A 412997 dihydrochloride

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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].

[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.