For research use only. Not for therapeutic Use.
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].
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].
| Catalog Number | I018499 |
| CAS Number | 2108806-02-4 |
| Synonyms | N-[1-[(3,4-difluorophenyl)methyl]piperidin-4-yl]-6-(trifluoromethyl)pyridazin-3-amine;dihydrochloride |
| Molecular Formula | C17H19Cl2F5N4 |
| Purity | ≥95% |
| InChI | InChI=1S/C17H17F5N4.2ClH/c18-13-2-1-11(9-14(13)19)10-26-7-5-12(6-8-26)23-16-4-3-15(24-25-16)17(20,21)22;;/h1-4,9,12H,5-8,10H2,(H,23,25);2*1H |
| InChIKey | UOLHGUUKFNZTNS-UHFFFAOYSA-N |
| SMILES | C1CN(CCC1NC2=NN=C(C=C2)C(F)(F)F)CC3=CC(=C(C=C3)F)F.Cl.Cl |
| 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 |
