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JNJ-18038683 free base

Names

[ CAS No. ]:
851373-91-6

[ Name ]:
JNJ-18038683 free base

[Synonym ]:
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

Biological Activity

[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

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
547.6±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C20H20ClN3

[ Molecular Weight ]:
337.846

[ Flash Point ]:
285.0±30.1 °C

[ Exact Mass ]:
337.134583

[ LogP ]:
3.84

[ Vapour Pressure ]:
0.0±1.5 mmHg at 25°C

[ Index of Refraction ]:
1.656

Related Compounds