ABT 724 trihydrochloride

Names

[ Name ]:
ABT 724 trihydrochloride

[Synonym ]:
MFCD08703101
1H-Benzimidazole, 2-[[4-(2-pyridinyl)-1-piperazinyl]methyl]-, hydrochloride (1:3)
2-{[4-(2-Pyridinyl)-1-piperazinyl]methyl}-1H-benzimidazole trihydrochloride
2-{[4-(Pyridin-2-yl)piperazin-1-yl]methyl}-1H-benzimidazole trihydrochloride
ABT-724 trihydrochloride

Biological Activity

[Description]:

ABT-724 trihydrochloride is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 trihydrochloride is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM), and has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 trihydrochloride 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

[ Molecular Formula ]:
C₁₇H₂₂Cl₃N₅

[ Molecular Weight ]:
402.749

[ Exact Mass ]:
401.094086

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H315-H319-H335

[ Precautionary Statements ]:
P261-P305 + P351 + P338

[ RIDADR ]:
NONH for all modes of transport

Articles

Effects of selective dopaminergic compounds on a delay-discounting task.

Behav. Pharmacol. 22 , 300-11, (2011)

Impulsivity is widely regarded as a multidimensional trait that encompasses two or more distinct patterns of behavior, and dopaminergic systems are implicated in the expression of impulsive behavior i...

Dopamine D4 receptor involvement in the discriminative stimulus effects in rats of LSD, but not the phenethylamine hallucinogen DOI.

Psychopharmacology 203 , 265-77, (2009)

Lysergic acid diethylamide (LSD) differs from other types of hallucinogens in that it possesses direct dopaminergic effects. The exact nature of this component has not been elucidated.The present stud...

Penile erection and yawning induced by dopamine D2-like receptor agonists in rats: influence of strain and contribution of dopamine D2, but not D3 and D4 receptors.

Behav. Pharmacol. 20 , 303-11, (2009)

Dopamine (DA) is implicated in penile erection (PE) and yawning (YA) in rats through activation of D2-like receptors. However, the exact role of each subtype (D2, D3 and D4) of this receptor family in...