| Cas No.: | 198419-91-9 |
| Chemical Name: | LY 367385 |
| Synonyms: | Benzeneacetic acid, a-amino-4-carboxy-2-methyl-, (aS)-;LY 367385;AC1NSKBK;CHEBI:252690;CHEMBL94631;LY-367385;LY-367385 hydrochloride;PDSP1_001314;PDSP2_001298;SureCN661700;Tocris-1237;SGIKDIUCJAUSRD-QMMMGPOBSA-N;(S)-4-[aMino(carboxy)Methyl]-3-Methylbenzoic acid;(S)-(+)-α-Amino-4-carboxy-2-methylbenzeneaceticacid;(S)-(+)-a-amino-4-carboxy-2-methylbenzeneacetic acid;(R)-(+)-alpha-Amino-4-carboxy-2-methylbenzeneacetic acid;(S)-(+)-ALPHA-AMINO-4-CARBOXY-2-METHYLBENZENEACETIC ACID;LY367385;(S)-(+)-?-Amino-4-carboxy-2-methylbenzeneacetic acid;D8UW47H17B;4-[(S)-amino(carboxy)methyl]-3-methylbenzoic acid;(s)-(+)-alpha-amino-4-carboxy-2-methylbenzeneacetic acid;CS-0028681;SR-01000597418-1;2-methyl-4-carboxyphenylglycine;D04JQR;198419-91-9;SR-01000597418;NCGC00025067-01;NCGC00025067-02;(s)-2-methyl-4-carboxyphenylglycine;(S)-(+)-alpha-Amino-4-carboxy-2-methylbenzeneaceticacid;BENZENEACETIC ACID, .ALPHA.-AMINO-4-CARBOXY-2-METHYL-, (.ALPHA.S)-;Benzeneacetic acid, alpha-amino-4-carboxy-2-methyl-, (S)-;BDBM50084140;(S)-2-(4-Carboxy-2-methylphenyl)glycine;(S)-4-(amino(carboxy)methyl)-3-methylbenzoic acid;GTPL1379;Metabotropic mGluR1 agonists, Lilly;UNII-D8UW47H17B;YHA41991;BENZENEACETIC ACID, .ALPHA.-AMINO-4-CARBOXY-2-METHYL-, (S)-;4-((S)-AMINO(CARBOXY)METHYL)-3-METHYLBENZOIC ACID;HB0398;SCHEMBL661700;HY-107515;DTXSID2042563;(+)-2-methyl-4-carboxyphenylglycine;4-[(1S)-1-amino-2-hydroxy-2-oxoethyl]-3-methylbenzoic acid;J-012816;Benzeneacetic acid, alpha-amino-4-carboxy-2-methyl-, (alphaS)-;MS-23147;Q27083034;Benzeneacetic acid,a-amino-4-carboxy-2-methyl-,(as)-;4-((S)-Amino-carboxy-methyl)-3-methyl-benzoic acid;LY-367385 hydrochloride, >=98% (HPLC);AKOS015923884 |
| SMILES: | OC([C@H](C1C=CC(C(=O)O)=CC=1C)N)=O |
| Formula: | C10H11NO4 |
| M.Wt: | 209.198642969131 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | LY367385 is a highly potent and selective mGluR1a antagonist. LY367385 has an IC50 of 8.8 μM for inhibits of quisqualate-induced phosphoinositide (PI) hydrolysis, compared with > 100 μM for mGlu5a. LY367385 has neuroprotective, anticonvulsant and antiepileptic effects[1][2]. |
| Target: | mGluR1a:8.8 μM (IC50) |
| In Vivo: | LY367385 has been administered intracerebroventricularly (i.c.v.) to DBA/2 mice and lethargic mice (lh/lh), and focally into the inferior colliculus of genetically epilepsy prone rats (GEPR). In DBA/2 mice, LY367385 produces a rapid, transient suppression of sound-induced clonic seizures ED50 = 12 nM, i.c.v., 5 min). In lethargic mice, LY367385 significantly reduces the incidence of spontaneous spike and wave discharges on the electroencephalogram, from 30 to >150 min after the administration of LY367385, 250 nM, i.c.v[3]. In genetically epilepsy prone rats, LY367385 reduces sound-induced clonic seizures. LY367385, 160 nM bilaterally, fully suppresses clonic seizures after 2-4 h[3]. |
| In Vitro: | LY367385 combined with N-methyl-D-aspartate (NMDA) during the toxic pulse attenuates neuronal degeneration in a concentration-dependent fashion, with a maximal reduction of NMDA toxicity ranging from 40 to 60%. LY367385 shows greater efficacy than LY367366 and neither of these compounds influenced neuronal viability per se. LY367385 shows potent neuroprotective effects, with causing a 50% reduction in (S)-3,5-Dihydroxyphenylglycine (DHPG) potentiation at a concentration of 10 nM. Under experimental conditions at higher concentrations of antagonist, LY367385 a completely antagonized the amplification of NMDA toxicity by DHPG[2]. |
| References: | [1]. Clark et al. (+)-2-Methyl-4-carboxyphenylglycine (LY 367385) selectively antagonises metabotropic glutamate mGluR1 receptors. Bioorg.Med.Chem.Lett. November 1997, 7 (21): 2777-2780. [2]. Bruno V, et al. Neuroprotective activity of the potent and selective mGlu1a metabotropic glutamate receptor antagonist, (+)-2-methyl-4 carboxyphenylglycine (LY367385): comparison with LY357366, a broader spectrum antagonist with equal affinity for mGlu1a and mGlu5 receptors. Neuropharmacology. 1999 Feb;38(2):199-207. [3]. Chapman AG, et al. Anticonvulsant actions of LY 367385 ((+)-2-methyl-4-carboxyphenylglycine) and AIDA ((RS)-1-aminoindan-1,5-dicarboxylic acid). Eur J Pharmacol. 1999 Feb 26;368(1):17-24. |
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| 2018-0101 |
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| 2018-0101 |
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| 2018-0101 |
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