2899250-94-1

Name	Dopamine D3 Receptor Agonist 13a
CAS	2899250-94-1

Synonyms

Dopamine D3 receptor ligand-5 Dopamine D3 Receptor Agonist 13a

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Chemical Properties

solubility

DMF: Soluble
Ethanol: 3 mg/ml

Hazard Information

Uses

Dopamine D3 receptor ligand-5 (13a), a Cariprazine (HY-14763) analogue, is a dopamine D3 receptor ligand, with Ki values of 2.85 nM and 0.14 nM for D2R and D3R, respectively[1].

in vivo

Dopamine D3 receptor ligand-5 (13a) decreases cocaine self-administration (FR2; 1-10 mg/kg, i.p.) in rats, suggesting that partial agonists/antagonists with modest D3R/D2R-selectivity may be effective in treating PSUD and potentially comorbidities with other affective disorders^[1].

IC 50

D₃ Receptor: 0.14 nM (Ki); 5-HT_2B Receptor: 1.47 nM (Ki); D₂ Receptor: 2.85 nM (Ki); 5-HT_1A Receptor: 6 nM (Ki); 5-HT_2A Receptor: 54 nM (Ki); 5-HT_2C Receptor: 252 nM (Ki); D₄ Receptor: 756 nM (Ki); D₁ Receptor: 4600 nM (Ki)

References

[1] Emma S Gogarnoiu, et al. Dopamine D3/D2 Receptor Ligands Based on Cariprazine for the Treatment of Psychostimulant Use Disorders That May Be Dual Diagnosed with Affective Disorders. J Med Chem. 2023 Feb 9;66(3):1809-1834. DOI:10.1021/acs.jmedchem.2c01624

Supplier

Shanghai Beckham Medical Technology Co., Ltd

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Websitehttps://www.chemicalbook.com/ShowSupplierProductsList16976/0_EN.htm

Suzhou Zhixin Biotechnology Co., Ltd.

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Shanghai Yifei Biotechnology Co. , Ltd.

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Websitehttp://www.efebio.com

TargetMol Chemicals Inc.

Telephone 15002134094

Websitehttps://www.targetmol.cn/

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