DL-AP5 是一种竞争性 NMDA (N-methyl-D-aspartate) 受体拮抗剂 | MedChemExpress (MCE)

DL-AP5

CAS：76326-31-3

品牌：MedChemExpress (MCE)

存储条件：Powder: -20°C, 3 years.In solvent: -80°C, 6 months; -20°C, 1 month.

生物活性：DL-AP5 (2-APV) 是一种竞争性 NMDA (N-methyl-D-aspartate) 受体拮抗剂。 DL-AP5 显示出显着的镇痛活性。 DL-AP5 特异性阻断兔视网膜[1][2][3] 中的通道。 

体外：DL-AP5 (100 μM) 部分阻止谷氨酸诱导的 Arc/Arg3.1 蛋白水平增加[5]。
DL-AP5 降低 NMDA 诱导的 Arc/Arg3.1 上调[5]。

体内：DL-AP5 (0-10 μg/rat, Intra-CA1) 显着降低NMDA[3]的作用。
DL-AP5 (0-10 nmol, Intracerebroventricular injection) 引起食物消耗的剂量依赖性增加[4]。
DL-AP5（5 nmol，脑室内注射）减轻脑室内注射生长素释放肽引起的食物消耗减少[4] 。

参考文献：

[1]. Murray CW, et al. Neurokinin and NMDA antagonists (but not a kainic acid antagonist) are antinociceptive in the mouse formalin model. Pain. 1991;44(2):179-185.
[2]. Massey SC, et al. N-methyl-D-aspartate receptors of ganglion cells in rabbit retina. J Neurophysiol. 1990;63(1):16-30.
[3]. Jafari-Sabet M. NMDA receptor blockers prevents the facilitatory effects of post-training intra-dorsal hippocampal NMDA and physostigmine on memory retention of passive avoidance learning in rats. Behav Brain Res. 2006 Apr 25;169(1):120-7.
[4]. Taati M, et al. The effects of DL-AP5 and glutamate on ghrelin-induced feeding behavior in 3-h food-deprived broiler cockerels. J Physiol Biochem. 2011 Jun;67(2):217-23.
[5]. Chen T, et al. Glutamate-induced rapid induction of Arc/Arg3.1 requires NMDA receptor-mediated phosphorylation of ERK and CREB. Neurosci Lett. 2017 Nov 20;661:23-28.