A partial agonist of the NMDA receptor
GLYX 13 is a monoclonal antibody-derived tetrapeptide that acts as a partial agonist at the glycine site of the N-methyl-D-aspartate (NMDA) receptor.1,2 It is active in vivo when administered intravenously, and it readily passes through the blood-brain barrier.1,3 GLYX 13 has diverse effects in animals, as it blocks neuropathic pain, enhances learning and memory, and significantly reduces anxiety.2,3,4 GLYX 13 induces rapid antidepressant-like effects in animal models and rescued normal behavior in a rat model of autism.5,6,7
1.Moskal, J.R., Kuo, A.G., Weiss, C., et al.GLYX-13: a monoclonal antibody-derived peptide that acts as an N-methyl-D-aspartate receptor modulatorNeuropharmacology49(7)1077-1087(2005) 2.Wood, P.L., Mahmood, S.A., and Moskal, J.R.Antinociceptive action of GLYX-13: An N-methyl-D-aspartate receptor glycine site partial agonistNeuroport.19(10)1059-1061(2008) 3.Burgdorf, J., Zhang, X.-l., Weiss, C., et al.The N-methyl-D-aspartate receptor modulator GLYX-13 enhances learning and memory, in young adult and learning impaired aging ratsNeurobiol. Aging32(4)698-706(2011) 4.Jin, Z.-L., Liu, J.-X., Liu, X., et al.Anxiolytic effects of GLYX-13 in animal models of posttraumatic stress disorder-like behaviorJ. Psychopharmacol.30(9)913-921(2016) 5.Burgdorf, J., Zhang, X.-l., Nicholson, K.L., et al.GLYX-13, a NMDA receptor glycine-site functional partial agonist, induces antidepressant-like effects without ketamine-like side effectsNeuropsychopharmacology38(5)729-742(2013) 6.Santini, A.C., Pierantoni, G.M., Gerlini, R., et al.Glix 13, a new drug acting on glutamatergic pathways in children and animal models of autism spectrum disordersBiomed. Res. Int.2014234295(2014) 7.Yang, B., Zhang, J.-c., Han, M., et al.Comparison of R-ketamine and rapastinel antidepressant effects in the social defeat stress model of depressionPsychopharmacology233(19-20)3647-3657(2016)
Animal experiment: | Male C57BL/6J mice are used in this study. Mice are group housed (five/cage) in a controlled environment held at 21±2°C with a 14:10 h light-dark period (lights on:±05:00 am). All experiments are conducted during the light phase. Food and water are available ad libitum. For acute drug treatments, Rapastinel Trifluoroacetate (1.0 mg/kg, iv) is administered 30 min prior to the acquisition trial of the novel object recognition (NOR) task to the subchronic ketamine or subchronic phencyclidine (PCP)-treated animals[1]. |
参考文献: [1]. Rajagopal L, et al. GLYX-13 (rapastinel) ameliorates subchronic phencyclidine- and ketamine-induced declarative memory deficits in mice. Behav Brain Res. 2016 Feb 15;299:105-10. | |
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