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L-687,414
L-687,414 is a glycine-site NMDA receptor antagonist or low-maximal efficacy, efficacy partial agonist ( ≈ 10%) which is used in scientific research. It is a close structural analog, analogue of HA-966. The drug has been found to produce hyperlocomotion (a psychostimulant-like effect), analgesia or antinociceptive effects, anticonvulsant effects, and neuroprotective effects in animals. In contrast to uncompetitive antagonist, uncompetitive NMDA receptor antagonists like ketamine and phencyclidine (PCP), L-687,414 has not been associated with the development of brain vacuoles (i.e., Olney's lesions) in animals. Trace amine-associated receptor 1 (TAAR1) partial and full agonists, including RO5166017, RO5203648, RO5256390, and RO5263397, have been found to reverse the hyperlocomotion induced by L-687,414 as well as by other NMDA receptor antagonists like PCP in rodents. Similarly, glycine reuptake inhibitor, glycine transporter 1 (GlyT1) inhibitors reverse the hyperlocomotion induce ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Glycine-site
The ''N''-methyl-D-aspartate receptor (also known as the NMDA receptor or NMDAR), is a glutamate receptor and predominantly Ca2+ ion channel found in neurons. The NMDA receptor is one of three types of ionotropic glutamate receptors, the other two being AMPA receptor, AMPA and kainate receptors. Depending on its subunit composition, its Ligand (biochemistry), ligands are Glutamate (neurotransmitter), glutamate and glycine (or D-Serine, D-serine). However, the binding of the ligands is typically not sufficient to open the channel as it may be blocked by Magnesium, Mg2+ ions which are only removed when the neuron is sufficiently depolarized. Thus, the channel acts as a "coincidence detector" and only once both of these conditions are met, the channel opens and it allows cation, positively charged ions (cations) to flow through the cell membrane. The NMDA receptor is thought to be very important for controlling synaptic plasticity and mediating learning and memory functions. The N ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
