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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] |
Hyperlocomotion
Locomotor activity is a measure of animal behavior which is employed in scientific research. Hyperlocomotion, also known as locomotor hyperactivity, hyperactivity, or increased locomotor activity, is an effect of certain drugs in animals in which locomotor activity (locomotion) is increased. It is induced by certain drugs like psychostimulants and NMDA receptor antagonists and is reversed by certain other drugs like antipsychotics and certain antidepressants. Stimulation of locomotor activity is thought to be mediated by increased signaling in the nucleus accumbens, a major brain area involved in behavioral activation and motivated behavior. Hypolocomotion, also known as locomotor hypoactivity, hypoactivity, and decreased locomotor activity, is an effect of certain drugs in animals in which locomotor activity is decreased. It is a characteristic effect of many sedative agents and general anesthetics. Antipsychotics, which are dopamine receptor antagonists, and many serotonerg ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
RO5263397
RO5263397, or RO-5263397, is a trace amine-associated receptor 1 (TAAR1) partial or full agonist which is used in scientific research. It is the most well-studied of all of the synthetic TAAR1 ligands. In addition to its use in research, RO5263397 is or was under development for potential clinical use as a medication. Pharmacology Pharmacodynamics Actions RO5263397 is a trace amine-associated receptor 1 (TAAR1) partial agonist to full agonist. Its values are 0.12 to 7.5nM for the mouse TAAR1 (mTAAR1), 35 to 47nM for the rat TAAR1 (rTAAR1), 251nM at the cynomolgus monkey TAAR1, and 17 to 85nM for the human TAAR1 (hTAAR1). Its intrinsic activity (Emax) is 59 to 100% at the mTAAR1, 69 to 76% at the rTAAR1, 85% at the cynomolgus monkey TAAR1, and 81 to 82% at the hTAAR1. The drug was found to have 392-fold higher potency at the mTAAR1 compared to the hTAAR1 ''in vitro'' in one comparative study, although it still activated the hTAAR1 with low-nanomolar potency ( = 0.12). Effects ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
