JNJ-18038683, inhibitor

JNJ-18038683

Cat. Num. AAA5753349

• Purity: 98.00%
• Synonyms: JNJ-18038683; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: DMSO: 200mg/mL (377.38mM) Need ultrasonic; (<1mg/ml refers to the product slightly soluble or insoluble)
• Formula: C26H28ClN3O7
• SMILES: ClC1=CC=C(C2=NN(CC3=CC=CC=C3)C4=C2CCNCC4)C=C1.O=C(CC(C(O)=O)(O)CC(O)=O)O
• CAS Number: 851376-05-1
• Target & IC50: Rat 5-HT7 Receptor: ic50 8.19 (pKi, in HEK293 cells); Human 5-HT7 Receptor: ic50 8.2 (pKi, in HEK293 cells)
• In Vitro: 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 1mg/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 (10mg/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 (1mg/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
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Structure

Related Product Information for JNJ-18038683, inhibitor

JNJ-18038683 is a 5-Hydroxytryptamine Type 7 (5-HT7) receptor antagonist, with pKis of 8.19, 8.20 for rat and human 5-HT7 in HEK293 cells, respectively.

Product Categories/Family for JNJ-18038683, inhibitor

GPCR/G Protein; Neuroscience

References

Bonaventure P, et al. Translational evaluation of JNJ-18038683, a 5-hydroxytryptamine type 7 receptor antagonist, on rapid eye movement sleep and in major depressive disorder. J Pharmacol Exp Ther. 2012 Aug;342(2):429-40.