trans-ACPD 是代谢型受体激动剂,可促进钙离子活动及产生内向电流。
产品描述
(±)-trans-ACPD is an equimolecular mixture of (1S, 3R)- and (1R, 3S)-ACPD. (±)-trans-ACPD is a selective agonist of the mGluR (metabotropic glutamate receptor); active at the group I/II mGlu receptors (EC50: 2/15/23/800 μM, mGluR2/1/5/4).
体外活性
Excitatory amino acid (EAA) analogues activate receptors that are coupled to the increased hydrolysis of phosphoinositides (PIs). Hippocampal slices are prepared from neonatal rats (6-11 days old) to characterize the effects of EAA analogues on these receptors in these studies. The concentration of trans-ACPD required to evoke half-maximal stimulation (EC50 value) is 51 μM. DL-2-Amino-3-phosphonopropionate (DL-AP3) is also equipotent as an inhibitor of PI hydrolysis stimulated by ibotenate, quisqualate, and trans-ACPD (IC50 values are 480-850 μM)[2].
体内活性
Intrathecal injection of NMDA, kainate, and trans-ACPD, TNF-α, or IL-1β causes significant (p<0.001) biting behaviour in mice compared to animals injected intrathecally with saline. In all groups, systemic pre-treatment with GM (100 mg/kg, i.p.) significantly (p<0.001) reduces the biting behaviour compared to mice treated with saline (10 mL/kg, i.p.). The greatest effect of GM is observed on the pro-inflammatory cytokines and NMDA, with the following inhibition percentages: TNF-α (92±7%), IL-1β (91±5%), NMDA (69±1%), and trans-ACPD (71±12%). On the contrary, at the same dose, GM has no significant effect on the kainate-mediated biting response[3].
Cas No.
67684-64-4
分子式
C7H11NO4
分子量
173.17
别名
1-amino-1,3-dicarboxycyclopentane;(±)-trans-ACPD;Trans-(±)-ACP
储存和溶解度
H2O:5 mM),with gentle warming
1eq. NaOH:50 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years