JNJ-18038683 free base is a potent, selective 5-HT7 receptor antagonist with pKi of 8.19 and 8.20 for rat and human 5-HT7 in cell-based assays.
JNJ-18038683 decreases 5-HT (100 nM)-stimulated adenylyl cyclase in rat and human 5-HT7/HEK293 cells with pKb of 8.01 and 7.99, respectively.
JNJ-18038683 shows 10-fold selectivity over h5-HT6 receptor, 15-fold selectivity over rat adrenergic α1 receptor, 14- to 25-fold selectivity over the h5-HT2 receptor subtypes, and 20-fold selectivity over h5-HT1B receptor.
JNJ-18038683 prolongs rapid eye movement (REM) sleep and decreases REM duration induced by citalopram in vivo.
