Potent dopamine D4
receptor partial agonist (EC50
= 12.4 nM; 61% efficacy vs. dopamine). Has no agonist activity at D2
> 10 μ
M). Selective in rats in vivo
; produces penile erection following i.c.v. administration; increases intracavernosal pressure and potentiates the proerectile effects of sildenafil following s.c. administration. Displays minimal side effects.
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Dopamine D4 ligands and models of receptor activation: 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole and related heteroarylmethylarylpiperazines exhibit a substituent effect responsible for additional efficacy tuning.
Stewart et al.
Discovery of 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole (ABT-724), a dopaminergic agent with a novel mode of action for the potential treatment of erectile dysfunction.
Cowart et al.
Activation of dopamine D4 receptors by ABT-724 induces penile erection in rats.
Brioni et al.