cis-ACBD - CAS 73550-55-7
Category: Inhibitor
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Molecular Formula:
C6H9NO4
Molecular Weight:
159.14
COA:
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Targets:
EAAT2
Description:
cis-ACBD has been found to be a potent inhibitor of EAAT.
Purity:
≥98% by HPLC
Appearance:
White Solid
Synonyms:
cis-1-Aminocyclobutane-1,3-dicarboxylic acid
MSDS:
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InChIKey:
GGMYWPBNZXRMME-UHFFFAOYSA-N
InChI:
InChI=1S/C6H9NO4/c7-6(5(10)11)1-3(2-6)4(8)9/h3H,1-2,7H2,(H,8,9)(H,10,11)
Canonical SMILES:
C1C(CC1(C(=O)O)N)C(=O)O
1.The glycine site of the NMDA receptor contributes to neurokinin1 receptor agonist facilitation of NMDA receptor agonist-evoked activity in rat dorsal horn neurons.
Heppenstall PA;Fleetwood-Walker SM Brain Res. 1997 Jan 9;744(2):235-45.
We have investigated the role of the glycine recognition site of the N-methyl-D-aspartate receptor (the GlyNMDA site) in the facilitation of NMDA receptor agonist-evoked activity in rat dorsal horn neurons that is brought about by neurokinin1 (NK1) receptor agonist and the contribution of protein kinase C (PKC) activation to this phenomenon. Ionophoresis of the selective NMDA receptor agonist 1-aminocyclobutane-cis-1,3-dicarboxylic acid (ACBD) produced a sustained increase in the firing rate of single laminae III-V neurons recorded extracellularly using multibarrelled glass electrodes. The highly selective NK1 receptor agonist acetyl-[Arg6,Sar9,Met(O2)11]-SP6-11 (Sar9-SP) greatly facilitated this response, but under the present conditions had no effect when applied alone or with alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor agonist) at the same current. In the presence of the GLyNMDA site antagonists 2-carboxy-4,6-dichloro-(1H)-indole-3-propanoic acid (MDL 29951), 7-chloro-3-(cyclopropylcarbonyl)-4-hydroxy-2(1H)-quinoline (L701,252), 5,7-dinitroquinaxoline-2,3-dione (MNQX) or 7-chlorothiokynurenic acid (7-CTK), or the PKC inhibitors, chelerythrine or GF109203X, the Sar9-SP-induced facilitation of ACBD-evoked activity was prevented, generally restoring activity to a level similar to that in the presence of ACBD alone, whilst an AMPA receptor antagonist, 6-nitro-7-sulfamoylbenzo(f)quinoxaline-2,3-dione (NBQX) did not inhibit the facilitation.
2.Differences in the release of L-glutamate and D-aspartate from primary neuronal chick cultures.
Lewin L;Mattsson MO;Sellström A Neurochem Res. 1996 Jan;21(1):79-85.
Primary neuronal cultures were made from eight-day-old embryonic chick telencephalon. Ten-day-old cultures were used to study the release of D-[3H]aspartate and L-[3H]glutamate. The D[3H]aspartate release was stimulated by increasing potassium concentrations, but it was not calcium dependent. In contrast, the potassium dependent L-[3H]glutamate release was calcium dependent, and furthermore L-[3H]glutamate release was optimal at potassium concentrations < 30 mM. The inhibitors of glutamate uptake, dihydrokainate and 1-aminocyclobutane-trans-1,3-dicarboxylic acid (CACB), also referred to as cis-1 -aminocyclobutane-1,3-dicarboxylate, were used in the release experiments. Dihydrokainate had no effect on aspartate release, whereas CACB increased both the basal efflux of D-[3H]aspartate and the potassium evoked release. CACB had no effect on the potassium stimulated L-glutamate release. We believe that L-glutamate is released mainly by a vesicular mechanism from the presumably glutamatergic neurons present in our culture. D-aspartate release observed by us, could be mediated by a transporter protein. The cellular origin of this release remains to be assessed.
3.Presynaptic excitability as a potential target for the treatment of the traumatic cerebellum.
Ai J;Baker A Pharmacology. 2004 Aug;71(4):192-8.
Using an extracellular recording method, we have previously shown a hyperexcitability of the presynaptic response in fluid percussion injury (FPI) in rats. In this study, we demonstrated that treatment with cis-ACBD, a glutamate reuptake inhibitor, depressed the presynaptic potential (PSP) in naive/sham controls, while it potentiated the PSP in FPI rats. On the contrary, (RS)-APICA, a selective group II metabotropic glutamate receptor antagonist, potentiated PSP in controls, but depressed PSP in FPI rats. These results indicate that an alteration of the normal function of metabotropic glutamate receptors and glutamate reuptake system or an altered reactivity of presynaptic fibers was induced by FPI. This alteration may contribute to the reported loss of Purkinje cells after FPI. PSP may be used as a potential tool for evaluating treatments of FPI or as a potential target for the prevention of Purkinje cell death.
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Chemical Structure

CAS 73550-55-7 cis-ACBD

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