Dopamine Receptor D3 Antagonist II, YQA14

A highly potent and selective antagonist of dopamine D3 receptors. Has two binding sites on human cloned D3 receptors (K_i = 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 (K_i = 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.

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 (K_i = 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.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Cell permeable: yes

Primary Target
D3

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C

Song, R., et al. 2014. Neuropharm.77, 398.
Song, R., et al. 2011. Addiction Biol.17, 259.

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