SB-568849 is a selective SLC-1 antagonist (pKi: 7.7) as determined in radioligand binding displacement assays. Coincubation of tissue with SB-568849 (1 μM) for 45 min fully inhibits the MCH induced increase in corticotropin-releasing factor (CRF) release to basal levels without causing any effect on its own [2].

SB-568849 has good receptor affinity and selectivity. SB-568849 displays >30-fold selectivity over a wide range of monoamine receptors and is an antagonist in the FLIPR assay with a pKb of 7.7. SB-568849 retains affinity, demonstrates greater in vivo stability (CLb=16 mL/min/kg), and shows an acceptable brain-blood ratio of 1 [3].