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2899250-94-1

2899250-94-1 Structure

2899250-94-1 Structure
IdentificationBack Directory
[Name]

Dopamine D3 Receptor Agonist 13a
[CAS]

2899250-94-1
[Synonyms]

Dopamine D3 receptor ligand-5
Dopamine D3 Receptor Agonist 13a
Chemical PropertiesBack Directory
[solubility ]

DMF: Soluble
Ethanol: 3 mg/ml
Hazard InformationBack Directory
[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-HT2B Receptor: 1.47 nM (Ki); D2 Receptor: 2.85 nM (Ki); 5-HT1A Receptor: 6 nM (Ki); 5-HT2A Receptor: 54 nM (Ki); 5-HT2C 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
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