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JNJ-18038683

Catalog No. T11720 CAS 851376-05-1

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.

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JNJ-18038683, CAS 851376-05-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 33.00
2 mg	In stock	$ 46.00
5 mg	In stock	$ 76.00
10 mg	In stock	$ 139.00
25 mg	In stock	$ 289.00
50 mg	In stock	$ 455.00
100 mg	In stock	$ 672.00
1 mL * 10 mM (in DMSO)	In stock	$ 84.00

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Purity: 98.31%

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Description	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.
Targets&IC50	5-HT7 receptor (human):8.2(pKi, in HEK293 cells ), 5-HT7 receptor (rat):8.19(pKi, in HEK293 cells )
In vitro	JNJ-18038683 produces a concentration-dependent decrease of 5-HT (100 nM)-stimulated adenylyl cyclase. The pKB values determined for JNJ-18038683 are in good agreement with the corresponding Ki values determined from [3H]5-CT binding studies.JNJ-18038683 displaced, with high affinity, specific [3H]5-CT binding sites from rat and human 5-HT7 receptor express in HEK293 cells (pKi=8.19±0.02 and 8.20±0.01, respectively). Similar values are obtained on the native 5-HT7 in membranes from rat thalamus (pKi=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.
In vivo	JNJ-18038683 dose-dependently reduces REM sleep, particularly within the first 4 hours post-administration, with a significant decrease observed from a dosage of 1 mg/kg (P<0.05). Furthermore, it extends REM sleep latency, showing a significant prolongation at the highest dose tested (10 mg/kg; P<0.05), indicating that these effects are specific to the REM sleep state. An additional study evaluated the impact of administering JNJ-18038683 daily for 7 days (1 mg/kg s.c. per day) on EEG sleep patterns in rats, focusing on REM sleep both during treatment and after its cessation. Initial treatment significantly reduced REM sleep duration in the first 8 hours and increased REM latency, which remained elevated throughout the 7-day treatment but returned to normal after treatment stopped. While the reduction in REM sleep persisted during the treatment period, a rebound increase in REM sleep occurred upon treatment discontinuation. Neither the latency nor the total time of NREM sleep was impacted over the treatment course.

Molecular Weight	529.97
Formula	C26H28ClN3O7
CAS No.	851376-05-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 200 mg/mL (358.51 mM), Sonification is recommended.

References and Literature

1. 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.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Neurodegenerative Disease Compound Library Inhibitor Library Anti-Cancer Drug Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library GPCR Compound Library Bioactive Compounds Library Max Anti-Cancer Compound Library Neuronal Signaling Compound Library Angiogenesis related Compound Library

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Keywords

JNJ-18038683 851376-05-1 GPCR/G Protein Neuroscience 5-HT Receptor Inhibitor 5-hydroxytryptamine Receptor inhibit Serotonin Receptor JNJ18038683 JNJ 18038683 inhibitor

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