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Related Concept Videos

Carrier-Mediated Transport01:06

Carrier-Mediated Transport

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Carrier-mediated transport is a pivotal process in drug absorption, particularly for lipid-insoluble drugs, and encompasses facilitated diffusion and active transport. Facilitated diffusion allows drugs to move along their concentration gradient without energy expenditure, while active transport utilizes ATP to drive drug movement against this gradient.
Active transport involves two types of membrane-spanning transporters: uptake and efflux. Uptake transporters are expressed in the small...
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Transcellular Transport of Solutes01:23

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Transcellular transport of solutes is the movement of substances like monosaccharides and amino acids through polarized cells. This transport mechanism is primarily seen in epithelial and endothelial cells aided by membrane transport proteins such as channels and transporters. The tight junctions between these cells confine the membrane proteins to the two sides of the cell. The epithelial cells have distinct apical and basolateral domains. In contrast, the endothelial cells show the luminal...
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Active Transport01:14

Active Transport

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Active transport is a critical biological process that allows cells to move solutes against an electrochemical gradient. This process requires direct energy input and is characterized by its selectivity, saturability, and susceptibility to competitive inhibition.
Primary active transporters, like Na+, K+ and -ATPase, directly utilize ATP to move ions across the membrane. These transporters play significant roles in various physiological processes. For instance, Na+, K+ and -ATPase maintain...
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Secondary Active Transport01:55

Secondary Active Transport

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One example of how cells use the energy contained in electrochemical gradients is demonstrated by glucose transport into cells. The ion vital to this process is sodium (Na+), which is typically present in higher concentrations extracellularly than in the cytosol. Such a concentration difference is due, in part, to the action of an enzyme “pump” embedded in the cellular membrane that actively expels Na+ from a cell. Importantly, as this pump contributes to the high concentration of...
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Secondary Active Transport01:32

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One example of how cells use the energy contained in electrochemical gradients is demonstrated by glucose transport into cells. The ion vital to this process is sodium (Na+), which is typically present in higher concentrations extracellularly than in the cytosol. Such a concentration difference is due, in part, to the action of an enzyme "pump" embedded in the cellular membrane that actively expels Na+ from a cell. Importantly, as this pump contributes to the high concentration of...
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Membrane Transporters01:31

Membrane Transporters

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Transporters are essential membrane transport proteins with functions related to cell nutrition, homeostasis, communication, etc. Approximately 7% of all genes in the human genome code for transporters or transporter-related proteins.
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Related Experiment Video

Updated: Nov 6, 2025

Study of the Functions and Activities of Neuronal K-Cl Co-Transporter KCC2 Using Western Blotting
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Organic Cation Transporter Expression and Function in the CNS.

Douglas H Sweet1

  • 1Department of Pharmaceutics, School of Pharmacy, Virginia Commonwealth University, Richmond, VA, USA. dsweet@vcu.edu.

Handbook of Experimental Pharmacology
|May 8, 2021
PubMed
Summary
This summary is machine-generated.

Organic cation transporters within the Solute Carrier (SLC) superfamily are crucial for maintaining central nervous system (CNS) homeostasis and function. Understanding their roles in CNS permeation and clearance is key for developing new therapeutics for neurological disorders.

Keywords:
Blood–brain barrierBlood–cerebrospinal fluid barrierBrain capillariesChoroid plexusOlfactory mucosaSolute carrier

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Area of Science:

  • Neuroscience
  • Pharmacology
  • Molecular Biology

Background:

  • The blood-brain barrier (BBB) and blood-cerebrospinal fluid barrier (BCSFB) tightly regulate CNS composition.
  • Various CNS cell types, including astrocytes and microglia, actively maintain the CNS environment.
  • Transporter proteins are essential for the function of these barriers and cells.

Purpose of the Study:

  • To highlight organic cation transporters from the Solute Carrier (SLC) superfamily expressed in the CNS.
  • To provide an overview of their identification, mechanisms, expression, and interactions.
  • To examine their role in CNS homeostasis and potential therapeutic applications.

Main Methods:

  • Review of literature on SLC transporters in the CNS.
  • Analysis of transporter substrates, expression profiles, and loss-of-function studies.
  • Examination of interactions with neurotransmitters and psychotropic drugs.

Main Results:

  • SLC transporters, particularly SLC22, SLC29, and SLC47 families, are critical for CNS permeation and clearance.
  • These transporters interact with neurotransmitters, antidepressants, and drugs of abuse.
  • Loss-of-function studies reveal their impact on CNS homeostasis and behavior.

Conclusions:

  • Organic cation transporters significantly influence CNS permeation, clearance, and overall homeostasis.
  • Understanding these transporters is vital for developing novel therapeutic strategies for CNS disorders.
  • Further research into SLC transporters will advance our knowledge of neuronal signaling and behavior.