839712-25-3
Chemical Structure
Didesmethyl cariprazine
- CAS No.: 839712-25-3
- Formula:C19H28Cl2N4O
- Molecular Weight:399.36
IUPAC Name: 1-((1r,4r)-4-(2-(4-(2,3-dichlorophenyl)piperazin-1-yl)ethyl)cyclohexyl)urea
InChIKey: UMTWXZNVNBBFLC-SHTZXODSSA-N
SMILES: O=C(N)N[C@H]1CC[C@H](CCN2CCN(C3=CC=CC(Cl)=C3Cl)CC2)CC1
Biological Activity: 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].
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Didesmethyl cariprazine | 99.63% | 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. | ||||||||||||||||||||
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Didesmethyl cariprazine (Standard) | ≥98% | Didesmethyl cariprazine (Standard) is the analytical standard of Didesmethyl cariprazine (HY-100658). This product is intended for research and analytical applications. 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. | ||||||||||||||||||||
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Didesmethyl cariprazine-d8 | 99.40% | Didesmethyl cariprazine-d8 is the deuterium labeled Didesmethyl cariprazine (HY-100658). 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. | ||||||||||||||||||||
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Similarity Score 0.90
HY-100656Desmethyl cariprazine -
Similarity Score 0.89
HY-14763RCariprazine (Standard) -
Similarity Score 0.88
HY-14763ACariprazine hydrochloride -
Similarity Score 0.86
HY-183776Dopamine D3 receptor agonist-2 -
Similarity Score 0.84
HY-156239Dopamine D3 receptor ligand-5 -
Similarity Score 0.84
HY-47412Cariprazine impurity 1 -
Similarity Score 0.81
HY-177122Raxlaprazine etomoxil -
Similarity Score 0.80
HY-14763SCariprazine-d6 -
Similarity Score 0.73
HY-W724128Cariprazine N-oxide -
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References
- [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. [Content Brief]
- [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. [Content Brief]
