Water-soluble, potent, selective group II antagonist. Group III antagonist at higher concentrations.
生理活性の詳細Water-soluble form of the very selective nanomolar potent antagonist for group II mGlu receptors. Also a relatively potent antagonist for group III mGlu receptors at high nanomolar to low micromolar concentrations. Kd values are 1.67 (human mGlu2), 0.75 (mGlu3), 31.6 (mGlu6), 72.7 (mGlu7a) and 14 nM (human mGlu8a ). IC50 values are 7.8, 8.2 and 22 μM for mGlu1a, mGlu5a and mGlu4 receptors, respectively. Readily brain penetrant and active in vivo. A more readily water soluble version is also available (ab120818)
Also available in simple stock solutions (ab146717) - add 1 ml of water to get an exact, ready-to-use concentration.
特記事項Sold under license from Eli Lilly and company
体系名(2S)-2-Amino-2-[(1S,2S)-2-carboxycycloprop-1-yl]-3-(xanth-9-yl) propanoic acid sodium salt
保存方法Store at -20°C. Store under desiccating conditions. The product can be stored for up to 12 months.
溶解性Soluble in water to 10 mM
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.
Linden AM et al. Use of MGLUR2 and MGLUR3 knockout mice to explore in vivo receptor specificity of the MGLUR2/3 selective antagonist LY341495. Neuropharmacology57:172-82 (2009).
Read more (PubMed: 19477188) »
Wright RA et al. Binding of [3H](2S,1'S,2'S)-2-(9-xanthylmethyl)-2-(2'-carboxycyclopropyl) glycine ([3H]LY341495) to cell membranes expressing recombinant human group III metabotropic glutamate receptor subtypes. Naunyn Schmiedebergs Arch Pharmacol362:546-54 (2000).
Read more (PubMed: 11138847) »
Johnson BG et al. [3H]-LY341495 as a novel antagonist radioligand for group II metabotropic glutamate (mGlu) receptors: characterization of binding to membranes of mGlu receptor subtype expressing cells. Neuropharmacology38:1519-29 (1999).
Read more (PubMed: 10530814) »
Kingston AE et al. LY341495 is a nanomolar potent and selective antagonist of group II metabotropic glutamate receptors. Neuropharmacology37:1-12 (1998).
Read more (PubMed: 9680254) »