Abstract
Two new quinoxalinone derivatives have been synthesized adopting the HONG method, and investigated for some neuropharmacological effects (anxiety- and depressive-like responses) in rats. The present experiment sought to determine whether treatment with these compounds produces changes in affective responses. We found that the chronic injection of 6-nitro-2(1H)-quinoxalinone (NQu) showed obvious anxiolytic- and antidepressant-like effects, respectively, measured in the behavioral tests of Elevated Plus Maze (EPM) and Forced Swim Test (FST). At the dose of 30 mg/kg, NQu showed a comparative anxiolytic-like effect in rats as diazepam (Dz) (1 mg/kg), and a comparative antidepressant effect as clomipramine (Clmp) (2 mg/kg; i.p). The 2(1H)-quinoxalinone (Qu) significantly reduced depressive-like responses as evaluated in FST, whereas no anxiolytic-like effect was found as measured by open field test (OF). Additionally, the locomotor activity levels were unaffected by treatment as measured by OF and EPM.
Highlights
Quinoxalinone derivatives and dihydroquinoxalin-2-ones are an important structural motif for the discovery of biologically active compounds
We found that the chronic injection of 6-nitro-2(1H)-quinoxalinone (NQu) showed obvious anxiolytic- and antidepressant-like effects, respectively, measured in the behavioral tests of Elevated Plus Maze (EPM) and Forced Swim Test (FST)
Open Field Test Three parameters were measured in the open field test (OF): The Number of Returns to the Center (NRC), Time Spent in the Central Area (TCA) and total of central and peripheral squares crossed (NTS)
Summary
Quinoxalinone derivatives and dihydroquinoxalin-2-ones are an important structural motif for the discovery of biologically active compounds. Various quinoxalinone compounds display diverse pharmacological activities. There are a lot of pharmaceuticals and candidates possessing such core structures including the inhibitor of histone deacetylase [14], bradykinin B1 receptor antagonist [15], agonist and antagonist acting through the GABAA/benzodiazepine receptor [16], vascular smooth muscle relaxants and antihypertensive agents [17]. The glutamate, excitatory amino acid neurotransmitter, is thought to be involved with several neurodegenerative and neuropathological disorders, including ischemia [18], epilepsy [19], Huntington’s [20] and Alzheimer’s disease [21]. There is much interest in the modulation of glutamate receptors, especially the N-methyl-Daspartate (NMDA) and α-amino-3-hydroxy-5-methylisoxazole-4-propionate (AMPA) subtypes [22]
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