Transport of gabapentin by LAT1 (SLC7A5)

Quantitative Targeted Proteomics for Membrane Transporter Proteins: Method and Application

“…Recently, the human cerebral microvascular endothelial cell line hCMEC/D3 was established and found to retain most of the morphological and functional characteristics of brain endothelial cells. The cell line is used as an in vitro model to investigate the function and their modulation in human BBB by many laboratories (68)(69)(70)(71). A series of investigations demonstrated that the expression pattern of ATP-binding cassette transporter messenger RNAs in hCMEC/D3 cells is, at least qualitatively, similar to that of human brain microvessels (72,73).…”

Blood–brain barrier endogenous transporters as therapeutic targets: a new model for small molecule CNS drug discovery

“…Once in brain, the L-DOPA is decarboxylated to dopamine, the pharmacologically active form of the drug. Gabapentin, a g-amino acid with a cyclic structure that mimics that of an a-amino acid, is a water-soluble drug active in the CNS, because gabapentin is transported into brain via the endogenous LAT1 on the BBB [6]. Melphalan, an alkylating chemotherapeutic agent, is active in brain cancer, because this form of phenylalanine mustard crosses the BBB via transport on the BBB LNAA transporter [7].…”

The Physiology, Pathology, and Pharmacology of Voltage-Gated Calcium Channels and Their Future Therapeutic Potential

“…Role of Amino Acid Transporters in the Action of Gabapentin. Pregabalin and gabapentin do not inhibit the transport of GABA in vitro However, both gabapentin and pregabalin are zwitterions at neutral pH and use the large neutral amino acid transporter "system L" for uptake across cell membranes (Belliotti et al, 2005;Su et al, 2005;Dickens et al, 2013).…”