JNJ-37822681 dihydrochloride (C09-1141-014)

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 disorderIn VivoJNJ-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:SolidIC50& Target:Ki: 158 nM (D 2 ). Specification: 0.99 Molecular Formula: C17H19Cl2F5N4 Molecular Weight: 445.26 PubChem CID: 91826482 Isomeric SMILES: C1CN(CCC1NC2=NN=C(C=C2)C(F)(F)F)CC3=CC(=C(C=C3)F)F.Cl.Cl