Results 41 to 50 of about 55,182 (297)

Effects of Single Nucleotide Polymorphism Ala270Ser (rs316019) on the Function and Regulation of hOCT2

open access: yesBiomolecules, 2019
The human organic cation transporter 2 (hOCT2) is highly expressed in proximal tubules of the kidneys, where it plays an important role in the secretion of organic cations.
Dominik Frenzel   +6 more
doaj   +1 more source

Functional selectivity of GPCR-directed drug action through location bias. [PDF]

open access: yes, 2017
G-protein-coupled receptors (GPCRs) are increasingly recognized to operate from intracellular membranes as well as the plasma membrane. The β 2 -adrenergic GPCR can activate G s -linked cyclic AMP (G s -cAMP) signaling from endosomes.
Conti, Marco   +6 more
core   +3 more sources

Cysteine Accessibility in the Hydrophilic Cleft of Human Organic Cation Transporter 2 [PDF]

open access: yesJournal of Biological Chemistry, 2006
Organic cation transporters (OCTs) are involved in the renal elimination of many cationic drugs and toxins. A hypothetical three-dimensional structure of OCT2 based on a homology model that used the Escherichia coli glycerol 3-phosphate transporter as a template has been described (Zhang, X., Shirahatti, N. V., Mahadevan, D., and Wright, S. H. (2005) J.
Ryan M, Pelis   +3 more
openaire   +2 more sources

Functional expression of the organic cation/carnitine transporter 2 in rat astrocytes [PDF]

open access: yesJournal of Neurochemistry, 2006
AbstractIn this study, we sought to identify the transporters that mediate the uptake ofl‐carnitine and acetyl‐l‐carnitine in cultured rat cortical astrocytes.l‐[3H]carnitine and acetyl‐l‐[3H]carnitine uptake were both saturable, and mediated by a single Na+‐dependent transport system.
Masato, Inazu   +5 more
openaire   +2 more sources

Recent Advances in Molecular Pharmacology of the Histamine Systems: Organic Cation Transporters as a Histamine Transporter and Histamine Metabolism

open access: yesJournal of Pharmacological Sciences, 2006
.: Histamine is inactivated by the histamine-metabolizing enzyme histamine N-methyl-transferase (HNMT) in bronchus, kidney, and the central nervous system.
Ogasawara Masahito   +7 more
doaj   +1 more source

Pharmacokinetic Interaction between Metformin and Verapamil in Rats: Inhibition of the OCT2-Mediated Renal Excretion of Metformin by Verapamil

open access: yesPharmaceutics, 2020
The incidence of hypertension in diabetic patients has been increasing and contributing to the high mortality of diabetic patients. Recently, verapamil use was found to lower fasting blood glucose levels in diabetic patients, which led to a new ...
Seung Yon Han, Young Hee Choi
doaj   +1 more source

Multiple blood-brain barrier transport mechanisms limit bumetanide accumulation, and therapeutic potential, in the mammalian brain [PDF]

open access: yes, 2017
There is accumulating evidence that bumetanide, which has been used over decades as a potent loop diuretic, also exerts effects on brain disorders, including autism, neonatal seizures, and epilepsy, which are not related to its effects on the kidney but ...
Erker, Thomas   +7 more
core   +2 more sources

Molecular basis for stereoselective transport of fenoterol by the organic cation transporters 1 and 2

open access: yesBiochemical Pharmacology, 2022
Stereoselectivity is important in many pharmacological processes but its impact on drug membrane transport is scarcely understood. Recent studies showed strong stereoselective effects in the cellular uptake of fenoterol by the organic cation transporters OCT1 and OCT2.
Gebauer, Lukas   +4 more
openaire   +4 more sources

Inhibition of Human Drug Transporter Activities by the Pyrethroid Pesticides Allethrin and Tetramethrin. [PDF]

open access: yesPLoS ONE, 2017
Pyrethroids are widely-used chemical insecticides, to which humans are commonly exposed, and known to alter functional expression of drug metabolizing enzymes. Limited data have additionally suggested that drug transporters, that constitute key-actors of
Lisa Chedik   +7 more
doaj   +1 more source

Corticosterone Regulates Both Naturally Occurring and Cocaine‐Induced Dopamine Signaling by Selectively Decreasing Dopamine Uptake [PDF]

open access: yes, 2017
Stressful and aversive events promote maladaptive reward‐seeking behaviors such as drug addiction by acting, in part, on the mesolimbic dopamine system. Using animal models, data from our laboratory and others show that stress and cocaine can interact to
Baker, David A.   +9 more
core   +2 more sources

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