851373-91-6

851373-91-6 structure

Name: JNJ-18038683 free base
Chemical Name: JNJ-18038683 FREE BASE
CAS Number: 851373-91-6
Molecular Formula: C₂₀H₂₀ClN₃
Molecular Weight: 337.846
Create Date: 2020-01-14 21:39:44
Modify Date: 2024-04-01 17:10:41
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.

Name	JNJ-18038683 FREE BASE
Synonyms	Pyrazolo[3,4-d]azepine, 3-(4-chlorophenyl)-1,4,5,6,7,8-hexahydro-1-(phenylmethyl)- 1-Benzyl-3-(4-chlorophenyl)-1,4,5,6,7,8-hexahydropyrazolo[3,4-d]azepine JNJ-18038683 FREE BASE

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.
References	References 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. View Related Products by Target Histamine Receptor