Cariprazine HCl

Description: Cariprazine hydrochloride (formerly known as MP-214 and RGH-188) is a novel and potent antipsychotic drug candidate that is in late-stage clinical development for the treatment of schizophrenia, as well as for bipolar disorder (manic/mixed and depressive episodes), and as an adjunctive agent for the treatment of major depressive disorder. Cariprazine is a dopamine D3-preferring D3/D2 receptor partial agonist that exhibits high affinity for the D3 receptor with Ki of 0.085 nM and D2 receptor with Ki of 0.49 nM, and moderate affinity for the 5-HT1A receptor with Ki of 2.6 nM. Cariprazine stimulates inositol phosphate (IP) formation with a high potency (pEC50 8.5) with relatively low efficacy (Emax 30%).

References: J Pharmacol Exp Ther. 2010 Apr; 333(1):328-40.

Related CAS#: 839712-12-8 (free base)