Potent, selective non-competitive mGlu 1 metabotropic glutamate receptor antagonist (IC 50 = 6.5 μM at hmGluR1 with no activity at hmGluR2, -4a, -5a, -7b, and -8a up to 100 μM).
Storage Temp
Store at 2-8°C,Desiccated
Shipped In
Wet ice
Grade
Moligand™
Action Type
ALLOSTERIC MODULATOR
Mechanism of action
Allosteric modulator of mGlu 1 receptor;Allosteric modulator of mGlu 5 receptor
Note
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description
Store at +4°C. Store under desiccating conditions. The product can be stored for up to 12 months.
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2.Su LD & Shen Y. (2009) Blockade of glutamate transporters facilitates cerebellar synaptic long-term depression.. Neuroreport, 20 (5):(502-7). [PMID:19289926]
3.Droste D et al.. (2017) Ca2+-permeable AMPA receptors in mouse olfactory bulb astrocytes.. Sci Rep, 7 (44817). [PMID:28322255]
4.Shin JH et al.. (2009) Depolarization-induced slow current in cerebellar Purkinje cells does not require metabotropic glutamate receptor 1.. Neuroscience, 162 (3):(688-93). [PMID:19409231]
5.Yang Y & Xu-Friedman MA. (2015) Different pools of glutamate receptors mediate sensitivity to ambient glutamate in the cochlear nucleus.. J Neurophysiol, 113 (10):(3634-45). [PMID:25855696]
6.Urbanski MJ et al.. (2010) Endocannabinoid-mediated synaptically evoked suppression of GABAergic transmission in the cerebellar cortex.. Neuroscience, 169 (3):(1268-78). [PMID:20553815]
7.Ster J et al.. (2011) Enhancement of CA3 hippocampal network activity by activation of group II metabotropic glutamate receptors.. Proc Natl Acad Sci U S A, 108 (24):(9993-7). [PMID:21628565]
8.Su LD et al.. (2010) Ethanol acutely modulates mGluR1-dependent long-term depression in cerebellum.. Alcohol Clin Exp Res, 34 (7):(1140-5). [PMID:20477778]
9.Chanda S & Xu-Friedman MA. (2011) Excitatory modulation in the cochlear nucleus through group I metabotropic glutamate receptor activation.. J Neurosci, 31 (20):(7450-5). [PMID:21593328]
10.Liu MG et al.. (2013) Long-term potentiation of synaptic transmission in the adult mouse insular cortex: multielectrode array recordings.. J Neurophysiol, 110 (2):(505-21). [PMID:23636718]
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14.Kovacs FE et al.. (2011) Purine receptor-mediated endocannabinoid production and retrograde synaptic signalling in the cerebellar cortex.. Br J Pharmacol, 162 (4):(974-88). [PMID:21054344]
15.Li JQ et al.. (2010) Regulation of increased glutamatergic input to spinal dorsal horn neurons by mGluR5 in diabetic neuropathic pain.. J Neurochem, 112 (162-72). [PMID:19840219]
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