ChemicalBook > CAS DataBase List > LY 341495
LY 341495
LY 341495
- CAS No.201943-63-7
- Chemical Name:LY 341495
- CBNumber:CB0200679
- Molecular Formula:C20H19NO5
- Formula Weight:353.37
- MOL File:201943-63-7.mol
LY 341495 Property
- Boiling point 580.8±40.0 °C(Predicted)
- Density 1.432
- storage temp. Store at RT
- solubility Limited solubility, soluble in DMSO
- form crystalline solid
- pka 2.02±0.10(Predicted)
- color White to off-white
- FDA UNII AQ73SP6QSF
Safety
-
Symbol(GHS)
- Signal wordWarning
- Hazard statements H315-H319-H335
- Precautionary statements P261-P264-P271-P280-P302+P352-P304+P340-P305+P351+P338-P312-P321-P362+P364-P332+P313-P337+P313-P403+P233-P405-P501
LY 341495 Chemical Properties,Usage,Production
- 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™ .
-
in vivo
LY341495 (0.3, 1, and 3 mg/kg, i.p.) displays a lower level of discrimination in rats[1]. LY341495 (3.0 mg/kg) decreases Dvl-2, pGSK-3α/β and β-catenin protein levels but Dvl-1, Dvl-3 and GSK-3α/β are unaffected in both the PFC and STR. LY341495 has the generally the opposite effect following acute and chronic administration compared to mGlu2/3 agonist, LY379268[2]. LY341495 (3 mg/kg, i.p., 2.5 h) -induced c-Fos expression is not altered in either KO brain. LY341495 is almost inactive in the central extended amygdala [central nucleus of the amygdala, lateral (CeL) and bed nucleus of the stria terminalis, laterodorsal (BSTLD)] in mGluR3-KO mice[3].
- IC 50 mGluR1a: 7.8 μM (IC50); mGluR2: 21 nM (IC50); mGluR3: 14 nM (IC50); mGluR4: 22 μM (IC50); mGluR5a: 8.2 μM (IC50); mGluR7: 990 nM (IC50); mGluR8: 170 nM (IC50)
- storage Room temperature
-
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.
LY 341495 Preparation Products And Raw materials
Raw materials
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- 9H-Xanthene-9-propanoic acid, α-amino-α-[(1S,2S)-2-carboxycyclopropyl]-, (αS)-
- LY 341495;LY-341495
- (1S,2S)-2-[(1S)-1-amino-1-carboxy-2-(9H-xanthen-9-yl)ethyl]cyclopropane-1-carboxylic acid
- CS-416
- (alphaS)-alpha-Amino-alpha-[(1S,2S)-2-carboxycyclopropyl]-9H-xanthene-9-propanoic acid
- (alphaS)-alpha-Amino-alpha-[(1S,2S)-2-carboxycyclopropyl]-9H-xanthene-9-propanoic acid LY 341495
- (2S)-2-AMINO-2-[(1S,2S)-2-CARBOXYCYCLOPROP-1-YL]-3-(XANTH-9-YL) PROPANOIC ACID
- LY 341495