RTI-13951-33 is a potent, selective, brain-penetrant agonist of the orphan receptor GPR88 with EC50 of 25 nM in in vitro cAMP functional assay.
RTI-13951-33 displays no significant off-target activity at 38 GPCRs, ion channels, and neurotransmitter transporters.
RTI-13951-33 exhibits enhanced aqueous solubility compared to (1R,2R)-2-PCCA (2) and had favorable pharmacokinetic properties for behavioral assessment.
RTI-13951-33 significantly reduces alcohol self-administration and alcohol intake in a dose-dependent manner without effects on locomotion and sucrose self-administration in rats
