Catalog Number: 2214
Chemical Name: 2-[[4-(2-Pyridinyl)-1-piperazinyl]methyl]-1H-benzimidazole trihydrochloride
Biological Activity
Potent dopamine D4 receptor partial agonist (EC50 = 12.4 nM; 61% efficacy vs. dopamine). Has no agonist activity at D2 receptors (EC50 > 10 μM). 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.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in water
  • Purity:
  • Storage:
    Desiccate at +4°C
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. 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.
    J.Med.Chem., 2004;47:2348
  2. 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.
    J.Med.Chem., 2004;47:3853
  3. Activation of dopamine D4 receptors by ABT-724 induces penile erection in rats.
    Brioni et al.
    Proc.Natl.Acad.Sci.USA, 2004;101:6758
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