LY341495

LY341495 is a potent and selective antagonist of the group II metabotropic glutamate receptors (mGluR), mGluR2 and mGluR3 (IC₅₀s = 21 and 14 nM, respectively, for human isoforms).^1,2,3 It less effectively blocks mGluR8 and mGluR7 (IC₅₀s = 173 and 990 nM, respectively) and weakly antagonizes mGluR1, mGluR5, and mGluR4 (IC₅₀s = 6.8, 8.2, and 22 μM, respectively).² In rat forebrain tissue, LY341495 may bind mGluR3 more avidly than mGluR2.⁴ LY341495 can be effectively used in isolated cells, tissues, and in vivo.^4,5,6 In mice, it penetrates the blood-brain barrier and has been used to study the roles of mGlu2/3 receptors in the brain.^5,7,8

WARNING This product is not for human or veterinary use.

1. Collado, I., Ezguerra, J., Mazón, A., et al. 2,3'-Disubstituted-2-(2'-carboxycyclopropyl)glycines as potent and selective antagonists of metabotropic glutamate receptors. Bioorg. Med. Chem. Lett. 8(20), 2849-2854 (1998).

2. Kingston, A.E., Ornstein, P.L., Wright, R.A., et al. LY341495 is a nanomolar potent and selective antagonist of group II metabotropic glutamate receptors. Neuropharmacology 37(1), 1-12 (1998).

3. Bräuner-Osborne, H., Egebjerg, J., Nielsen, E.O., et al. Ligands for glutamate receptors: Design and therapeutic prospects. J. Med. Chem. 43(14), 2609-2645 (2000).

4. Wright, R.A., Arnold, M.B., Wheeler, W.J., et al. [³H]LY341495 binding to group II metabotropic glutamate receptors in rat brain. J. Pharmacol. Exp. Ther. 298(2), 453-460 (2001).

5. Battaglia, G., Busceti, C.L., Pontarelli, F., et al. Protective role of group-II metabotropic glutamate receptors against nigro-striatal degeneration induced by 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine in mice. Neuropharmacology 45(2), 155-166 (2003).

6. Fitzjohn, S.M., Bortolotto, Z.A., Palmer, M.J., et al. The potent mGlu receptor antagonist LY341495 identifies roles for both cloned and novel mGlu receptors in hippocampal synaptic plasticity. Neuropharmacology 37(12), 144-1458 (1998).

7. Benneyworth, M.A., Xiang, Z., Smith, R.L., et al. A selective positive allosteric modulator of metabotropic glutamate receptor subtype 2 blocks a hallucinogenic drug model of psychosis. Mol. Pharmacol. 72(2), 477-484 (2007).

8. Galici, R., Jones, C.K., Hemstapat, K., et al. Biphenyl-indanone A, a positive allosteric modulator of the metabotropic glutamate receptor subtype 2, has antipsychotic- and anxiolytic-like effects in mice. J. Pharmacol. Exp. Ther. 318(1), 173-185 (2006).