ABT-724 是高度选择性的多巴胺D4受体激动剂，对人多巴胺D4受体的EC50=12.4 nM。它是大鼠D4(EC50为 14.3 nM) 和雪貂D4受体 (EC50为 23.2 nM) 的有效部分激动剂，对多巴胺 D1，D2，D3或 D5受体没有影响。它可用于勃起功能障碍的研究，并具有较少的副作用。

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

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].

70006-24-5

C17H19N5

293.374

2 - [(4-吡啶-2-基哌嗪-1-基)甲基]-1H-苯并咪唑

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years