JNJ-18038683

JNJ-18038683 is a 5-Hydroxytryptamine Type 7 ( 5-HT 7 ) receptor antagonist, with pK i s of 8.19, 8.20 for rat and human 5-HT 7 in HEK293 cells, respectively. In Vitro JNJ-18038683 displaced, with high affinity, specific [ 3 H]5-CT binding sites from rat and human 5-HT 7 receptor express in HEK293 cells (pK i =8.19±0.02 and 8.20±0.01, respectively). Similar values are obtained on the native 5-HT 7 in membranes from rat thalamus (pK i =8.50±0.20). Hill slope values are close to unity, suggesting one-site competitive binding. Antagonist potency of JNJ-18038683 is determined by the measurement of adenylate cyclase activity in HEK293 cells expressing the human or rat 5-HT 7 receptor. 5-HT stimulates adenylyl cyclase activity in rat and human 5-HT 7 /HEK293 cells with a pEC 50 of 8.09 and 8.12, respectively. JNJ-18038683 produces a concentration-dependent decrease of 5-HT (100 nM)-stimulated adenylyl cyclase. The pK B values determined for JNJ-18038683 are in good agreement with the corresponding K i values determined from [ 3 H]5-CT binding studies. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo JNJ-18038683 dose-dependently suppresses REM sleep mainly during the first 4 h after the treatment. The duration of REM sleep is significantly decreased from the dose of 1 mg/kg onward (P IC50& Target:Rat 5-HT 7 Receptor 8.19 (pKi, in HEK293 cells ) Human 5-HT 7 Receptor 8.20 (pKi, in HEK293 cells )

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