JNJ-18038683 ( JNJ18038683 )

Catalog No. M16185 CAS No. 851376-05-1

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Datasheet

HNMR

HPLC

MSDS

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Product Name

JNJ-18038683
Note

Research use only, not for human use.
Brief Description

JNJ-18038683 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; 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.
Description

JNJ-18038683 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; 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; 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; prolongs rapid eye movement (REM) sleep and decreases REM duration induced by citalopram in vivo.Depression Phase 2 Clinical
Synonyms

JNJ18038683
Pathway

GPCR/G Protein
Target

Histamine Receptor
Recptor

Histamine Receptor
Research Area

Neurological Disease
Indication

Depression

CAS Number

851376-05-1
Formula Weight

529.97
Molecular Formula

C26H28ClN3O7
Purity

>98% (HPLC)
Solubility

——
SMILES

C1CNCCC2=C1C(=NN2CC3=CC=CC=C3)C4=CC=C(C=C4)Cl.C(C(=O)O)C(CC(=O)O)(C(=O)O)O
Chemical Name

3-(4-chlorophenyl)-1,4,5,6,7,8-hexahydro-1-(phenylmethyl)pyrazolo[3,4-d]azepine 2-hydroxy-1,2,3-propanetricarboxylate

1. Bonaventure P, et al. J Pharmacol Exp Ther. 2012 Aug;342(2):429-40.
2. Shelton J, et al. Front Behav Neurosci. 2015 Jan 15;8:453.

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