ABT724 - CAS 70006-24-5
Catalog number: 70006-24-5
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C17H19N5
Molecular Weight:
293.37
COA:
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Targets:
Dopamine Receptor
Description:
ABT-724 is a dopamine D4 agonist originated by Abbott Laboratories with EC50 value of 12.4 nM. In Dec 2007, Phase-II for Erectile dysfunction was discontinued in USA. Now ABT-724 continues to be used in scientific research into the function of the D4 receptor.
Purity:
98%
Appearance:
Powder
Synonyms:
ABT724; ABT 724; ABT-724; 2-((4-Pyridin-2-ylpiperazine-1-yl)methyl)-1H-benzimidazole;587870-77-7(ABT 724 trihydrochloride)
Solubility:
Soluble in DMSO
Storage:
-20℃ Freezer
MSDS:
Inquire
Application:
Erectile dysfunction
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
InChIKey:
FRPJGTNLZNXQEX-UHFFFAOYSA-N
InChI:
1S/C17H19N5/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)
Canonical SMILES:
c1ccc2c(c1)[nH]c(n2)CN3CCN(CC3)c4ccccn4
Current Developer:
Originator Abbott Laboratories
1.Agonist and antagonist properties of antipsychotics at human dopamine D4.4 receptors: G-protein activation and K+ channel modulation in transfected cells.
Newman-Tancredi A;Heusler P;Martel JC;Ormière AM;Leduc N;Cussac D Int J Neuropsychopharmacol. 2008 May;11(3):293-307. Epub 2007 Sep 26.
Interaction at dopamine D4 receptors may improve cognitive function, which is highly impaired in individuals with schizophrenia, but comparative studies of recent antipsychotics in cellular models of D4 receptor activation are lacking. Here, we report the in-vitro profile of over 30 ligands at recombinant hD4.4 receptors. In [35S]GTPgammaS binding experiments using membranes of CHO-hD4.4 cells, apomorphine, preclamol and the selective D4 agonists, ABT724, CP226269, Ro-10-5824 and PD168077, behaved as partial agonists (Emax 20-60% vs. dopamine), whereas L745870 and RBI257, displayed antagonist properties. The 'conventional' antipsychotic, haloperidol and the 'atypicals', clozapine and risperidone, exhibited antagonist properties, while 'third generation' compounds bifeprunox, SLV313 and F15063, acted as partial agonists (10-30%). Aripiprazole and SSR181507 slightly stimulated [35S]GTPgammaS binding at micromolar concentrations. In Xenopus laevis oocytes co-expressing hD4.4 receptors with G-protein-coupled inwardly rectifying potassium (GIRK) channels, apomorphine, preclamol, ABT724, CP226269, and PD168077 stimulated GIRK currents (Emax 70-80%). The 5-HT1A receptor ligands, WAY100635 and flibanserin, also exhibited partial agonist activity (30% and 15%, respectively).
2.Discovery of 3-methyl-N-(1-oxy-3',4',5',6'-tetrahydro-2'H-[2,4'-bipyridine]-1'-ylmethyl)benzamide (ABT-670), an orally bioavailable dopamine D4 agonist for the treatment of erectile dysfunction.
Patel MV;Kolasa T;Mortell K;Matulenko MA;Hakeem AA;Rohde JJ;Nelson SL;Cowart MD;Nakane M;Miller LN;Uchic ME;Terranova MA;El-Kouhen OF;Donnelly-Roberts DL;Namovic MT;Hollingsworth PR;Chang R;Martino BR;Wetter JM;Marsh KC;Martin R;Darbyshire JF;Gintant G;Hsieh GC;Moreland RB;Sullivan JP;Brioni JD;Stewart AO J Med Chem. 2006 Dec 14;49(25):7450-65.
The goal of this study was to identify a structurally distinct D(4)-selective agonist with superior oral bioavailability to our first-generation clinical candidate 1a (ABT-724) for the potential treatment of erectile dysfunction. Arylpiperazines such as (heteroarylmethyl)piperazine 1a, benzamide 2, and acetamides such as 3a,b exhibit poor oral bioavailability. Structure-activity relationship (SAR) studies with the arylpiperidine template provided potent partial agonists such as 4d and 5k that demonstrated no improvement in oral bioavailability. Further optimization with the (N-oxy-2-pyridinyl)piperidine template led to the discovery of compound 6b (ABT-670), which exhibited excellent oral bioavailability in rat, dog, and monkey (68%, 85%, and 91%, respectively) with comparable efficacy, safety, and tolerability to 1a. The N-oxy-2-pyridinyl moiety not only provided the structural motif required for agonist function but also reduced metabolism rates. The SAR study leading to the discovery of 6b is described herein.
3.ABT-724 alleviated hyperactivity and spatial learning impairment in the spontaneously hypertensive rat model of attention-deficit/hyperactivity disorder.
Yin P;Cao AH;Yu L;Guo LJ;Sun RP;Lei GF Neurosci Lett. 2014 Sep 19;580:142-6. doi: 10.1016/j.neulet.2014.08.008. Epub 2014 Aug 12.
Dysfunction of dopamine D4 receptor (D4R) is linked to attention-deficit/hyperactivity disorder (ADHD) as well as ADHD associated cognitive impairment. Here, we tested the possible therapeutic benefit of the D4R-selective agonist ABT-724 in adolescent spontaneously hypertensive rats (SHRs). ABT-724-treated SHRs were administered ABT-724 (0.04mg/kg, 0.16mg/kg or 0.64mg/kg) from postnatal day (P) 28 to P32. Control SHRs and Sprague-Dawley (SD) rats were injected with saline. Then two cohorts of rats were tested in the open field and Làt maze that measured locomotion and non-selective attention (NSA), respectively. Another cohort of rats was subjected to water maze task for evaluation of spatial learning and memory. We found that control SHRs displayed hyperactivity as well as impaired NSA and spatial learning compared with normotensive SD rats. ABT-724 (0.16 and 0.64mg/kg) treatment alleviated hyperactivity and spatial learning impairment in SHRs. No dose of ABT-724 tested altered NSA in SHRs. Our results raise the possibility that ABT-724 may be used as a therapeutic intervention for ADHD patients during adolescence.
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CAS 70006-24-5 ABT724

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