JNJ-37822681 dihydrochloride_product_DataBase

Bioactivity	JNJ-37822681 dihydrochloride is a potent, specific, centrally active, fast-dissociating dopamine D2 receptor antagonist with a moderate binding affinity for the dopamine D2L receptor (Ki =158 nM), which has potential for the treatment of schizophrenia and bipolar disorder[1][2].
Target	Ki: 158 nM (D2)
In Vivo	JNJ-37822681 (0.0025-40 mg/kg; i.h.; once) blocks D2 receptors in rat brain at relatively low doses with an ED50 value of 0.39 mg/kg and has effective in animal models of psychosis[2].JNJ-37822681 (0.01-2.5 mg/kg; i.h.; once) induces minimal prolactin release at the lowest doses required for central D2 receptor blockade[2]. Animal Model:
Name	JNJ-37822681 dihydrochloride
CAS	2108806-02-4
Formula	C17H19Cl2F5N4
Molar Mass	445.26
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Reference	[1]. Langlois X, et, al. Pharmacology of JNJ-37822681, a specific and fast-dissociating D2 antagonist for the treatment of schizophrenia. J Pharmacol Exp Ther. 2012 Jul;342(1):91-105. [2]. de Waal EJ, et, al. Differential responses to JNJ-37822681, a specific and fast dissociating dopamine D2 receptor antagonist, in cynomolgus monkey and Sprague-Dawley rat general toxicology studies: clinical observations, prolactin levels, mammary histopat

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