with MDCKII cells expressing OCT3, PMAT, THTR2 or SERT confirmed that metformin is a substrate of these transporters. | Metformin | solute carrier family 19 member 3 | Homo sapiens |
| 3 | 7-Cyclopentyl inhibited OCT3- and THTR2-mediated uptake of metformin. | Metformin | solute carrier family 19 member 3 | Homo sapiens |
| 4 | AG835, thiamine and paroxetine specifically inhibited PMAT-, THTR2- and SERT-mediated uptake of metformin, respectively. | Metformin | solute carrier family 19 member 3 | Homo sapiens |
| 5 | Using these inhibitors, the relative contributions of OCT3, PMAT, THTR2, SERT, OCTN2 and others to the intestinal permeation of metformin across Caco-2 cells were estimated to be 9.77%, 9.68%, 22.2%, 1.52%, 0% and 0.66%, respectively. | Metformin | solute carrier family 19 member 3 | Homo sapiens |
| 6 | Concentration-dependent analysis of metformin uptake by Caco-2 cells revealed nonlinear kinetics with the similar Km(app) value to the value for THTR2. | Metformin | solute carrier family 19 member 3 | Homo sapiens |
| 7 | The present study indicated that THTR2 is the major determinant of the nonlinear absorption of metformin, although multiple transport mechanisms contribute to its intestinal absorption. | Metformin | solute carrier family 19 member 3 | Homo sapiens |