The organic cation transporters (OCT1, OCT2, EMT) and the plasma membrane monoamine transporter (PMAT) show differential distribution and cyclic expression pattern in human endometrium and early pregnancy decidua

2007 ◽  
Vol 74 (10) ◽  
pp. 1303-1311 ◽  
Author(s):  
Barbara Bottalico ◽  
Vera Noskova ◽  
Radovan Pilka ◽  
Irene Larsson ◽  
Henryk Domanski ◽  
...  
Keyword(s):  
Plasma Membrane ◽  
Expression Pattern ◽  
Early Pregnancy ◽  
Organic Cation ◽  
Human Endometrium ◽  
Organic Cation Transporters ◽  
Differential Distribution ◽  
Monoamine Transporter ◽  
Cation Transporters ◽  
Cyclic Expression

scholarly journals Interaction Profiles of Central Nervous System Active Drugs at Human Organic Cation Transporters 1–3 and Human Plasma Membrane Monoamine Transporter

2021 ◽  
Vol 22 (23) ◽  
pp. 12995
Author(s):  
Thomas J. F. Angenoorth ◽  
Stevan Stankovic ◽  
Marco Niello ◽  
Marion Holy ◽  
Simon D. Brandt ◽  
...  
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Plasma Membrane ◽  
Human Plasma ◽  
Organic Cation ◽  
Hek293 Cells ◽  
Monoamine Transporters ◽  
Organic Cation Transporters ◽  
Monoamine Transporter ◽  
Cation Transporters

Many psychoactive compounds have been shown to primarily interact with high-affinity and low-capacity solute carrier 6 (SLC6) monoamine transporters for norepinephrine (NET; norepinephrine transporter), dopamine (DAT; dopamine transporter) and serotonin (SERT; serotonin transporter). Previous studies indicate an overlap between the inhibitory capacities of substances at SLC6 and SLC22 human organic cation transporters (SLC22A1–3; hOCT1–3) and the human plasma membrane monoamine transporter (SLC29A4; hPMAT), which can be classified as high-capacity, low-affinity monoamine transporters. However, interactions between central nervous system active substances, the OCTs, and the functionally-related PMAT have largely been understudied. Herein, we report data from 17 psychoactive substances interacting with the SLC6 monoamine transporters, concerning their potential to interact with the human OCT isoforms and hPMAT by utilizing radiotracer-based in vitro uptake inhibition assays at stably expressing human embryonic kidney 293 cells (HEK293) cells. Many compounds inhibit substrate uptake by hOCT1 and hOCT2 in the low micromolar range, whereas only a few substances interact with hOCT3 and hPMAT. Interestingly, methylphenidate and ketamine selectively interact with hOCT1 or hOCT2, respectively. Additionally, 3,4-methylenedioxymethamphetamine (MDMA) is a potent inhibitor of hOCT1 and 2 and hPMAT. Enantiospecific differences of R- and S-α-pyrrolidinovalerophenone (R- and S-α-PVP) and R- and S-citalopram and the effects of aromatic substituents are explored. Our results highlight the significance of investigating drug interactions with hOCTs and hPMAT, due to their role in regulating monoamine concentrations and xenobiotic clearance.

Histamine uptake mediated by plasma membrane monoamine transporter and organic cation transporters in rat mast cell lines

2019 ◽  
Vol 849 ◽  
pp. 75-83 ◽  
Author(s):  
Trivadila Slamet Soetanto ◽  
Shuang Liu ◽  
Muhammad Novrizal Abdi Sahid ◽  
Kensuke Toyama ◽  
Kazutaka Maeyama ◽  
...  
Keyword(s):  
Mast Cell ◽  
Plasma Membrane ◽  
Cell Lines ◽  
Organic Cation ◽  
Organic Cation Transporters ◽  
Monoamine Transporter ◽  
Histamine Uptake ◽  
Cation Transporters

scholarly journals Organic Cation Transporters in Human Physiology, Pharmacology, and Toxicology

2020 ◽  
Vol 21 (21) ◽  
pp. 7890 ◽  
Author(s):  
Sophia L. Samodelov ◽  
Gerd A. Kullak-Ublick ◽  
Zhibo Gai ◽  
Michele Visentin
Keyword(s):  
Plasma Membrane ◽  
Organic Cation ◽  
Chemical Exchange ◽  
Therapeutic Index ◽  
Organic Cation Transporter ◽  
Organic Cation Transporters ◽  
Waste Products ◽  
Carnitine Transporter ◽  
Cation Transporters ◽  
And Function

Individual cells and epithelia control the chemical exchange with the surrounding environment by the fine-tuned expression, localization, and function of an array of transmembrane proteins that dictate the selective permeability of the lipid bilayer to small molecules, as actual gatekeepers to the interface with the extracellular space. Among the variety of channels, transporters, and pumps that localize to cell membrane, organic cation transporters (OCTs) are considered to be extremely relevant in the transport across the plasma membrane of the majority of the endogenous substances and drugs that are positively charged near or at physiological pH. In humans, the following six organic cation transporters have been characterized in regards to their respective substrates, all belonging to the solute carrier 22 (SLC22) family: the organic cation transporters 1, 2, and 3 (OCT1–3); the organic cation/carnitine transporter novel 1 and 2 (OCTN1 and N2); and the organic cation transporter 6 (OCT6). OCTs are highly expressed on the plasma membrane of polarized epithelia, thus, playing a key role in intestinal absorption and renal reabsorption of nutrients (e.g., choline and carnitine), in the elimination of waste products (e.g., trimethylamine and trimethylamine N-oxide), and in the kinetic profile and therapeutic index of several drugs (e.g., metformin and platinum derivatives). As part of the Special Issue Physiology, Biochemistry, and Pharmacology of Transporters for Organic Cations, this article critically presents the physio-pathological, pharmacological, and toxicological roles of OCTs in the tissues in which they are primarily expressed.

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