The saturated analog of kainic acid. Reduction of the isopropylene side-chain destroys the affinity to binding sites. It enhances the antitumor activity of doxorubicin presumably acting as a glutamate transporter inhibitor.

Dihydrokainic acid (DHK) is an inhibitor of excitatory amino acid transporter 2 (EAAT2, Ki = 23 µM for glutamate uptake by COS cells expressing EAAT2). It is selective for EAAT2 over EAAT1 and EAAT3 (Ki = >3 mM for both). DHK microinfusion (5 nmol) into the rat infralimbic cortex reduces the time spent immobile in...

Description: EAAT2(GLT1)-selective non-transportable inhibitor of L-glutamate and L-aspartate uptake. Target: Others. Smiles: CC(C)[C@H]1CN[C@@H]([C@H]1CC(O)=O)C(O)=O