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A 412997 dihydrochloride

Catalog No.GC14610

A 412997 dihydrochloride Chemical Structure

Selective D4 agonist

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5mg
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25mg
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Sample solution is provided at 25 µL, 10mM.

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Background

A 412997 dihydrochloride is a selective agonist of dopamine D4 receptor with Ki values of 7.9 and 12.1 nM for human and rat D4 receptors, respectively [1].

Dopamine D4 receptor is a G protein-coupled receptor and is activated by dopamine. It plays an important role in cognition, Parkinsons disease, addictive behaviors and so on.

A 412997 dihydrochloride is a selective dopamine D4 receptor agonist. In calcium flux functional assays, A-412997 activated the rat dopamine D4 receptor with EC50 value and intrinsic activity of 28.4 nM and 0.83, respectively [1].

In Spontaneous Hypertensive Rat pups (SHR pups), A 412997 significantly increased acquisition in the 5-trial repeated acquisition model. In the short-term social memory, A 412997 significantly shortened the second investigation time. In Wistar rats and Dawley rats, A 412997 (3 μM/kg, 10 μM/kg) increased locomotor activity [2]. In rats, A 412997 reduced non-rapid eye movement (NREM) sleep duration and increased waking duration. Also, A 412997 reduced rapid eye movement (REM) sleep duration and delayed the onset of REM sleep [3].

References:
[1].  Moreland RB, Patel M, Hsieh GC, et al. A-412997 is a selective dopamine D4 receptor agonist in rats. Pharmacol Biochem Behav, 2005, 82(1): 140-147.
[2].  Browman KE, Curzon P, Pan JB, et al. A-412997, a selective dopamine D4 agonist, improves cognitive performance in rats. Pharmacol Biochem Behav, 2005, 82(1): 148-155.
[3].  Nakazawa S, Nakamichi K, Imai H, et al. Effect of dopamine D4 receptor agonists on sleep architecture in rats. Prog Neuropsychopharmacol Biol Psychiatry, 2015, 63: 6-13.

Chemical Properties

Cas No. 1347744-96-0 SDF
Chemical Name (Z)-2-(4-(pyridin-2-yl)piperidin-1-yl)-N-(m-tolyl)acetimidic acid dihydrochloride
Canonical SMILES CC1=CC(/N=C(O)/CN2CCC(C3=CC=CC=N3)CC2)=CC=C1.Cl.Cl
Formula C19H23N3O.2HCl M.Wt 382.33
Solubility <38.23mg/ml in H2O; <19.12mg/ml in DMSO Storage Desiccate at RT
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.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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