JNJ-37822681 dihydrochloride is a potent, specific, centrally active, fast-dissociating dopamine D 2 receptor antagonist with a moderate binding affinity for the dopamine D 2L receptor ( K i =158 nM), which has potential for the treatment of schizophrenia and bipolar disorder In Vivo JNJ-37822681 (0.0025-40 mg/kg; i.h.; once) blocks D 2 receptors in rat brain at relatively low doses with an ED 50 value of 0.39 mg/kg and has effective in animal models of psychosis. JNJ-37822681 (0.01-2.5 mg/kg; i.h.; once) induces minimal prolactin release at the lowest doses required for central D 2 receptor blockade. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female Sprague-Dawley rats with apomorphine-induced, d-amphetamine-induced, or phencyclidine-inducedDosage: 0.0025-40 mg/kg Administration: Subcutaneous injection; once Result: Inhibited of D-amphetamine-induced hyperlocomotion with an ED 50 value of 1.0 mg/kg. Inhibited of apomorphine-induced stereotypy with an ED 50 value of 0.19 mg/kg. Inhibited of phencyclidine-induced hyperlocomotion with an ED 50 value of 4.7 mg/kg. Animal Model: Female Sprague-Dawley ratsDosage: 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. Form:Solid IC50& Target:Ki: 158 nM (D 2 )
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JNJ-37822681 dihydrochloride
CAS number：2108806-02-4 molecular formula：C17H19Cl2F5N4
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| Chinese alias | JNJ-37822681 二盐酸盐 | ||
| English alias | HY-111066A | N-{1-[(3,4-difluorophenyl)methyl]piperidin-4-yl}-6-(trifluoromethyl)pyridazin-3-amine dihydrochloride | 3-Pyridazinamine, N-(1-((3,4-difluorophenyl)methyl)-4-piperidinyl)-6-(trifluoromethyl)-, hydrochloride (1:2) | E98972 | JNJ-37822681 dihyd | ||
| CAS number | 2108806-02-4 | molecular formula | C17H19Cl2F5N4 |
| molecular weight | 445.26 g/mol | Exact mass | ≥99% |
| PSA | 41.100 Ų | logp | - |
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