Characterization of the human intestinal drug transport with using chamber system incorporating freshly isolated human jejunum was written by Michiba, Kazuyoshi;Maeda, Kazuya;Kurimori, Ko;Enomoto, Tsuyoshi;Shimomura, Osamu;Takeuchi, Tomoyo;Nishiyama, Hiroyuki;Oda, Tatsuya;Kusuhara, Hiroyuki. And the article was included in Drug Metabolism & Disposition in 2021.Product Details of 83799-24-0 The following contents are mentioned in the article:
The present study aimed to characterize the Ussing chamber system incorporating human intestinal tissue as an in vitro model for investigating the impact of intestinal uptake/efflux transporters on the intestinal absorption of substrate drugs in humans. We confirmed the functions of major intestinal uptake/efflux drug transporters in freshly isolated human jejunum sections by demonstrating a significant decrease in the mucosal uptake of cefadroxil and methotrexate (proton-coupled folate transporter), mucosal-to-serosal permeability of ribavirin and serosal-to-mucosal permeability of P-glycoprotein and breast cancer resistance protein substrates in the presence of their typical inhibitors. The mucosal-to-serosal apparent permeability coefficients (Papp) of 19 drugs, including substrates of drug transporters and cytochrome P 450 3A, ranged from 0.60 x 10-6 to 29 x 10-6 cm/s and showed a good correlation with reported fraction of an oral dose that enters the gut wall and passes into the portal circulation with escaping intestinal metabolism (FaFg) values in humans. Furthermore, the Papp values for cefadroxil, methotrexate, and ribavirin in the presence of the corresponding transporter inhibitors underestimated the FaFg of these drugs, which clearly showed that intestinal uptake transporters facilitate their intestinal absorption in humans. In conclusion, the functions of major intestinal uptake/efflux drug transporters could be maintained in freshly isolated human jejunum sections. This study involved multiple reactions and reactants, such as 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0Product Details of 83799-24-0).
2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Product Details of 83799-24-0
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem