Potent，selective group II拮抗剂. Group III拮抗剂at higher concentrations.
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 for human receptors are 1.67 (mGlu2), 0.75 (mGlu3), 31.6 (mGlu6), 72.7 (mGlu7a) and 14 nM (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.
Store at Room Temperature. The product can be stored for up to 12 months.
Soluble in DMSO to 10 mM and in 1.2 eq. NaOH to 100 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) »