ABT 724 trihydrochloride

Biological Activity

ABT 724 trihydrochloride is an ABT 724 is a potent dopamine D₄ receptor partial agonist (EC₅₀ = 12.4 nM; 61% efficacy vs. dopamine), which displays no agonist activity at D₂ receptors (EC₅₀ > 10 μM). ABT 724 is selective in rats in vivo and produces penile erection following i.c.v. administration, and increases intracavernosal pressure and potentiates the proerectile effects of sildenafil following s.c. administration. This compound displays minimal side effects.

External Portal information

The Chemical Probes webpages of the Structural Genomics Consortium are a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of ABT 724 is reviewed on the chemical probes website.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. DA 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 DArgic 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 DA 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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