CAS NO: | 67684-64-4 |
生物活性 | trans-ACPD, a metabotropic receptor agonist, producescalciummobilization and an inward current in cultured cerebellar Purkinje neurons. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | 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 (EC50value) 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 (IC50values are 480-850 μM)[2]. | ||||||||||||||||
体内研究 (In Vivo) | 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[3]. | ||||||||||||||||
分子量 | 173.17 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C7H11NO4 | ||||||||||||||||
CAS 号 | 67684-64-4 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 50 mg/mL(288.73 mM;Need ultrasonic) H2O : 3.57 mg/mL(20.62 mM;Need ultrasonic) 配制储备液
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以下溶剂前显示的百
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