NMDA 是一种氨基酸,作为 D-异构体,是谷氨酸受体的 NMDA 受体亚型的定义激动剂。
产品描述
N-Methyl-D-aspartic acid is an amino acid that, as the D-isomer, is the defining agonist for the NMDA receptor subtype of glutamate receptors.
体外活性
NMDA is an excitatory amino acid neurotransmitter, which only binds to the NMDA receptor without effecting other glutamate receptors (such as those for AMPA and kainate). NMDA specifically binds to the NR2 subunits of NMDA receptor, and then stimulates the open of non-specific cation channel which can allow the passage of Ca2+ and Na+ into the cell and K+ out of the cell. Activation of the NMDA receptor is able to produce the excitatory postsynaptic potential (EPSP), and trigger the increase of intracellular Ca2+ content which may further take participating in various signaling pathways. NMDA receptor plays a key role in a wide range of physiological (e.g. long-term potentiation and neuronal plasticity) and pathological processes (e.g. excitotoxicity and epilepsy). [1]
体内活性
The microinjection of NMDA (0.2 nM) exhibits significant effects on MF, IF, IL, and EL, respectively, decreasing the mount and intromission frequencies, and shortening the intromission and ejaculation latencies. NMDA and AP-5 significantly, respectively, facilitates and inhibits the ejaculatory behavior during the copulation testing 30 min. Bilateral microinjection of NMDA into PVN significantly increases the baseline LSNA, the peaking increment of LSNA occurred within 5 min from the time of NMDA microinjected into PVN[3].
激酶实验
Adrenal membranous homogenate suspensions are incubated with 10 nM [3H]Glu in 500/zl 50 mM Tris-acetate buffer (pH 7.4) at 2°C or 30°C in the presence and absence of various compounds. Incubation is terminated by the addition of 3 mL ice-cold buffer and subsequent filtration through a Whatman GF/B glass filter under a constant vacuum of 15 mm Hg. After washing the filter 4 times with 3 mL icecold buffer, the radioactivity trapped on the filter is measured by a liquid scintillation spectrometer using 5 mL modified Triton-toluene scintillant at a counting efficiency of 40-42%. The radioactivity found in the presence of 1 mM non-radioactive Glu is subtracted from each experimental value to obtain the specific binding of [3H]GIu in accordance with the y-aminobutyric acid (GABA) receptor binding assay system. The kinetic parameters of [3H]GIu binding, Kd and Bma x, are calculated by Scatchard analysis of the specific binding using a personal computer with a programme for non-linear regression analysis developed in our own laboratory.
Cas No.
6384-92-5
分子式
C5H9NO4
分子量
147.13
别名
N-甲基-D-天冬氨酸;N-Methyl-D-aspartic acid
储存和溶解度
DMSO:34 mM
H2O:203.9 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years