TABLE 5

Inhibitors of glycine transporters

InhibitorKiApplicationBinding Site Model
GLYT1GLYT2
nM
GLYT1 inhibitors
    Sarcosinea,b55,000>100,000Pharmacological tool
    NFPS (ALX 5407)c3>1000Pharmacological tool
    ORG 24598b32>100,000Pharmacological tool
    LY2365109d15.8>30,000Pharmacological tool
GLY2 inhibitors
    ORG 25543e>10016Pharmacological tool
    N-Arachidonylglycinef>100,0003000Pharmacological toolEdington et al., 2009
  • NFPS, N-[3-(4′-fluorophenyl)-3-(4′-phenylphenoxy)propyl]sarcosine.

  • a Synthetic substrate.

  • b Mallorga et al., 2003; rat GLYTs.

  • c Atkinson et al., 2001.

  • d Perry et al., 2008a.

  • e Caulfield et al., 2001.

  • f Wiles et al., 2006.