ChemicalBook CAS DataBase List 2108806-02-4

2108806-02-4

Name	JNJ-37822681 dihydrochloride
CAS	2108806-02-4
Molecular Formula	C??H??Cl?F?N?
MDL Number	MFCD22580411
Molecular Weight	408.8
MOL File	2108806-02-4.mol

Chemical Properties

storage temp.	Store at -20°C
solubility	DMSO: Soluble; Water: Soluble
form	A solid
color	White to off-white

Hazard Information

Uses

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].

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:	Female Sprague-Dawley rats with apomorphine-induced, d-amphetamine-induced, or phencyclidine-induced^[2]
Dosage:	0.0025-40 mg/kg
Administration:	Subcutaneous injection; once
Result:	Inhibited of D-amphetamine-induced hyperlocomotion with an ED₅₀ value of 1.0 mg/kg. Inhibited of apomorphine-induced stereotypy with an ED₅₀ value of 0.19 mg/kg. Inhibited of phencyclidine-induced hyperlocomotion with an ED₅₀ value of 4.7 mg/kg.

Animal Model:	Female Sprague-Dawley rats^[2]
Dosage:	0.01, 0.02, 0.04, 0.08, 0.16, 0.31, 0.63, 1.25, and 2.5 mg/kg
Administration:	Subcutaneous injection; once
Result:	Increased prolactin release in a dose-dependent manner.

References

[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. DOI:10.1124/jpet.111.190702
[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 DOI:10.1002/jat.2916

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