High-affinity choline transporter (CHT1) (CHT1)

The high-affinity choline transporter (CHT1) is an integral membrane protein responsible for the reuptake of choline into presynaptic terminals of cholinergic neurons, a critical and rate-limiting step for acetylcholine synthesis[2][3][4][10]. CHT1 is a **Na(+)- and Cl(-)-dependent symporter** and a member of the solute carrier family 5 (SLC5), with a 13-transmembrane domain structure[2][8][10]. By mediating high-affinity choline uptake, it maintains the supply of acetylcholine required for synaptic transmission in both the central and peripheral nervous systems[3][4][6][7]. Mutations in the gene encoding CHT1 (SLC5A7) are linked to hereditary motor neuropathies and have implications in neurological and cognitive disorders[10]. Its activity is selectively inhibited by compounds such as hemicholinium-3 and ML352, while compounds like coluracetam can enhance its function[5][10]. This transporter is a validated therapeutic target due to its essential role in cholinergic neurotransmission and disease association.

Other names

Solute carrier family 5 member 7SLC5A7Choline transporterCHThCHTHMN7ACMS20

Competitive inhibition of choline binding and transport (e.g., by HC-3, ML352); Enhancement of choline uptake and acetylcholine synthesis (by coluracetam)