Didesmethyl cariprazine

Didesmethyl cariprazine is an orally active, BBB-permeable metabolite of Cariprazine (HY-14763) . Didesmethyl cariprazine is a partial agonist at the D2 and D3 receptors, full agonist at the 5-HT1A receptor, and antagonist at the human 5-HT2B receptor (Ki: 1.41 nM (human D2L), 0.056 nM (human D3), 1.7 nM (human 5-HT1A), 0.52 nM (human 5-HT2B) ) . Didesmethyl cariprazine dose-dependently inhibits the spontaneous activity of rat midbrain dopaminergic neurons[1][2].

Product Specifications

CAS Number

[839712-25-3]

UNSPSC

12352005

Target

5-HT Receptor; Dopamine Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/didesmethyl-cariprazine.html

Concentration

10mM

Purity

99.63

Solubility

DMSO : 11.36 mg/mL (ultrasonic; warming; heat to 80°C)

Smiles

O=C(N)N[C@H]1CC[C@H](CCN2CCN(C3=CC=CC(Cl)=C3Cl)CC2)CC1

Molecular Formula

C19H28Cl2N4O

Molecular Weight

399.36

References & Citations

[1]Citrome L, et al. Cariprazine for acute and maintenance treatment of adults with schizophrenia: an evidence-based review and place in therapy. Neuropsychiatr Dis Treat. 2018 Oct 5;14:2563-2577.|[2]Kiss B, et al. Preclinical pharmacodynamic and pharmacokinetic characterization of the major metabolites of cariprazine. Drug Des Devel Ther. 2019 Sep 16;13:3229-3248.