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Cellular uptake properties of lamotrigine in human placental cell lines: Investigation of involvement of organic cation transporters (SLC22A1-5).
Authors: Hasegawa N, Furugen A, Ono K, Koishikawa M, Miyazawa Y, Nishimura A, Umazume T, Narumi K, Kobayashi M, Iseki K Abstract Lamotrigine (LTG) is an important antiepileptic drug for the treatment of seizures in pregnant women with epilepsy. However, it is not known if the transport of LTG into placental cells occurs via a carrier-mediated pathway. The aim of this study was to investigate the uptake properties of LTG into placental cell lines (BeWo and JEG-3), and to determine the involvement of organic cation transporters (OCTs, SLC22A1-3) and organic cation/carnitine transporter (OCTNs, SLC22A4-5) in the uptak...
Source: Drug Metabolism and Pharmacokinetics - April 20, 2020 Category: Drugs & Pharmacology Tags: Drug Metab Pharmacokinet Source Type: research

Hesperidin alleviates rat postoperative ileus through anti-inflammation and stimulation of Ca(2+)-dependent myosin phosphorylation.
CONCLUSION: Oral administration of hesperidin effectively alleviates rat POI through inhibition of inflammatory responses and stimulation of Ca(2+)-dependent MLC phosphorylation. PMID: 27345626 [PubMed - as supplied by publisher]
Source: Acta Pharmacologica Sinica - June 26, 2016 Category: Drugs & Pharmacology Authors: Xiong YJ, Chu HW, Lin Y, Han F, Li YC, Wang AG, Wang FJ, Chen DP, Wang JY Tags: Acta Pharmacol Sin Source Type: research

Intestinal absorption mechanisms of MTBH, a novel hesperetin derivative, in Caco-2 cells, and potential involvement of monocarboxylate transporter 1 and multidrug resistance protein 2.
Abstract Hesperetin, the aglycone of hesperidin, occurs naturally in citrus fruits. It exerts extensive pharmacological activities. However, hesperetin's poor solubility and low bioavailability limits its wide application. In order to overcome these limitations, recently a series of novel hesperitin derivatives containing Mannich base moieties were synthesized and the anti-inflammatory activity was evaluated, among which MTBH (8-methylene-tert-butylamine-3',5,7-trihydroxy-4'-methoxyflavanone) showed a significantly improved water solubility, and promising anti-inflammatory activity in vitro and in vivo compared wi...
Source: European Journal of Pharmaceutical Sciences - July 28, 2015 Category: Drugs & Pharmacology Authors: Shen C, Chen R, Qian Z, Meng X, Hu T, Li Y, Chen Z, Huang C, Hu C, Li J Tags: Eur J Pharm Sci Source Type: research

Memantine transport by a proton-coupled organic cation antiporter in hCMEC/D3 cells, an in vitro human blood-brain barrier model.
Authors: Higuchi K, Kitamura A, Okura T, Deguchi Y Abstract Memantine is clinically used for the treatment of patients with Alzheimer's disease and is highly distributed to the brain. The aim of this study is to characterize memantine transport at the blood-brain barrier (BBB) using hCMEC/D3 cells, a human BBB model. The initial uptake velocity of memantine in hCMEC/D3 cells was concentration-dependent, and was reduced by metabolic inhibitors, but was independent of extracellular sodium ion and membrane potential. Intracellular alkalization and intracellular acidification markedly reduced and enhanced the uptake, r...
Source: Drug Metabolism and Pharmacokinetics - April 12, 2015 Category: Drugs & Pharmacology Tags: Drug Metab Pharmacokinet Source Type: research