Bioactivity | trans-ACPD, a metabotropic receptor agonist, produces calcium mobilization and an inward current in cultured cerebellar Purkinje neurons. | ||||||||||||
Invitro | 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)[2]. | ||||||||||||
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]. | ||||||||||||
Name | trans-ACPD | ||||||||||||
CAS | 67684-64-4 | ||||||||||||
Formula | C7H11NO4 | ||||||||||||
Molar Mass | 173.17 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Linden DJ, et al. Trans-ACPD, a metabotropic receptor agonist, produces calcium mobilization and an inward current in cultured cerebellar Purkinje neurons. J Neurophysiol. 1994 May;71(5):1992-8. [2]. Littman L, et al. Multiple mechanisms for inhibition of excitatory amino acid receptors coupled to phosphoinositide hydrolysis. J Neurochem. 1992 Nov;59(5):1893-904. [3]. Córdova MM, et al. Polysaccharide glucomannan isolated from Heterodermia obscurata attenuates acute and chronic pain in mice. Carbohydr Polym. 2013 Feb 15;92(2):2058-64. |