didesmethyl cariprazine

Didesmethyl cariprazine, a metabolite of Cariprazine, is the major cyclic active part. Didesmethyl cariprazine has a long half-life of 1-3 weeks. Cariprazine is a potent D3 preference D3/D2 receptor partial agonist of dopamine for the treatment of schizophrenia, bipolar mania, and depression, with a high affinity for d3 and d2 receptors and a moderate affinity for 5-HT 1A receptors.

Didesmethyl cariprazine-d8 is a deuterium-labeled version of Didesmethyl cariprazine, an orally active metabolite of Cariprazine capable of crossing the blood-brain barrier. It acts as a partial agonist at D2 and D3 receptors and a full agonist at the 5-HT1A receptor, while serving as an antagonist for the human 5-HT2B receptor. Its binding affinities are Ki: 1.41 nM for human D2L, 0.056 nM for human D3, 1.7 nM for human 5-HT1A, and 0.52 nM for human 5-HT2B. Didesmethyl cariprazine also dose-dependently suppresses the spontaneous activity of midbrain dopaminergic neurons in rats.