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ABT 724 trihydrochloride

Dopamine D4 receptor agonist,potent and selective CAS# 587870-77-7

ABT 724 trihydrochloride

Catalog No. BCC7293----Order now to get a substantial discount!

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Chemical structure

ABT 724 trihydrochloride

3D structure

Chemical Properties of ABT 724 trihydrochloride

Cas No. 587870-77-7 SDF Download SDF
PubChem ID 16759165 Appearance Powder
Formula C17H22Cl3N5 M.Wt 402.75
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in water
Chemical Name 2-[(4-pyridin-2-ylpiperazin-1-yl)methyl]-1H-benzimidazole;trihydrochloride
SMILES C1CN(CCN1CC2=NC3=CC=CC=C3N2)C4=CC=CC=N4.Cl.Cl.Cl
Standard InChIKey AZFUVPBLKQGSRI-UHFFFAOYSA-N
Standard InChI InChI=1S/C17H19N5.3ClH/c1-2-6-15-14(5-1)19-16(20-15)13-21-9-11-22(12-10-21)17-7-3-4-8-18-17;;;/h1-8H,9-13H2,(H,19,20);3*1H
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of ABT 724 trihydrochloride

DescriptionPotent 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.

ABT 724 trihydrochloride Dilution Calculator

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ABT 724 trihydrochloride Molarity Calculator

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Preparing Stock Solutions of ABT 724 trihydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.4829 mL 12.4146 mL 24.8293 mL 49.6586 mL 62.0732 mL
5 mM 0.4966 mL 2.4829 mL 4.9659 mL 9.9317 mL 12.4146 mL
10 mM 0.2483 mL 1.2415 mL 2.4829 mL 4.9659 mL 6.2073 mL
50 mM 0.0497 mL 0.2483 mL 0.4966 mL 0.9932 mL 1.2415 mL
100 mM 0.0248 mL 0.1241 mL 0.2483 mL 0.4966 mL 0.6207 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on ABT 724 trihydrochloride

ABT 724 trihydrochloride is a highly selective D4 dopamine agonist [1][2], with an EC50 of 281 nM in increasing the binding activity of GTPγS in CHO cells transfected with human D4 receptors, and of 12.4 nM in increasing Ca2+ influx of HEK-293 cells co-transfected with a G protein (Gαq05) and rat/human D4 receptors [3].

The neurotransmitter dopamine (DA) is important for regulating functions of human T cell. Through D1/D5, D2, and D3 receptors, DA can activate resting T cells by stimulating the expression of surface integrins and the release of cytokines. By down-regulating nonreceptor tyrosine kinases, DA can inhibit the proliferation of activated T cells. Stimulation of dopamine D4 receptors can induce T cell quiescence [1].

With the presence of the D4 receptors, T cells were treated with the specific D4 DA agonist PD 168,077 at a concentration of 1 ?M at the onset of 48 h of TCR stimulation with anti-CD3/CD28 so that the D4 DA agonist remained throughout this period, The proliferation of these cells was significantly inhibited. This result was from the evidence of [3H]thymidine incorporation. When treated with another D4 DA agonist, ABT 724 trihydrochloride at a concentration of 1 ?M, T cells also showed similar results [1].

Clozapine has high affinity for the dopamine D4 receptor [4]. Compared to treatment with clozapine alone, clozapine plus 50 ?M or 25 ?M ABT-724 significantly increase the locomotor activity of zebrafish larvae. The effect of ABT-724 to protect larvae from the clozapine-induced hypoactivity is in a dose-dependent fashion [5].

References:
[1].  Sarkar C, Das S, Chakroborty D, et al. Cutting Edge: Stimulation of dopamine D4 receptors induce T cell quiescence by up-regulating Kruppel-like factor-2 expression through inhibition of ERK1/ERK2 phosphorylation. J Immunol, 2006, 177(11):7525-9.
[2].  Melis MR, Succu S, Mascia MS, et al. PD-168077, a selective dopamine D4 receptor agonist, induces penile erection when injected into the paraventricular nucleus of male rats. Neurosci Lett, 2005, 379(1):59-62.
[3].  Sanna F, Contini A, Melis MR, et al. Role of dopamine D4 receptors in copulatory behavior: Studies with selective D4 agonists and antagonists in male rats. Pharmacol Biochem Behav, 2015, 137:110-8.
[4].  Arranz M, Collier D, Sodhi M, et al. Association between clozapine response and allelic variation in 5-HT2A receptor gene. Lancet, 1995, 346(8970):281-2.
[5].  Boehmler W, Carr T, Thisse C, et al. D4 Dopamine receptor genes of zebrafish and effects of the antipsychotic clozapine on larval swimming behaviour. Genes Brain Behav, 2007, 6(2):155-66.

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References on ABT 724 trihydrochloride

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.[Pubmed:15239663]

J Med Chem. 2004 Jul 15;47(15):3853-64.

A new class of agents with potential utility for the treatment of erectile dysfunction has been discovered, guided by the hypothesis that selective D4 agonists are erectogenic but devoid of the side effects typically associated with dopaminergic agents. The lead agent 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole (1, ABT-724) was discovered by optimization of a series of benzimidazole arylpiperazines. This highly selective D4 agonist was found to be very potent and efficacious in vivo, eliciting penile erections in rats at a dose of 0.03 micromol/kg, with a positive response rate of 77% erectile incidence. Even at high doses, it was devoid of side effects in animal models of central nervous system behaviors, emesis, or nausea. The structure-activity relationship of the parent benzimidazole series leading to 1 is described, with the detailed in vitro and in vivo profiles described. Distinctive structural features were discovered that are associated with D4 selective agonism in this series of analogues.

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.[Pubmed:15084133]

J Med Chem. 2004 Apr 22;47(9):2348-55.

A series of subtype selective dopamine D(4) receptor ligands from the hetroarylmethylphenylpiperazine class have been discovered that exhibit a remarkable structure-activity relationship (SAR), revealing a substituent effect in which regiosubstitution on the terminal arylpiperazine ring can modulate functional or intrinsic activity. Other structure-dependent efficacy studies in the dopamine D(4) field have suggested a critical interaction of the heteroarylmethyl moiety with specific protein microdomains in controlling intrinsic activity. Our studies indicate that for some binding orientations, the phenylpiperazine moiety also plays a key role in determining efficacy. These data also implicate a kinetic or efficiency term, contained within measured functional affinities for agonists, which support a sequential binding and conformational stabilization model for receptor activation. The structural similarity between partial agonist and antagonist, within this subset of ligands, and lack of bioisosterism for this substituent effect are key phenomena for these hypotheses.

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.

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