| Identification | Back Directory | [Name]
JNJ-37822681 dihydrochloride | [CAS]
2108806-02-4 | [Synonyms]
Dopamine Receptor,JNJ-37822681,d-amphetamine,phencyclidine,bipolar disorder,JNJ 37822681,schizophrenia,JNJ37822681,JNJ37822681 dihydrochloride,apomorphine,JNJ 37822681 dihydrochloride,Inhibitor,inhibit | [Molecular Formula]
C??H??Cl?F?N? | [MDL Number]
MFCD22580411 | [MOL File]
2108806-02-4.mol | [Molecular Weight]
408.8 |
| Hazard Information | Back Directory | [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 |
|
| Company Name: |
MedChemExpress
|
| Tel: |
021-58955995 |
| Website: |
www.medchemexpress.com |
|