ABT-724 is an agonist of dopamine D4 receptor(EC50: 12.4 nM)

D4:12.4 nM(EC50), D4 receptor:12.4 nM(EC50)

ABT-724 is a selective dopamine D(4) receptor agonist that activates human dopamine D(4) receptors with an EC(50) of 12.4 nM and 61% efficacy, with no effect on dopamine D(1), D(2), D(3), or D(5) receptors[1].

ABT-724 dose-dependently facilitates penile erection when given s.c. to conscious rats, an effect that is blocked by haloperidol and clozapine but not by domperidone.?A proerectile effect is observed after intracerebroventricular but not intrathecal administration, suggesting a supraspinal site of action.?s.c. injections of ABT-724 increase intracavernosal pressure in awake freely moving rats.?In the presence of sildenafil, a potentiation of the proerectile effect of ABT-724 is observed in conscious rats.?The ability of ABT-724 to facilitate penile erection together with the favorable side-effect profile indicates that ABT-724 could be useful for the treatment of erectile dysfunction[1].

ABT-724 (maleate salt) was freshly prepared and administered to rats via s.c. injection into the back neck area (1 ml/kg injection volume). For intracerebroventricular (ICV) or intrathecal administrations, rats were allowed at least 1 week of recovery from surgery before behavioral testing. The compounds of interest were infused ICV (left lateral ventricle) in a 5-μl volume or 10 μl intrathecally. After the experiment was completed, infusion of 0.5% fast-green dye in saline solution and subsequent dissection were carried out to confirm the diffusion of the injection solution[1].