本发明涉及化合物(I)或其药学上可接受的盐的剂量方案,其用于治疗由NR2BNMDA受体的负变构调节或抑制介导的疾病或病症,包括,但不限于严重抑郁障碍,难治性抑郁症和自杀倾向.本发明还涉及化合物(I)或其药学上可接受的盐在治疗在具有自杀观念与意图的的患者中的严重抑郁障碍中的用途....
Structure of the zinc-bound amino-terminal domain of the NMDA receptor NR2B subunit. The EMBO journal 28, 3910–3920 (2009). 13. Mony, L., Kew, J. N., Gunthorpe, M. J. & Paoletti, P. Allosteric modulators of NR2B-containing NMDA receptors: molecular mechanisms and therapeutic potential...
606 infusion on cognition in patients with treatment-resistant depression was not reported. The therapeutic margin between antidepressant effect and cognitive impairment is therefore not well established. In nonhuman primates there are no published reports describing the impact of systemic NR2B NAM ...
同.如在背根神经节,NR2B和NR2D的表达水平明 显高于NR2A和NR2C¨.Q.P.MA等的研究发现, NR2B主要在细的初级传人纤维中表达,而含有 NR2B亚基的NMDA受体可能对初级传人神经的神 经递质的释放有调节作用J. 2外周NMDA受体在炎症及神经病理性疼 痛发生及维持中的作用 ...
(2003) Novel N1-(benzyl)cin- namamidine derived NR2B subtype-selective NMDA receptor antagonists. Bioorg Med Chem Lett;13:693- 696.N.R. Curtis, H.J. Diggle, J.J. Kulagowski, C. London, S. Grimwood, P.H. Hutson, F. Murray, P. Richards, A. Macaulay, K.A. Wafford, Novel N1-...
These agents have opposite effects on mean open time as well as on mean shut time consistent with their PAM and NAM activities. They also have generally opposite effects on the time spent in the different closed states. UBP684 decreases the area of the 3 slowest shut states while increasing ...
Protons trap NR1/NR2B NMDA receptors in a nonconducting state J. Neurosci., 25 (2005), pp. 42-51 View in ScopusGoogle Scholar Borza and Domany, 2006 I. Borza, G. Domany NR2B selective NMDA antagonists: the evolution of the ifenprodil-type pharmacophore Curr. Top. Med. Chem., 6 (200...
The invention relates to a dosage regimen of Compound (I), or a pharmaceutically acceptable salt thereof, for the treatment of diseases or disorders mediated by negative allosteric modulation or inhibition of NR2B-NMDA receptor including, but not limited to, major depressive disorder, treatment ...
Fear, anxiety, and trauma-related disorders, including post-traumatic stress disorder (PTSD), are quite common and debilitating, with an estimated lifetime prevalence of ~28% in Western populations. They are associated with excessive fear reactions, ofte
NR2Btemperature-dependencezincThe N-methyl-d-aspartate receptor (NMDAR) exhibits strong voltage-dependent block by extracellular Mg2+, which is relieved by sustained depolarization and glutamate binding, and which is central to the function of the NMDAR in synaptic plasticity. Rapid membrane ...