5.30463
Dopamine Receptor D3 Antagonist II, YQA14
Synonym(s):
Dopamine Receptor D3 Antagonist II, YQA14, D3R Antagonist
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About This Item
Empirical Formula (Hill Notation):
C23H27ClN4O3
CAS Number:
Molecular Weight:
442.94
UNSPSC Code:
12352200
assay
≥98% (HPLC)
form
powder
potency
0.068 pM Ki
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
tan
solubility
DMSO: 100 mg/mL
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Cell permeable: yes
Primary Target
D3
D3
Disclaimer
Toxicity: Standard Handling (A)
General description
A highly potent and selective antagonist of dopamine D3 receptors. Has two binding sites on human cloned D3 receptors (Ki = 0.0680 pM high affinity and 2.11 nM low affinity).
An orally bioavailable benzoxazolone carboxamide derivative that acts as a highly potent and selective antagonist of dopamine D3 receptors. Has two binding sites on human cloned D3 receptors (Ki = 0.0680 pM high affinity and 2.11 nM low affinity). Displays >150-fold greater selectivity for D3 over D2 receptors and about 1000-fold selectivity over other dopamine receptors. Exhibits strong anti-addiction profile and reduces self administration of cocaine in rodent models (6.25 to 25 mg/kg in rats) without affecting their sucrose water self-administration and locomotor activity.
Other Notes
Song, R., et al. 2014. Neuropharm.77, 398.
Song, R., et al. 2011. Addiction Biol.17, 259.
Song, R., et al. 2011. Addiction Biol.17, 259.
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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