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A 412997 dihydrochloride

Selective D4 agonist CAS# 1347744-96-0

A 412997 dihydrochloride

2D Structure

Catalog No. BCC6224----Order now to get a substantial discount!

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A 412997 dihydrochloride

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Chemical Properties of A 412997 dihydrochloride

Cas No. 1347744-96-0 SDF Download SDF
PubChem ID 90488953 Appearance Powder
Formula C19H25Cl2N3O M.Wt 382.33
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in water and to 50 mM in DMSO
Chemical Name N-(3-methylphenyl)-2-(4-pyridin-2-ylpiperidin-1-yl)acetamide;dihydrochloride
SMILES CC1=CC(=CC=C1)NC(=O)CN2CCC(CC2)C3=CC=CC=N3.Cl.Cl
Standard InChIKey KIGNSSHMCNBHQX-UHFFFAOYSA-N
Standard InChI InChI=1S/C19H23N3O.2ClH/c1-15-5-4-6-17(13-15)21-19(23)14-22-11-8-16(9-12-22)18-7-2-3-10-20-18;;/h2-7,10,13,16H,8-9,11-12,14H2,1H3,(H,21,23);2*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 A 412997 dihydrochloride

DescriptionSelective agonist for the dopamine D4 receptor (Ki values are 7.9 and 12.1 nM for human D4 and rat D4 receptors). Displays no affinity (<1000 nM) for other dopamine receptors. Shows efficacy in rat models of ADHD and short-term memory.

A 412997 dihydrochloride Dilution Calculator

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A 412997 dihydrochloride Molarity Calculator

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Preparing Stock Solutions of A 412997 dihydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.6155 mL 13.0777 mL 26.1554 mL 52.3108 mL 65.3885 mL
5 mM 0.5231 mL 2.6155 mL 5.2311 mL 10.4622 mL 13.0777 mL
10 mM 0.2616 mL 1.3078 mL 2.6155 mL 5.2311 mL 6.5389 mL
50 mM 0.0523 mL 0.2616 mL 0.5231 mL 1.0462 mL 1.3078 mL
100 mM 0.0262 mL 0.1308 mL 0.2616 mL 0.5231 mL 0.6539 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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References on A 412997 dihydrochloride

Discovery of 3-methyl-N-(1-oxy-3',4',5',6'-tetrahydro-2'H-[2,4'-bipyridine]-1'-ylmethyl)benzam ide (ABT-670), an orally bioavailable dopamine D4 agonist for the treatment of erectile dysfunction.[Pubmed:17149874]

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.

A-412997, a selective dopamine D4 agonist, improves cognitive performance in rats.[Pubmed:16154186]

Pharmacol Biochem Behav. 2005 Sep;82(1):148-55.

The recent development of a highly selective dopamine D4 receptor agonist, A-412997 (2-(3',4',5',6'-tetrahydro-2'H-[2,4'] bipyridinyl-1'-yl)-N-m-tolyl-acetamide), has provided a pharmacological tool with which to conduct systematic investigations into the putative role for dopamine D4 receptors in the central nervous system. These present studies evaluated the potential cognitive enhancing properties of A-412997 in rat models of ADHD (5-trial repeated acquisition inhibitory avoidance in Spontaneous Hypertensive Rat pups) and short-term memory (Social Recognition), in comparison with the less selective dopamine D4 receptor agonists PD168077 and CP226269. A-412997 showed significant dose-dependent efficacy in both models. PD168077 repeatedly improved acquisition in the 5-trial inhibitory avoidance model but failed to reach significance at any dose tested, although significantly improved social recognition was observed (albeit less potent than A-412997). CP226269 showed a significant enhancement in the 5-trial inhibitory avoidance model. These results support a role for the dopamine D4 receptor subtype in cognition.

A-412997 is a selective dopamine D4 receptor agonist in rats.[Pubmed:16153699]

Pharmacol Biochem Behav. 2005 Sep;82(1):140-7.

A-412997 (2-(3',4',5',6'-tetrahydro-2'H-[2,4'] bipyridinyl-1'-yl)-N-m-tolyl-acetamide) is a highly selective dopamine D4 receptor agonist that binds with high affinity to rat dopamine D4 and human dopamine D4.4 receptors (Ki=12.1 and 7.9 nM, respectively). In contrast to the dopamine D4 receptor agonists PD168077 and CP226269, A-412997 showed a better selectivity profile and no affinity <1000 nM for other dopamine receptors or any other proteins in a panel of seventy different receptors and channels. In functional assays using calcium flux, A-412997 was a potent full agonist at rat dopamine D4 receptors (28.4 nM, intrinsic activity=0.83) and did not activate rat dopamine D2L receptors, unlike CP226269. Dopamine D4 receptor selective agonists have been shown to induce penile erection in rats by central mechanisms. A-412997 induces penile erection in a conscious rat model (effective dose=0.1 micromol/kg, s.c.) with comparable efficacy as the nonselective D2-like agonist, apomorphine. When dosed systemically, A-412997 crossed the blood brain barrier rapidly and achieved significantly higher levels than PD168077. A-412997 is a highly selective dopamine D4 receptor agonist and a useful tool to understand the role of dopamine D4 receptors in rat models of central nervous system processes and disease.

Description

Selective D4 agonist

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