Biochem/physiol Actions

Primary TargetD3

Cell permeable: yes

General description

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.

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

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

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

Packaging

10 mg in Glass bottle

Reconstitution

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

Warning

Toxicity: Standard Handling (A)