The Transport of Choline

  title={The Transport of Choline},
  author={Paul R. Lockman and David D. Allen},
  journal={Drug Development and Industrial Pharmacy},
  pages={749 - 771}
  • P. Lockman, D. D. Allen
  • Published 1 January 2002
  • Biology, Chemistry
  • Drug Development and Industrial Pharmacy
ABSTRACT Choline has many physiological functions throughout the body that are dependent on its available local supply. However, since choline is a charged hydrophilic cation, transport mechanisms are required for it to cross biological membranes. Choline transport is required for cellular membrane construction and is the rate-limiting step for acetylcholine production. Transport mechanisms include: (1) sodium-dependent high-affinity uptake mechanism in synaptosomes, (2) sodium-independent low… 
Cation Transport Specificity at the Blood–Brain Barrier
The molecular family of the blood–brain barrier (BBB) choline transporter may be elucidated in vitro by its interaction with physiologic thiamine levels, and two cationic transporters at the BBB may be responsible forThiamine brain uptake.
Inhibition of choline uptake by N-cyclohexylcholine, a high affinity ligand for the choline transporter at the blood–brain barrier
Five novel N-cycloalkyl derivatives of choline showed promising inhibition properties and a cyclohexyl moiety substituting one of the methyl groups attached to the cationic nitrogen in choline helped improve affinity for this transporter.
Impaired trafficking of choline transporter-like protein-1 at plasma membrane and inhibition of choline transport in THP-1 monocyte-derived macrophages.
Investigating choline transport processes and regulation of choline transporter-like protein-1 (CTL1) in human THP-1 monocytic cells and phorbol myristate 13-acetate (PMA)-differentiated macrophages reveals that CTL1 is the most plausible candidate that possesses the described kinetic and inhibitory properties.
Choline uptake in human intestinal Caco-2 cells is carrier-mediated.
Results indicate the presence of a carrier-mediated transport system for choline in Caco-2 cells, the substrate specificity of this carrier is unlike that seen in the rat intestinal epithelium, and the human transport protein is distinct from those for TEA and NMN.
The choline transporter-like family SLC44: properties and roles in human diseases.
Molecular and functional characterization of an Na+‐independent choline transporter in rat astrocytes
It is concluded that rat astrocytes express an intermediate‐affinity Na+‐independent choline transport system that seems to occur through a CTL1 and is responsible for the uptake of choline and organic cations in these cells.
Active Transport of High-Affinity Choline and Nicotine Analogs into the Central Nervous System by the Blood-Brain Barrier Choline Transporter
It is hypothesized that the N-n-octyl group on the pyridinium nitrogen of NONI facilitates brain entry via the BBB choline transporter, and may have utility as a smoking cessation agent.


Choline mustard: an irreversible ligand for use in studies of choline transport mechanisms at the cholinergic nerve terminal.
  • R. J. Rylett
  • Biology, Chemistry
    Canadian journal of physiology and pharmacology
  • 1986
This mustard analogue did not inhibit synaptosomal uptake of 5-hydroxytryptamine, noradrenaline, or gamma-aminobutyric acid, thereby confirming further the specificity of this compound for the choline carrier.
Novel Choline Transport Characteristics in Caco-2 Cells
Choline transport across Caco-2 cells is demonstrated to be active and both pH- and Ca2+-dependent and has unique characteristics when compared to traditional choline transport models.
Choline transport into rat liver mitochondria. Characterization and kinetics of a specific transporter.
Characteristics of Choline Transport Across the Blood-Brain Barrier in Mice: Correlation with In Vitro Data
These in situ (in vivo) results corresponded well to the in vitro results and suggest that the choline transporter at the BBB is a member of the organic cation transporter (OCT) family.
Functional characterization of the human high-affinity choline transporter.
The molecular cloning and functional characterization of the human high-affinity choline transporter (hCHT1) is reported, which exhibits significant homology with known members of the Na(+)-dependent glucose transporter family, but not withMembers of the neurotransmitter transporter family.
Pharmacological characteristics of choline transport system in mouse cerebral cortical neurons in primary culture.
The present results strongly suggest that the primary cultured neurons used in this study possess a sodium- and energy-dependent high-affinity choline uptake system as well as a synthesizing system for acetylcholine.
Inhibition of the rat blood–brain barrier choline transporter by manganese chloride
The results suggest that choline uptake into the CNS can be inhibited by divalent cationic metals and monovalent cations, and the choline transporter may be a means by which manganese enters the brain.
Blood–brain barrier choline transport in the senescent rat