Uses
LY-341495 is a potent and selective group II metabotropic glutamate receptor (mGluR) antagonist.
Uses
LY 341495 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). 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). In rat forebrain tissue, LY341495 may bind mGluR3 more avidly than mGluR2. LY341495 can be effectively used in isolated cells, tissues, and in vivo. In mice, it penetrates the blood-brain barrier and has been used to study the roles of mGlu2/3 receptors in the brain.[Cayman Chemical]
Definition
ChEBI: (1S,2S)-2-[(1S)-1-amino-1-carboxy-2-(9H-xanthen-9-yl)ethyl]-1-cyclopropanecarboxylic acid is a member of xanthenes.
Biological Activity
Highly potent and selective group II metabotropic glutamate receptor antagonist (K i /IC 50 values are 2.3, 1.3, 173, 990, 6800, 8200 and 22000 nM for human mGlu 2 , mGlu 3 , mGlu 8 , mGlu 7a , mGlu 1a , mGlu 5a and mGlu 4a receptors respectively). Readily brain penetrant and active in vivo . Also available as part of the Group II mGlu Receptor Tocriset™ , Group III mGlu Receptor Tocriset™ and Mixed mGlu Receptor Tocriset™ .
References
[1] 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, 1998, 37(1): 1-12.
[2] 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, 1998, 37(12): 1445-1458.
[3] pitsikas n, kaffe e, markou a. the metabotropic glutamate 2/3 receptor antagonist ly341495 differentially affects recognition memory in rats. behavioural brain research, 2012, 230(2): 374-379.
