Oleoyl-L-carnitine inhibits glycine transport by GlyT2.

ABSTRACT:

Background and purpose

Concentrations of extracellular glycine in the CNS are regulated by two Na(+)/Cl(-) -dependent glycine transporters, GlyT1 and GlyT2. Selective inhibitors of GlyT1 have been developed for the treatment of schizophrenia, whilst selective inhibitors of GlyT2 are analgesic in animal models of pain. We have assessed a series of endogenous lipids as inhibitors of GlyT1 and GlyT2.

Experimental approach

Human GlyT1 and GlyT2 were expressed in Xenopus laevis oocytes, and the inhibitory actions of a series of acylcarnitines on glycine transport were measured using electrophysiological techniques.

Key results

Oleoyl-L-carnitine inhibited glycine transport by GlyT2, with an IC(50) of 340 nM, which is 15-fold more potent than the previously identified lipid

SUBMITTER: Carland JE 

PROVIDER: S-EPMC3631378 | biostudies-literature | 2013 Feb

REPOSITORIES: biostudies-literature