(±)-trans-ACPD

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

(±)-trans-ACPD 是 (1S, 3R)- 和 (1R, 3S)-ACPD 的等分子混合物。 (±)-trans-ACPD 是 mGluR（代谢型谷氨酸受体）的选择性激动剂。

(±)-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).

Excitatory amino acid (EAA) analogues activate receptors that are coupled to the increased hydrolysis of phosphoinositides (PIs). In these studies, hippocampal slices are prepared from neonatal rats (6-11 days old) to characterize the effects of EAA analogues on these receptors. The concentrations 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).

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%). By contrast, at the same dose, GM has no significant effect on the kainate-mediated biting response.

trans-ACPD

Others

Other Targets

Calcium Channel

Metabolic Disease

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67684-64-4

173.17

C7H11NO4

>98% (HPLC)

H2O : 6.2 mg/mL. 35.80 mM;

[C@@]1(C[C@H](CC1)C(=O)O)(C(=O)O)N

(±)-1-Aminocyclopentane-trans-1,3-dicarboxylic acid

(-20℃)

With Ice Pack

≥ 2 years