ABT-724 is a potent and highly selective dopamine D4 receptor agonist with EC50s of 12.4 nM, 14.3 nM and 23.2 nM for human dopamine D4 receptor, rat D4 receptor and ferret D4 receptor.
Dopamine is the main catecholamine in the central nervous system. The dopamine D4 receptor is abundantly expressed in the cortex and hypothalamus, and plays a key role in the regulation of sexual function in mammals. ABT-724 is a highly potent, selective dopamine D4 receptor with an EC50 value of 12.4nM and 61% efficacy for human dopamine D4 receptor, but shows no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 also exhibits potent but partial agonist effects on rat and ferret D4 receptors with EC50 values of 14.3±0.6nM and 23.2±1.3nM, respectively. Subcutaneous injection of ABT-724 at doses of 0.01, 0.03, 0.1, 0.3, and 1μmol/kg induced significant facilitation of penile erection in rats. The maximal effect was observed at 0.03μmol/kg with a 77% incidence, compared to 23% incidence in the control group. The latency to induce a penile erection in ABT-724-treated rats was 18.7 minutes. Also in rats with chronically implanted cannulas, injection of ABT-724 directly into the lateral ventricle significantly facilitated erectile responses at 3nmol. Subcutaneous administration of ABT-724 at 0.0025μmol/kg resulted in 2.0±0.6 episodes of increase in intracavernous pressure in an awake freely moving rat.[1]
作用机制
ABT-724 is a selective dopamine D4 receptor agonist that facilitates penile erection in rats without affecting cardiovascular, gastrointestinal, or central nervous system function.[1]
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