HOCPCA is an effective and selective ligand for the GHB binding sites that acts by binding with 27 times better affinity than GHB itself and crossing the blood-brain barrier in vitro and in vivo.
Monocarboxylate transporter (MCT1) inhibitor (pKi = 7.6. Exhibits approximately 10-fold selectivity for MCT1 over MCT2 and no significant activity against MCT3 or 4. Inhibits graft versus host response and prolongs cardiac graft survival in a rat model. Immunosuppressant. Also inhibits brain penetration of GHB analog HOCPCA.