ABT-724

Names

[ Name ]:
ABT-724

[Synonym ]:
abt 724 trihydrochloride
abt 724

Biological Activity

[Description]:

ABT-724 is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM). ABT-724 has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 could be useful for the treatment of erectile dysfunction and has favorable side-effect profile[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor

Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor

Research Areas >> Neurological Disease

[Target]

EC50: 12.4 nM (Human dopamine D4 receptor), 14.3 nM (Rat dopamine D4 receptor) and 23.2 nM (Ferret dopamine D4 receptor)[1]

[In Vitro]

ABT-724 exhibits a selective biochemical profile, as indicates by a lack of binding affinity for >70 neurotransmitter/uptake/ion channels including D2, D3, or D5 receptors up to a 10 μM concentration. A weak affinity to 5-HT1A receptors (Ki = 2780 nM) is observed. ABT-724 does not inhibit the PDE activity of PDE1, PDE5, or PDE6 at 10 μM concentrations[1].

[In Vivo]

ABT-724 (8.8 μg/kg; subcutaneous injection; daily; for 5 days; male adult Wistar rats) treatment dose-dependently facilitates penile erection when given s.c. to conscious rats[1]. Animal Model: Male adult Wistar rats (~300 g)[1] Dosage: 8.8 μg/kg Administration: Subcutaneous injection; daily; for 5 days Result: Dose-dependently facilitated penile erection.

[References]

[1]. Brioni JD, et al. Activation of dopamine D4 receptors by ABT-724 induces penile erection in rats. Proc Natl Acad Sci U S A. 2004 Apr 27;101(17):6758-63.

Chemical & Physical Properties

[ Density]:
1.275g/cm3

[ Boiling Point ]:
548.6ºC at 760 mmHg

[ Molecular Formula ]:
C₁₇H₁₉N₅

[ Molecular Weight ]:
293.36600

[ Flash Point ]:
285.6ºC

[ Exact Mass ]:
293.16400

[ PSA ]:
48.05000

[ LogP ]:
2.28300

[ Index of Refraction ]:
1.687

Safety Information

[ Hazard Codes ]:
Xi

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds

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