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
Storage condition:
OK to freeze, protect from light
assay
≥98% (HPLC)
Quality Segment
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
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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
D3
D3
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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