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JNJ-18038683

CAS No. : 851376-05-1

MCE 站：JNJ-18038683

产品活性：JNJ-18038683 是 5-羟色胺受体 7 (5-HT₇) 的拮抗剂，HEK293 细胞中检测出其对大鼠和人类 5-羟色胺受体 7 的 pK_i 值分别为 8.19，8.20。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：5-HT Receptor

In Vitro: JNJ-18038683 displaced, with high affinity, specific [³H]5-CT binding sites from rat and human 5-HT₇ 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-HT₇ 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-HT₇ receptor. 5-HT stimulates adenylyl cyclase activity in rat and human 5-HT₇/HEK293 cells with a pEC₅₀ 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 [³H]5-CT binding studies.

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<0.05) during the first 4 h after oral administration. Concomitantly, the REM sleep latency tends to be prolonged in a dose-related manner with a significant increase in REM latency occurring only at the highest dose tested (10 mg/kg; P<0.05). These alterations in REM sleep seem to be state-specific. A separate study is conducted to determine whether repeated administration of JNJ-18038683 for 7 days would result in an adaptation of the EEG sleep response in particular on REM sleep in rats during the course of the treatment and after its discontinuation. JNJ-18038683 is administered for 7 consecutive days (1 mg/kg s.c. per day) at 2 h into the light phase. On the first day of treatment, JNJ-18038683 produces a significant decrease in the time spent in REM sleep during the first 8 h after the injection and a prolongation of the REM sleep latency. The REM sleep latency is increased during the 7-day repeated treatment and is normalized on the first recovery day after cessation of treatment. The significant decrease in REM sleep time is maintained during the 7-day repeated treatment, with a rebound occurring on the first recovery day after treatment discontinuation. The NREM sleep latency and the total NREM sleep time are not affected during the entire treatment.

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