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.
Påhlman et al (2012) Immunosuppressive properties of a series of novel inhibitors of the monocarboxylate transporter MCT-1. Transpl.Int. 26 22 PMID:23137339 |Thiesen et al (2015) In vitro and in vivo evidence for active brain uptake of the GHB analog HOCPCA by the monocarboxylate transporter subtype 1. J.Pharmacol.Exp.Ther. 354 166 PMID:25986445